Discovery of pyrazolthiazoles as novel and potent inhibitors of bacterial gyrase

Synthesis and applications of 2,4-disubstituted thiazole derivatives as small molecule modulators of cellular development

“…Procedures for the conversion of hydroxythiazoles to triflates are known 20 and have been 10 employed in the derivatisation of these compounds into biologically useful agents. 21 Initially, the Comins' reagent was used as the triflating agent; however, after stirring with 5 for 6 hours in tetrahydrofuran, TLC analysis showed predominately a mixture of starting materials.…”

Pyridine-3-carboxamide-6-yl-ureas as novel inhibitors of bacterial DNA gyrase: Structure based design, synthesis, SAR and antimicrobial activity

“…[6] More recently, the development of small molecule ATPase inhibitors of gyrase (GyrB) and topo IV (ParE), aided by the elucidation of proteinligand structures of GyrB, has gained attention as a means to inhibit these classical enzyme targets in the pursuit of novel antibacterial compounds. [7][8][9][10] Encouraged by these reports, our interest in the discovery of novel ATPase inhibitors of GyrB / ParE began with the observation that a number of reports in the literature demonstrated that heterocyclic N-ethylurea derivatives to be conducive with potent dualinhibitory ATPase activity coupled to antimicrobial activity. [7,8,10,11].…”

In-Vitro Antibacterial / Antifungal Screening of 2-Chloroquinoline Scaffold Derivatives

“…The benzimidazole derivatives (23)(24)(25)(26) showed moderate antifungal activity against the test strain C. albicans, A. niger and A. flavus was and there MIC observed at 25 to 50 µg/ml. To understand the mechanism of action underlying activity of most active compound 21, we proceeded to examine the interaction of compound 21 with bacterial DNA gyrase (PDB code: 3G75) [30]. All docking runs were carried out as per Glide XP Docking protocol in Schrodinger 9.4 [31,32].…”