PUBLICATIONS

# equal contribution, * corresponding author
2024

Characterization of the dispirotripiperazine derivative PDSTP as antibiotic adjuvant and antivirulence compound against Pseudomonas aeruginosa
Bonacorsi A, Trespidi G, Scoffone VC, Irudal S, Barbieri G, Riabova O, Monakhova N, Makarov V, Buroni S*
Frontiers in Microbiology. 2024; 15: online

Molecular mechanism of rhinovirus escape from the pyrazolo[3,4-d]pyrimidine capsid-binding inhibitor OBR-5-340 via mutations distant from the binding pocket: derivatives that brake resistance
Richter M, Döring K, Blaas D, Riabova O, Khrenova M, Kazakova E, Egorova A, Makarov V*, Schmidtke M*
Antiviral Research. 2024; 222: 105810.

Antidepressant-like effect of the eburnamine-type molecule vindeburnol in rat and mouse models of ultrasound-induced depression
Zubkov E#, Riabova O#, Zorkina Y, Egorova A, Ushakova V, Lepioshkin A, Novoselova E, Abramova O, Morozova A, Chekhonin VP, Makarov V*
ACS Chemical Neuroscience. 2024; 15(3): 560-571
Highlighted in TASS, PRO Zdorovie, GxP News, Pharmprom, PharmMedProm, Pharmvestnik

Determination of alkaloid-inspired molecule vindeburnol in rabbit plasma by UPLC–HRMS and its application to pharmacokinetic studies and preliminary metabolite identification
Tsedilin A, Borets L, Riabova O, Kazakova E, Tafeenko V, Makarov V*
Journal of Pharmaceutical and Biomedical Analysis. 2024; 239: 115917

Benzothiozinone derivatives with anti-tubercular activity−further side chain investigation
Wu X, Wang W, Stelitano G, Riabova O, Wang B, Niu W, Cocorullo M, Shi R, Chiarelli LR, Makarov V, Lu Y, Li C, Qiao C
European Journal of Medicinal Chemistry. 2024; 264: 115976
Highlighted in BioWorld
2023

1‑Sulfonyl-3-amino‑1H‑1,2,4-triazoles as yellow fever virus inhibitors: synthesis and structure-activity relationship
Kazakova E#, Lane TR#, Jones J#, Puhl AC, Riabova O, Makarov V, Ekins S
ACS Omega. 2023; 8(45): 42951-42965

Synthesis and evaluation of 9-aminoacridines with SARS-CoV-2 antiviral activity
Jones T#, Monakhova N#, Guivel-Benhassine F, Lepioshkin L, Bruel T, Lane TR, Schwartz O, Puhl AC, Makarov V, Ekins S
ACS Omega. 2023; 8(43): 40817-40822

Antiviral evaluation of dispirotripiperazines against hepatitis B virus
Jones T, Tavis JE, Li Q, Riabova O, Monakhova N, Bradley DP, Lane TR, Makarov V, Ekins S
Journal of Medicinal Chemistry. 2023; 22(17): 12459-12467

Side chain-modified benzothiazinone derivatives with anti-mycobacterial activity
Fan D, Wang B, Stelitano G, Savková K, Riabova O, Shi R, Wu X, Chiarelli LR, Mikušová K, Makarov V*, Lu Y, Hong Y, Qiao C*
Biomedicines. 2023; 11(7): 1975

CanB, a druggable cellular target in Mycobacterium tuberculosis
Degiacomi G, Gianibbi B, Recchia D, Stelitano G, Truglio GI, Marra P, Stamilla A, Makarov V, Chiarelli LB, Manetti F, Pasca MR
ACS Omega. 2023; 8 (28): 25209-25220

Pyrrolo[2,3-e]indazole as a novel chemotype for both influenza A virus and pneumococcal neuraminidase inhibitors
Egorova A#, Richter M#, Khrenova M, Dietrich E, Tsedilin A, Kazakova E, Lepioshkin A, Jahn B, Chernyshev V, Schmidtke M, Makarov V*
RSC Advances. 2023; 13: 18253

Efficacy of an isoxazole-3-carboxamide analog of pleconaril in mouse models of Enterovirus-D68 and Coxsackie B5
Lane TR, Fu J, Sherry B, Tarbet B, Hurst BL, Riabova O, Kazakova E, Egorova A, Clarke P, Leser JS, Frost J, Rudy M, Tyler KL, Klose T, Volobueva AS, Belyaevskaya SV, Zarubaev VV, Kuhn RJ, Makarov V, Ekins S
Antiviral Research. 2023; 216: 105654
Highlighted in BioWorld

