scholarly journals Synthesis and biological evaluation of benzenesulphonamide-bearing 1,4,5-trisubstituted-1,2,3-triazoles possessing human carbonic anhydrase I, II, IV, and IX inhibitory activity

2017 ◽  
Vol 32 (1) ◽  
pp. 1187-1194 ◽  
Author(s):  
Rajiv Kumar ◽  
Vikas Sharma ◽  
Silvia Bua ◽  
Claudiu T. Supuran ◽  
Pawan K. Sharma
Keyword(s):  
Carbonic Anhydrase ◽  
Inhibitory Activity ◽  
Biological Evaluation ◽  
Carbonic Anhydrase I ◽  
Human Carbonic Anhydrase ◽  
Synthesis And Biological Evaluation

scholarly journals Design, Synthesis, and Biological Evaluation of 1,2,3-Triazole-linked triazino[5,6-b]indole-benzene sulfonamide Conjugates as Potent Carbonic Anhydrase I, II, IX, and XIII Inhibitors

Metabolites ◽  
2020 ◽  
Vol 10 (5) ◽  
pp. 200
Author(s):  
Krishna Kartheek Chinchilli ◽  
Andrea Angeli ◽  
Pavitra S. Thacker ◽  
Laxman Naik Korra ◽  
Rashmita Biswas ◽  
...  
Keyword(s):  
Carbonic Anhydrase ◽  
Inhibitory Activity ◽  
Biological Evaluation ◽  
Moderate Activity ◽  
Design Synthesis ◽  
Carbonic Anhydrase I ◽  
Potent Inhibition ◽  
Lead Candidate ◽  
Synthesis And Biological Evaluation ◽  
Nanomolar Range

A series of 1,2,3-triazole-linked triazino[5,6-b]indole-benzene sulfonamide hybrids (6a–6o) was synthesized and evaluated for carbonic anhydrase (CA, EC 4.2.1.1) inhibitory activity against the human (h) isoforms hCA I, II, XIII (cytosolic isoforms), and hCA IX (transmembrane tumor-associated isoform). The results revealed that the compounds 6a–6o exhibited Ki values in the low to medium nanomolar range against hCA II and hCA IX (Kis ranging from 7.7 nM to 41.3 nM) and higher Ki values against hCA I and hCA XIII. Compound 6i showed potent inhibition of hCA II (Ki = 7.7nM), being more effective compared to the standard inhibitor acetazolamide (AAZ) (Ki = 12.1 nM). Compounds 6b and 6d showed moderate activity against hCA XIII (Ki = 69.8 and 65.8 nM). Hence, compound 6i could be consider as potential lead candidate for the design of potent and selective hCA II inhibitors.

scholarly journals Synthesis and biological evaluation of cyclic imides incorporating benzenesulfonamide moieties as carbonic anhydrase I, II, IV and IX inhibitors

2017 ◽  
Vol 25 (5) ◽  
pp. 1666-1671 ◽  
Author(s):  
Alaa A.-M. Abdel-Aziz ◽  
Andrea Angeli ◽  
Adel S. El-Azab ◽  
Mohamed A. Abu El-Enin ◽  
Claudiu T. Supuran
Keyword(s):  
Carbonic Anhydrase ◽  
Biological Evaluation ◽  
Carbonic Anhydrase I ◽  
Cyclic Imides ◽  
Synthesis And Biological Evaluation

Synthesis and Biological Evaluation of New 4-Thiazolidinone Derivatives as Carbonic Anhydrase Inhibitors

2017 ◽  
Vol 14 (2) ◽  
pp. 80-85 ◽  
Author(s):  
Hayriye Genc ◽  
Busra Ceken ◽  
Cigdem Bilen ◽  
Zubeyde Sackes ◽  
Nahit Gencer ◽  
...  
Keyword(s):  
Carbonic Anhydrase ◽  
Biological Evaluation ◽  
Carbonic Anhydrase Inhibitors ◽  
Synthesis And Biological Evaluation
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