ArticleBioorganic & medicinal chemistry letters2011
Synthesis and biochemical evaluation of triazole/tetrazole-containing sulfonamides against thrombin and related serine proteases.
Article in Bioorganic & medicinal chemistry letters, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
4 citing papers in PubMed, 28 citations in OpenAlex.
- Copper-Catalyzed Synthesis of 4-CFMolecules (Basel, Switzerland) · 2024Article
- Towards Anticancer and Antibacterial Agents: Design and Synthesis of 1,2,3-Triazol-quinobenzothiazine Derivatives.International journal of molecular sciences · 2023Article
- Development of Orally Active Thrombin Inhibitors for the Treatment of Thrombotic Disorder Diseases.Molecules (Basel, Switzerland) · 2015Review
- Identification of protease inhibitors by a fast fluorimetric assay.Molecular biotechnology · 2013Article
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
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 (K(i)=880 nM) and significant selectivity against other human related serine proteases like trypsin (K(i)=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.
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