N-Phenyl-1-(phenylsulfonyl)-1H-1,2,4-triazol-3-amine as a new class of HIV-1 non-nucleoside reverse transcriptase inhibitor
Lane T#, Makarov V#*, Nelson JAE, Meeker RB, Sanna G, Riabova O, Kazakova E, Monakhova N, Tsedilin A, Urbina F, Jones T, Suchy A, Ekins S
Journal of Medicinal Chemistry. 2023; 66(9): 6193-6217
Highlighted in Forbes, Snob, N+1, Scientific Russia, Naked Science, PCR.news, Rossiyskaya Gazeta

Antituberculosis macozinone extended-release tablets to enhance bioavailability: a pilot pharmacokinetic study in Beagle dogs
Koryakova A, Shcherbakova V, Riabova O, Kazaishvili Y, Bolgarin R, Makarov V*
Microbiology Spectrum. 2023; 11(1): e0232722

Optimized LC-MS/MS quantification of tuberculosis drug candidate macozinone (PBTZ169), its dearomatized Meisenheimer Complex and other metabolites, in human plasma and urine
Desfontaine V, Guinchard S, Marques S, Vocat A, Moulfi F, Versace F, Huser-Pitteloud J, Ivanyuk A, Bardinet C, Makarov V, Ryabova O, André P, Prod'Hom S, Chtioui H, Buclin T, Cole ST, Decosterd L
Journal of Chromatography B. 2023; 1215: 123555
2022

A new benzothiazolthiazolidine derivative, 11726172, is active in vitro, in vivo, and against nonreplicating cells of Mycobacterium tuberculosis
Salina EG, Postiglione U, Chiarelli LR, Recchia D, Záhorszká M, Lepioshkin A, Monakhova N, Pál A, Porta A, Zanoni G, Korduláková J, Kazakova E, Sassera D, Pasca MR, Makarov V*, Degiacomi G
mSphere. 2022; 7(6): e0036922

Mycobacterium tuberculosis dormancy: how to fight a hidden danger
Salina EG, Makarov VA
Microorganisms. 2022, 10(12): 2334

Bactericidal and anti-biofilm activity of the FtsZ inhibitor C109 against Acinetobacter baumannii
Scoffone VC, Irudal S, Alshaar A, Piazza A, Trespidi G, Barbieri G, Makarov V, Migliavacca R, De Rossi E, Buroni S
Antibiotics. 2022; 11(11): 1571

New drugs and novel cellular targets against tuberculosis
Degiacomi G, Makarov V, Pasca MR, Chiarelli LR.
International Journal of Molecular Sciences. 2022; 23(22): 13680

Multiple approaches to repurposing drugs for neuroblastoma
Rank L, Puhl AC, Havener TM, Anderson E, Foil DH, Zorn KM, Monakhova N, Riabova O, Hickey AJ, Makarov V, Ekins S
Bioorganic & Medicinal Chemistry. 2022; 73: 117043

PDSTP is the first drug in class to treat coronavirus infection
Makarov VA*, Popov VO
Herald of the Russian Academy of Sciences. 2022; 92(4): 488-490

Broad-spectrum antiviral diazadispiroalkane core molecules block attachment and cell-to-cell spread of herpesviruses
Dohme A, Knoblauch M, Egorova A, Makarov V, Bogner E
Antiviral Research. 2022; 206: 105402
Highlighted in Russian Academy of Sciences, TASS

Dimethyl fumarate eliminates differentially culturable Mycobacterium tuberculosis in an intranasal murine model of tuberculosis
Glenn SM, Turapov O, Makarov V, Kell DB, Mukamolova GV.
Frontiers in Cellular and Infection Microbiology. 2022; 12: 957287

Thieno[2,3-d]pyrimidine-core compounds show activity against clinically relevant gram-positive bacteria
Riabova O, Egorova A, Lepioshkin A, Li Y, Voigt K, Kloss F, Makarov V*
ChemMedChem. 2022; 17(17): e202200207

Pyronaridine protects against SARS-CoV-2 infection in mouse
Puhl AC, Gomes GF, Damasceno S, Godoy AS, Noske GD, Nakamura AM, Gawriljuk VO, Fernandes RS, Monakhova N, Riabova O, Lane TR, Makarov V, Veras FP, Batah SS, Fabro AT, Oliva G, Cunha FQ, Alves-Filho JC, Cunha TM, Ekins S
ACS Infectious Diseases. 2022; 8(6): 1147-1160

A proof-of-concept study for the efficacy of dispirotripiperazine PDSTP in a rabbit model of herpes simplex epithelial keratitis
Alimbarova L#, Egorova A#, Riabova O, Monakhova N, Makarov V*
Antiviral Research. 2022; 202: 105327

Copper(II) complexes with terpene derivatives of ethylenediamine: synthesis, and antibacterial, antifungal and antioxidant activity
Gur'eva YA, Zalevskaya OA, Shevchenko OG, Slepukhin PA, Makarov VA, Kuchin AV
RSC Advances. 2022; 12(15): 8841-8851

