Natural product-inspired small molecule for the therapy of cognitive impairment associated with depressive disorder and other CNS diseases
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Non-nucleoside reverse transcriptase HIV-1 inhibitors
Small-molecule protein kinase inhibitors
Search for M. tuberculosis resuscitation promoting factor inhibitors
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Dispirotripiperazine as an unusual scaffold for new antivirals
Dispirotripiperazines are tricyclic molecules with two shared atoms, or “spiro atoms”. A unique feature of these compounds is the presence of two quaternary positively charged nitrogen atoms in their structure, the meaning of which is not fully understood and is the subject of study. It is assumed that these atoms may be responsible for electrostatic interactions with the negatively charged host cell-surface heparan sulfate residues, involving in host-pathogen interactions.
PDSTP, the most important member of this chemical class to date, inhibits in vitro a panel of viruses known to use heparan sulfate for early interaction with host cells. The molecule recently demonstrated fascinating efficacy in a rabbit model of herpes simplex epithelial keratitis.
This research is being carried out in partnership with the Charité – Berlin University of Medicine and the University of Cagliari.
Chemical probe C109 blocking the bacterial protein FtsZ
Chemical probe TP053 active against replicating and non-replicating M. tuberculosis
Small-molecule inhibitors of Picornaviridae entry
The common cold is predominantly caused by entero- or rhinoviruses. These viruses belonging to the Picornaviridae family have a so-called "pocket" on the viral capsid surface responsible for attachment to the host cell and subsequent infection. Being an attractive target, this pocket can be bonded by small molecules called "capsid binders".Our medicinal chemistry efforts are focused on a comprehensive structure-activity investigation of two distinct small-molecule scaffolds. The pyrazolo[3,4-d]pyrimidine-based OBR-5-340 and the pleconaril-core cmpd 10g (see ref #4), selected as lead molecules, are being studied in-depth.
Benzothiazinones as a promising class of potent anti-TB agents