40353-60-4Relevant articles and documents
Synthesis, characterization, and study the inhibitory effect of thiazole and thiadiazole derivatives toward the corrosion of copper in acidic media
Tomi, Ivan Hameed R.,Al-Daraji, Ali H. R.,Aziz, Sherien A.
, (2015)
The authors describe the synthesis and characterization of two different five-member heterocycle derivatives (thiazole and thiadiazole) by several organic procedures. These compounds were characterized by FTIR, 1H NMR, and elemental analyses. A
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.