Mycobacterium abscessus drug discovery using machine learning
Schmalstig AA, Zorn KM, Murcia S, Robinson A, Savina S, Komarova E, Makarov V, Braunstein M, Ekins S
Tuberculosis. 2022; 132: 102168

Machine learning models for Mycobacterium tuberculosis in vitro activity: prediction and target visualization`
Lane TR, Urbina F, Rank L, Gerlach J, Riabova O, Lepioshkin A, Kazakova E, Vocat A, Tkachenko V, Cole S, Makarov V, Ekins S
Molecular Pharmaceutics. 2022; 19(2): 674-689
2021

Targeting non-replicating Mycobacterium tuberculosis and latent infection: alternatives and perspectives (mini-review)
Egorova A, Salina EG, Makarov V*
International Journal of Molecular Sciences. 2021; 22(24): 13317

Antistaphylococcal activity of the FtsZ inhibitor C109
Trespidi G, Scoffone VC, Barbieri G, Marchesini F, Abualsha'ar A, Coenye T, Ungaro F, Makarov V, Migliavacca R, De Rossi E, Buroni S
Pathogens. 2021; 10(7): 886

Development of machine learning models and the discovery of a new antiviral compound against yellow fever virus
Gawriljuk VO, Foil DH, Puhl AC, Zorn KM, Lane TR, Riabova O, Makarov V, Godoy AS, Oliva G, Ekins S
Journal of Chemical Information and Modeling. 2021; 61(8): 3804-3813
Highlighted in Digital Health News, Poisk

Discovery of 5-Nitro-6-thiocyanatopyrimidines as Inhibitors of Cryptococcus neoformans and Cryptococcus gattii
Donlin MJ, Lane TR, Riabova O, Lepioshkin A, Xu E, Lin J, Makarov V, Ekins S
ACS Medicinal Chemistry Letters. 2021; 12(5): 774-781

Diazadispiroalkane derivatives are new viral entry inhibitors
Adfeldt R, Schmitz J, Kropff B, Thomas M, Monakhova N, Hölper JE, Klupp BG, Mettenleiter TC, Makarov V, Bogner E
Antimicrobial Agents and Chemotherapy. 2021; 65(4): e02103-20

Small molecules — prospective novel HCMV inhibitors
Bogner E, Egorova A, Makarov V
Viruses. 2021; 13(3): 474

Pipeline of anti-Mycobacterium abscessus small molecules: Repurposable drugs and promising novel chemical entities
Egorova A#, Jackson M#, Gavrilyuk V, Makarov V*
Medicinal Research Reviews. 2021; 41(4): 2350-2387

Nitric oxide-releasing compounds for the treatment of lung infections
Chiarelli LR, Degiacomi G, Egorova A, Makarov V, Pasca MR
Drug Dicovery Today. 2021; 26(2): 542-550

Dispirotripiperazine-core compounds, their biological activity with a focus on broad antiviral property, and perspectives in drug design (mini-review)
Egorova A, Bogner E, Novoselova E, Zorn KM, Ekins S, Makarov V*
European Journal of Medicinal Chemistry. 2021; 211: 113014

Design and synthesis of pyrano[3,2-b]indolones showing antimycobacterial activity
Monakhova N#, Korduláková J#, Vocat A#, Egorova A, Lepioshkin A, Salina EG, Nosek J, Repková E, Zemanová J, Jurdáková H, Górová R, Roh J, Degiacomi G, Sammartino JC, Pasca MR, Cole ST, Mikušová K*, Makarov V*
ACS Infectious Diseases. 2021; 7(1): 88-100
2020

6,11-Dioxobenzo[f]pyrido[1,2-a]indoles kill Mycobacterium tuberculosis by targeting iron-sulfur protein Rv0338c (IspQ), a putative redox sensor
Székely R, Rengifo-Gonzalez M, Singh V, Riabova O, Benjak A, Piton J, Cimino M, Kornobis E, Mizrahi V, Johnsson K, Manina G, Makarov V, Cole ST
ACS Infectious Diseases 2020; 6(11): 3015-3025

WIN compounds: on the way to efficient antipicornaviral agent. A historical survey
Egorova AP, Makarov VA*
Russian Chemical Bulletin. 2020; 69: 635-646

Molecule property analyses of active compounds for Mycobacterium tuberculosis
Makarov V, Salina E, Reynolds RC, Kyaw Zin PP, Ekins S
Journal of Medicinal Chemistry. 2020; 63(17): 8917-8955

Chemical, metabolic, and cellular characterization of a FtsZ inhibitor effective against Burkholderia cenocepacia
Chiarelli LR, Scoffone VC, Trespidi G, Barbieri G, Riabova O, Monakhova N, Porta A, Manina G, Riccardi G, Makarov V, Buroni S
Front Microbiol. 2020; 11: 562

Development of macozinone for TB treatment: an update
Makarov V*, Mikušová K.
Applied Sciences. 2020; 10(7): 2269

