5657-42-1Relevant academic research and scientific papers
Synthesis and carbonic anhydrase I, II, VII, and IX inhibition studies with a series of benzo[d]thiazole-5- and 6-sulfonamides
Abdoli, Morteza,Angeli, Andrea,Bozdag, Murat,Carta, Fabrizio,Kakanejadifard, Ali,Saeidian, Hamid,Supuran, Claudiu T.
, p. 1071 - 1078 (2017/08/02)
A series of benzo[d]thiazole-5- and 6-sulfonamides has been synthesized and investigated for the inhibition of several human (h) carbonic anhydrase (CA, EC 4.2.1.1) isoforms, using ethoxzolamide (EZA) as lead molecule. 2-Amino-substituted, 2-acylamino- an
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.
THIAZOLE DERIVATIVES AND USE THEREOF
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Page/Page column 141, (2008/06/13)
The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.
THIAZOLE DERIVATIVES
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Page 32-33, (2010/02/06)
Compounds of formula (I) as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R4 have the significance given in claim 1 can be used in the form of pharmaceutical compositions.
