Delving into the Latest Updates on Compound 49c(University of Geneva) with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms-

Target

PfPMX

Mechanism

PfPMX inhibitors(Plasmodium falciparum plasmepsin X inhibitors)

Therapeutic Areas

Infectious Diseases

Active Indication

Malaria

Inactive Indication-

Originator Organization

University of Geneva

Active Organization

University of Geneva

Inactive Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

Author: Dos Santos, Marina ; Bur, Daniel ; Seiler, Peter ; Boehme, Maria ; Zumbrunn, Cornelia ; Enderlin-Paput, Michel ; Kohl, Christopher ; Gaertner, Mika ; Delers, Jonathan ; Kaegi, Verena ; Locher, Hans ; Bruyère, Thierry ; Ritz, Daniel ; Gauvin, Jean-Christophe ; Keck, Wolfgang ; Mirre, Azely ; Surivet, Jean-Philippe ; Rueedi, Georg ; Hubschwerlen, Christian

There is an urgent need for new antibacterial drugs that are effective against infections caused by multidrug-resistant pathogens. Novel nonfluoroquinolone inhibitors of bacterial type II topoisomerases (DNA gyrase and topoisomerase IV) have the potential to become such drugs because they display potent antibacterial activity and exhibit no target-mediated cross-resistance with fluoroquinolones. Bacterial topoisomerase inhibitors that are built on a tetrahydropyran ring linked to a bicyclic aromatic moiety through a syn-diol linker show potent anti-Gram-positive activity, covering isolates with clinically relevant resistance phenotypes. For instance, analog 49c was found to be a dual DNA gyrase-topoisomerase IV inhibitor, with broad antibacterial activity and low propensity for spontaneous resistance development, but suffered from high hERG K(+) channel block. On the other hand, analog 49e displayed lower hERG K(+) channel block while retaining potent in vitro antibacterial activity and acceptable frequency for resistance development. Furthermore, analog 49e showed moderate clearance in rat and promising in vivo efficacy against Staphylococcus aureus in a murine infection model.

100 Deals associated with Compound 49c(University of Geneva)

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