The evolution of pleconaril: modified O-alkyl linker analogs have biological activity towards Coxsackievirus B3 Nancy
Volobueva A, Egorova A, Galochkina A, Ekins S, Zarubaev V, Makarov V*
Molecules. 2020; 25(6): 1345

The cell division protein FtsZ as a cellular target to hit cystic fibrosis pathogens
Buroni S, Makarov V, Scoffone VC, Trespidi G, Riccardi G, Chiarelli LR
European Journal of Medicinal Chemistry. 2020; 190: 112132

Rv0579 is involved in the resistance to the TP053 antitubercular prodrug
Mori G, Orena BS, Chiarelli LR, Degiacomi G, Riabova O, Sammartino JC, Makarov V, Riccardi G, Pasca MR
Frontiers in Microbiology. 2020; 11: 292

Novel pleconaril derivatives: Influence of substituents in the isoxazole and phenyl rings on the antiviral activity against enteroviruses
Egorova A, Kazakova E, Jahn B, Ekins S, Makarov V*, Schmidtke M*
European Journal of Medicinal Chemistry. 2020; 188: 112007

New 2-ethylthio-4-methylaminoquinazoline derivatives inhibiting two subunits of cytochrome bc1 in Mycobacterium tuberculosis
Lupien A, Foo CS, Savina S, Vocat A, Piton J, Monakhova N, Benjak A, Lamprecht DA, Steyn AJC, Pethe K, Makarov VA*, Cole ST
PLoS Pathogens. 2020; 16(1): e1008270

PEGylated mucus-penetrating nanocrystals for lung delivery of a new FtsZ inhibitor against Burkholderia cenocepacia infection
Costabile G, Provenzano R, Azzalin A, Scoffone VC, Chiarelli LR, Rondelli V, Grillo I, Zinn T, Lepioshkin A, Savina S, Miro A, Quaglia F, Makarov V, Coenye T, Brocca P, Riccardi G, Buroni S, Ungaro F
Nanomedicine. 2020; 23: 102113

New insights into the mechanism of action of the thienopyrimidine antitubercular prodrug TP053
Chiarelli LR, Salina EG, Mori G, Azhikina T, Riabova O, Lepioshkin A, Grigorov A, Forbak M, Madacki J, Orena BS, Manfredi M, Gosetti F, Buzzi A, Degiacomi G, Sammartino JC, Marengo E, Korduláková J, Riccardi G, Mikušová K, Makarov V*, Pasca MR
ACS Infectious Diseases. 2020; 6(2): 313-323
2019

Specific antiviral activity of pyrimidinedispirotripiperazinium alone and in combination with acyclovir on a herpes-simplex-virus model
Novoselova EA, Ryabova OB, Leneva IA, Makarov VA
Pharmaceutical Chemistry Journal. 2019; 53: 781-785

Mycobacterium abscessus, an emerging and worrisome pathogen among cystic fibrosis patients
Degiacomi G, Sammartino JC, Chiarelli LR, Riabova O, Makarov V, Pasca MR
International Journal of Molecular Sciences. 2019; 20(23): 5868

The effect of 2-thiocyanatopyridine derivative 11026103 on Burkholderia cenocepacia: resistance mechanisms and systemic impact
Nunvar J, Hogan AM, Buroni S, Savina S, Makarov V, Cardona ST, Drevinek P.
Antibiotics. 2019; 8(4): 159

Back to the future: Advances in development of broad-spectrum capsid-binding inhibitors of enteroviruses
Egorova A, Ekins S, Schmidtke M, Makarov V*
European Journal of Medicinal Chemistry. 2019; 178: 606-622

Cryo-EM structure of pleconaril-resistant rhinovirus-B5 complexed to the antiviral OBR-5-340 reveals unexpected binding site
Wald J, Pasin M, Richter M, Walther C, Mathai N, Kirchmair J, Makarov VA, Goessweiner-Mohr N, Marlovits TC, Zanella I, Real-Hohn A, Verdaguer N, Blaas D, Schmidtke M
Proceedings of the National Academy of Sciences. 2019; 116(38): 19109-19115

Development and validation of a multiplex UHPLC-MS/MS method for the determination of the investigational antibiotic against multi-resistant tuberculosis macozinone (PBTZ169) and five active metabolites in human plasma
Spaggiari D, Desfontaine V, Cruchon S, Guinchard S, Vocat A, Blattes E, Pitteloud J, Ciullini L, Bardinet C, Ivanyuk A, Makarov V, Ryabova O, Buclin T, Cole ST, Decosterd LA
PLoS One. 2019; 14(5): e0217139

New targets for HIV drug discovery
Puhl AC, Garzino Demo A, Makarov VA, Ekins S
Drug Discovery Today. 2019; 24(5): 1139-1147

