66121-82-2Relevant academic research and scientific papers
Synthesis and evaluation of sulfonamide-bearing thiazole as carbonic anhydrase isoforms hCA I and hCA II
K?l?caslan, Soner,Arslan, Mustafa,Ruya, Zeynep,Bilen, ?igdem,Ergün, Adem,Gen?er, Nahit,Arslan, Oktay
, p. 1300 - 1305 (2016/10/09)
Sulfonamide-bearing thiazole compounds were synthesized and their inhibitory effects on the activity of purified human carbonic anhydrase I and II were evaluated. Human carbonic anhydrase isoenzymes (hCA-I and hCA-II) were purified from erythrocyte cells
A library of novel allosteric inhibitors against fructose 1,6-bisphosphatase
Heng, Sabrina,Gryncel, Kimberly R.,Kantrowitz, Evan R.
experimental part, p. 3916 - 3922 (2009/10/02)
The identification of a proper lead compound for fructose 1,6-bisphosphatase (FBPase) is a critical step in the process of developing novel therapeutics against type-2 diabetes. Herein, we have successfully generated a library of allosteric inhibitors against FBPase as potential anti-diabetic drugs, of which, the lead compound 1b was identified through utilizing a virtual high-throughput screening (vHTS) system, which we have developed. The thiazole-based core structure was synthesized via the condensation of α-bromo-ketones with thioureas and substituents on the two aryl rings were varied. 4c was found to inhibit pig kidney FBPase approximately fivefold better than 1b. In addition, we have also identified 10b, a tight binding fragment, which can be use for fragment-based drug design purposes.
