1158142-60-9Relevant academic research and scientific papers
Synthesis and biochemical evaluation of triazole/tetrazole-containing sulfonamides against thrombin and related serine proteases
Siles, Rogelio,Kawasaki, Yuko,Ross, Patrick,Freire, Ernesto
, p. 5305 - 5309 (2011)
A small library of 25 triazole/tetrazole-based sulfonamides have been synthesized and further evaluated for their inhibitory activity against thrombin, trypsin, tryptase and chymase. In general, the triazole-based sulfonamides inhibited thrombin more efficiently than the tetrazole counterparts. Particularly, compound 26 showed strong thrombin inhibition (Ki = 880 nM) and significant selectivity against other human related serine proteases like trypsin (Ki = 729 μM). Thrombin binding affinity of the same compound was determined by ITC and demonstrated that the binding of this new triazole-based scaffold is enthalpically driven, making it a good candidate for further development.