Multiple machine learning comparisons of HIV cell-based and reverse transcriptase data sets
Zorn KM, Lane TR, Russo DP, Clark AM, Makarov V, Ekins S
Molecular Pharmaceutics. 2019; 16(4): 1620-1632

A rapid method for estimation of the efficacy of potential antimicrobials in humans and animals by agar diffusion assay
Salina EG, Ekins S, Makarov VA*
Chemical Biology & Drug Design. 2019; 93(6): 1021-1025
2018

How to kill dormant Mycobacterium tuberculosis
Kaprelyants AS, Salina EG, Makarov VA
International Journal of Mycobacteriology. 2018; 7(4): 399-400

Thienopyrimidines are new nitrogen donors highly active against Mycobacterium tuberculosis
Salina EG, Chiarelli LR, Pasca MR, Makarov VA
Bulletin of the Central Tuberculosis Research Institute. 2018; 4: 17-22 [In Russian]

Competitive fitness of essential gene knockdowns reveals a broad-spectrum antibacterial inhibitor of the cell division protein FtsZ
Hogan AM, Scoffone VC, Makarov V, Gislason AS, Tesfu H, Stietz MS, Brassinga AKC, Domaratzki M, Li X, Azzalin A, Biggiogera M, Riabova O, Monakhova N, Chiarelli LR, Riccardi G, Buroni S, Cardona ST
Antimicrobial Agents and Chemotherapy. 2018; 62(12): e01231-18

Optimized background regimen for treatment of active tuberculosis with the next-generation benzothiazinone macozinone (PBTZ169)
Lupien A, Vocat A, Foo CS, Blattes E, Gillon JY, Makarov V, Cole ST
Antimicrobial Agents and Chemotherapy. 2018; 62(11): e00840-18

Fluorescent benzothiazinone analogues efficiently and selectively label DprE1 in mycobacteria and actinobacteria
Sommer R, Neres J, Piton J, Dhar N, van der Sar A, Mukherjee R, Laroche T, Dyson PJ, McKinney JD, Bitter W, Makarov V, Cole ST
ACS Chemical Biology. 2018; 13(11): 3184-3192

Structure-based drug design and characterization of sulfonyl-piperazine benzothiazinone inhibitors of DprE1 from Mycobacterium tuberculosis
Piton J, Vocat A, Lupien A, Foo CS, Riabova O, Makarov V, Cole ST
Antimicrobial Agents and Chemotherapy. 2018; 62(10): e00681-18

Investigating the mechanism of action of diketopiperazines inhibitors of the Burkholderia cenocepacia quorum sensing synthase CepI: a site-directed mutagenesis study
Buroni S, Scoffone VC, Fumagalli M, Makarov V, Cagnone M, Trespidi G, De Rossi E, Forneris F, Riccardi G, Chiarelli LR
Frontiers in Pharmacology. 2018; 9: 836

Copper-related toxicity in replicating and dormant Mycobacterium tuberculosis caused by 1-hydroxy-5-R-pyridine-2(1H)-thiones
Salina EG, Huszár S, Zemanová J, Keruchenko J, Riabova O, Kazakova E, Grigorov A, Azhikina T, Kaprelyants A, Mikušová K, Makarov V
Metallomics. 2018; 10(7): 992-1002

Vindeburnol's influence on the neurologic status and morphological changes in the brain of rats in model of experimental allergic encephalomyelitis
Karantysh GV, Gafiyatullina GS, Mendzheritskii AM, Prokofev VN, Zhukova MV, Makarov VA
Modern problems of science and education. Surgery. 2018; 1: 84 [In Russian]

A multitarget approach to drug discovery inhibiting Mycobacterium tuberculosis PyrG and PanK
Chiarelli LR, Mori G, Orena BS, Esposito M, Lane T, de Jesus Lopes Ribeiro AL, Degiacomi G, Zemanová J, Szádocka S, Huszár S, Palčeková Z, Manfredi M, Gosetti F, Lelièvre J, Ballell L, Kazakova E, Makarov V, Marengo E, Mikusova K, Cole ST, Riccardi G, Ekins S, Pasca MR.
Scientific Reports. 2018; 8(1): 3187
2017

Benzoylphenyl thiocyanates are new, effective inhibitors of the mycobacterial resuscitation promoting factor B protein
Demina GR, Nikitushkin VD, Shleeva MO, Riabova OB, Lepioshkin AY, Makarov VA, Kaprelyants AS
Annals of Clinical Microbiology and Antimicrobials. 2017; 16(1): 69

New 1-hydroxy-2-thiopyridine derivatives active against both replicating and dormant Mycobacterium tuberculosis
Salina EG, Ryabova O, Vocat A, Nikonenko B, Cole ST, Makarov V
Journal of Infection and Chemotherapy. 2017; 23(11): 794-797

NOS2-deficient mice with hypoxic necrotizing lung lesions predict outcomes of tuberculosis chemotherapy in humans
Gengenbacher M, Duque-Correa MA, Kaiser P, Schuerer S, Lazar D, Zedler U, Reece ST, Nayyar A, Cole ST, Makarov V, Barry III CE, Dartois V, Kaufmann SHE
Scientific Reports. 2017; 7(1): 8853

The antibacterial prodrug activator Rv2466c is a mycothiol-dependent reductase in the oxidative stress response of Mycobacterium tuberculosis
Rosado LA, Wahni K, Degiacomi G, Pedre B, Young D, de la Rubia AG, Boldrin F, Martens E, Marcos-Pascual L, Sancho-Vaello E, Albesa-Jové D, Provvedi R, Martin C, Makarov V, Versées W, Verniest G, Guerin ME, Mateos LM, Manganelli R, Messens J
Journal of Biological Chemistry. 2017; 292(32): 13097-13110

Cmr is a redox-responsive regulator of DosR that contributes to M. tuberculosis virulence
Smith LJ, Bochkareva A, Rolfe MD, Hunt DM, Kahramanoglou C, Braun Y, Rodgers A, Blockley A, Coade S, Lougheed KEA, Hafneh NA, Glenn SM, Crack JC, Le Brun NE, Saldanha JW, Makarov V, Nobeli I, Arnvig K, Mukamolova GV, Buxton RS, Green J
Nucleic Acids Research. 2017; 45(11): 6600-6612

Antiretroviral activity of a novel pyrimidyl-di(diazaspiroalkane) derivative
Novoselova EA, Riabova OB, Leneva IA, Nesterenko VG, Bolgarin RN, Makarov VA
Acta Naturae. 2017; 9(1): 105-107
2016

Killing two birds with one stone — Prenylated flavonoids disrupt the lethal synergism of influenza A viruses and pneumococci
Grienke U, Richter M, Walther E, Hoffmann A, Kirchmair J, Makarov V, Nietzsche S, Schmidtke M, Rollinger JM
Planta Medica. 2016; 82(S 01): S1-S381

Discovery of new diketopiperazines inhibiting Burkholderia cenocepacia quorum sensing in vitro and in vivo
Scoffone VC, Chiarelli LR, Makarov V, Brackman G, Israyilova A, Azzalin A, Forneris F, Riabova O, Savina S, Coenye T, Riccardi G, Buroni S
Scientific Repots. 2016; 6: 32487

Discovery of prenylated flavonoids with dual activity against influenza virus and Streptococcus pneumoniae
Grienke U, Richter M, Walther E, Hoffmann A, Kirchmair J, Makarov V, Nietzsche S, Schmidtke M, Rollinger JM
Scientific Reports. 2016; 6: 27156

Synthesis and biological properties of pyrrolo[1,2-a]indoles
Monakhova N, Ryabova S, Makarov V*
Journal of Heterocyclic Chemistry. 2016; 53(3): 685-709
2015

The redox state regulates the conformation of Rv2466c to activate the antitubercular prodrug TP053
Albesa-Jové D, Comino N, Tersa M, Mohorko E, Urresti S, Dainese E, Chiarelli LR, Pasca MR, Manganelli R, Makarov V, Riccardi G, Svergun DI, Glockshuber R, Guerin ME
Journal of Biological Chemistry. 2015; 290(52): 31077-31089

Molecular mechanism of a specific capsid binder resistance caused by mutations outside the binding pocket
Braun H, Kirchmair J, Williamson MJ, Makarov VA, Riabova OB, Glen RC, Sauerbrei A, Schmidtke M
Antiviral Research. 2015; 123: 138-145

In vivo activity of the benzothiazinones PBTZ169 and BTZ043 against Nocardia brasiliensis
González-Martínez NA, Lozano-Garza HG, Castro-Garza J, De Osio-Cortez A, Vargas-Villarreal J, Cavazos-Rocha N, Ocampo-Candiani J, Makarov V, Cole ST, Vera-Cabrera L
PLOS Neglected Tropical Diseases. 2015; 9(10): e0004022

Pyrazolopyrimidines: potent inhibitors targeting the capsid of rhino- and enteroviruses
Makarov VA, Braun H, Richter M, Riabova OB, Kirchmair J, Kazakova ES, Seidel N, Wutzler P, Schmidtke M
ChemMedChem. 2015; 10(10): 1629-1634

Efflux-mediated resistance to a benzothiadiazol derivative effective against Burkholderia cenocepacia
Scoffone VC, Ryabova O, Makarov V, Iadarola P, Fumagalli M, Fondi M, Fani R, De Rossi E, Riccardi G, Buroni S
Frontiers in Microbiology. 2015; 6: 815

Thiophenecarboxamide derivatives activated by EthA kill Mycobacterium tuberculosis by inhibiting the CTP synthetase PyrG
Mori G, Chiarelli LR, Esposito M, Makarov V, Bellinzoni M, Hartkoorn RC, Degiacomi G, Boldrin F, Ekins S, de Jesus Lopes Ribeiro AL, Marino LB, Centárová I, Svetlíková Z, Blaško J, Kazakova E, Lepioshkin A, Barilone N, Zanoni G, Porta A, Fondi M, Fani R, Baulard AR, Mikušová K, Alzari PM, Manganelli R, de Carvalho LP, Riccardi G, Cole ST, Pasca MR
Chemistry & Biology. 2015; 22(7): 917-927

The 8-pyrrole-benzothiazinones are noncovalent inhibitors of DprE1 from Mycobacterium tuberculosis
Makarov V, Neres J, Hartkoorn RC, Ryabova OB, Kazakova E, Šarkan M, Huszár S, Piton J, Kolly GS, Vocat A, Conroy TM, Mikušová K, Cole ST
Antimicrobial Agents and Chemotherapy. 2015; 59(8): 4446-4452

2-Carboxyquinoxalines kill Mycobacterium tuberculosis through noncovalent inhibition of DprE1
Neres J, Hartkoorn RC, Chiarelli LR, Gadupudi R, Pasca MR, Mori G, Venturelli A, Savina S, Makarov V, Kolly GS, Molteni E, Binda C, Dhar N, Ferrari S, Brodin P, Delorme V, Landry V, de Jesus Lopes Ribeiro AL, Farina D, Saxena P, Pojer F, Carta A, Luciani R, Porta A, Zanoni G, De Rossi E, Costi MP, Riccardi G, Cole ST
ACS Chemical Biology. 2015; 10(3): 705-714
2014

The in vivo environment accelerates generation of resuscitation-promoting factor-dependent mycobacteria
Turapov O, Glenn S, Kana B, Makarov V, Andrew PW, Mukamolova GV
American Journal of Respiratory and Critical Care Medicine. 2014; 190(12): 1455-1457

Towards a new combination therapy for tuberculosis with next generation benzothiazinones
Makarov V, Lechartier B, Zhang M, Neres J, van der Sar AM, Raadsen SA, Hartkoorn RC, Ryabova OB, Vocat A, Decosterd LA, Widmer N, Buclin T, Bitter W, Andries K, Pojer F, Dyson PJ, Cole ST
EMBO Molecular Medicine. 2014; 6(3): 372-383
Highlighted in Medical Xpress, Medical News, Working Group on New TB Drugs, Financial Times, l'Actualité Chimique

Mechanism of resistance to an antitubercular 2-thiopyridine derivative that is also active against Burkholderia cenocepacia
Scoffone VC, Spadaro F, Udine C, Makarov V, Fondi M, Fani R, De Rossi E, Riccardi G, Buroni S
Antimicrobial Agents and Chemotherapy. 2014; 58(4): 2415-2417

DSTP-27 prevents entry of human cytomegalovirus
Paeschke R, Woskobojnik I, Makarov V, Schmidtke M, Bogner E
Antimicrobial Agents and Chemotherapy. 2014; 58(4): 1963-1971

Rv2466c mediates the activation of TP053 to kill replicating and non-replicating Mycobacterium tuberculosis
Albesa-Jové D, Chiarelli LR, Makarov V, Pasca MR, Urresti S, Mori G, Salina E, Vocat A, Comino N, Mohorko E, Ryabova S, Pfieiffer B, Lopes Ribeiro AL, Rodrigo-Unzueta A, Tersa M, Zanoni G, Buroni S, Altmann KH, Hartkoorn RC, Glockshuber R, Cole ST, Riccardi G, Guerin ME
ACS Chemical Biology. 2014; 9(7): 1567-1575

Mechanism of action of 5-nitrothiophenes against Mycobacterium tuberculosis
Hartkoorn RC, Ryabova OB, Chiarelli LR, Riccardi G, Makarov V, Cole ST
Antimicrobial Agents and Chemotherapy. 2014; 58(5): 2944-2947

New 2-thiopyridines as potential candidates for killing both actively growing and dormant Mycobacterium tuberculosis cells
Salina E, Ryabova O, Kaprelyants A, Makarov V
Antimicrobial Agents and Chemotherapy. 2014; 58(1): 55-60

DprE1 — from the discovery to the promising tuberculosis drug target
Mikusová K, Makarov V, Neres J

Current Pharmaceutical Design. 2014; 20(27): 4379-403

2013

Amphiphilic star-shaped block copolymers as unimolecular drug delivery systems: investigations using a novel fungicide
Knop K, Pavlov GM, Rudolph T, Martin K, Pretzel D, Jahn BO, Scharf DH, Brakhage AA, Makarov V, Mollmann U, Schacher FH, Schubert US
Soft Matter. 2013; 9 : 715-726

Molecular determinants of inactivation of the resuscitation promoting factor B from Mycobacterium tuberculosis
Ruggiero A, Marchant J, Squeglia F, Makarov V, De Simone A, Berisio R
Journal of Biomolecular Structure and Dynamics. 2013; 31(2): 195-205
2012

Resuscitation-promoting factors (Rpf): in search of inhibitors
Kaprelyants AS, Mukamolova GV, Ruggiero A, Makarov VA, Demina GR, Shleeva MO, Potapov VD, Shramko PA

Protein & Peptide Letters. 2012; 19(10): 1026-1034


Synthesis of pyrazolo[3,4-b]pyridine-6-ones
Komarova E, Makarov V, Granik V, Párkányi C
Journal of Heterocyclic Chemistry. 2012; 4(5): 969-998

Benzothiazinones are suicide inhibitors of mycobacterial decaprenylphosphoryl-β-D-ribofuranose 2'-oxidase DprE1
Trefzer C, Škovierová H, Buroni S, Bobovská A, Nenci S, Molteni E, Pojer F, Pasca MR, Makarov V, Cole ST, Riccardi G, Mikušová K, Johnsson K
Journal of the American Chemical Society. 2012; 134(2): 912-915
2011

QSAR analysis of [(biphenyloxy)propyl]isoxazoles: agents against coxsackievirus B3
Muratov EN, Varlamova EV, Artemenko AG, Khristova T, Kuz'min VE, Makarov VA, Riabova OB, Wutzler P, Schmidtke M
Future Medicinal Chemistry. 2011; 3(1): 15-27
2010

Benzothiazinones: prodrugs that covalently modify the decaprenylphosphoryl-β-D-ribose 2'-epimerase DprE1 of Mycobacterium tuberculosis
Trefzer C, Rengifo-Gonzalez M, Hinner MJ, Schneider P, Makarov V, Cole ST, Johnsson K
Journal of the American Chemical Society. 2010; 132(39): 13663-13665

Biological and structural characterization of the Mycobacterium smegmatis nitroreductase NfnB, and its role in benzothiazinone resistance
Manina G, Bellinzoni M, Pasca MR, Neres J, Milano A, Ribeiro AL, Buroni S, Skovierová H, Dianišková P, Mikušová K, Marák J, Makarov V, Giganti D, Haouz A, Lucarelli AP, Degiacomi G, Piazza A, Chiarelli LR, De Rossi E, Salina E, Cole ST, Alzari PM, Riccardi G
Molecular Microbiology. 2010; 77(5): 1172-1185

Per aspera ad astra: application of simplex QSAR approach in antiviral research
Muratov EN, Artemenko AG, Varlamova EV, Polischuk PG, Lozitsky VP, Fedchuk AS, Lozitska RL, Gridina TL, Koroleva LS, Sil'nikov VN, Galabov AS, Makarov VA, Riabova OB, Wutzler P, Schmidtke M, Kuz'min VE
Future Medicinal Chemistry. 2010; 2(7): 1205-1226

Clinical isolates of Mycobacterium tuberculosis in four European hospitals are uniformly susceptible to benzothiazinones
Pasca MR, Degiacomi G, Ribeiro AL, Zara F, De Mori P, Heym B, Mirrione M, Brerra R, Pagani L, Pucillo L, Troupioti P, Makarov V, Cole ST, Riccardi G
Antimicrobial Agents and Chemotherapy. 2010; 54(4): 1616-1618
2009

Finding of the low molecular weight inhibitors of resuscitation promoting factor enzymatic and resuscitation activity
Demina GR, Makarov VA, Nikitushkin VD, Ryabova OB, Vostroknutova GN, Salina EG, Shleeva MO, Goncharenko AV, Kaprelyants AS
PLoS One. 2009; 4(12): e8174

Benzothiazinones kill Mycobacterium tuberculosis by blocking arabinan synthesis
Makarov V#, Manina G#, Mikusova K#, Möllmann U#, Ryabova O, Saint-Joanis B, Dhar N, Pasca MR, Buroni S, Lucarelli AP, Milano A, De Rossi E, Belanova M, Bobovska A, Dianiskova P, Kordulakova J, Sala C, Fullam E, Schneider P, McKinney JD, Brodin P, Christophe T, Waddell S, Butcher P, Albrethsen J, Rosenkrands I, Brosch R, Nandi V, Bharath S, Gaonkar S, Shandil RK, Balasubramanian V, Balganesh T, Tyagi S, Grosset J, Riccardi G, Cole ST
Science. 2009; 324(5928): 801-804
Highlighted in Nature Reviews Drug Discovery, Reuters

New pleconaril and [(biphenyloxy)propyl]isoxazole derivatives with substitutions in the central ring exhibit antiviral activity against pleconaril-resistant coxsackievirus B3
Schmidtke M, Wutzler P, Zieger R, Riabova OB, Makarov VA
Antiviral Research. 2009; 81(1): 56-63