Synthesis and biological evaluation of novel N,N′-diaryl cyanoguanidines acting as potent and selective carbonic anhydrase II inhibitors

2018 ◽  
Vol 77 ◽  
pp. 245-251 ◽  
Author(s):  
Suleyman Akocak ◽  
Nabih Lolak ◽  
Silvia Bua ◽  
Idris Turel ◽  
Claudiu T. Supuran
Keyword(s):  
Carbonic Anhydrase ◽  
Biological Evaluation ◽  
Carbonic Anhydrase Ii ◽  
Synthesis And Biological Evaluation

scholarly journals Synthesis and Biological Evaluation of Imidazo[2,1-b]Thiazole based Sulfonyl Piperazines as Novel Carbonic Anhydrase II Inhibitors

Metabolites ◽  
2020 ◽  
Vol 10 (4) ◽  
pp. 136 ◽  
Author(s):  
Kesari Lakshmi Manasa ◽  
Sravya Pujitha ◽  
Aaftaab Sethi ◽  
Mohammed Arifuddin ◽  
Mallika Alvala ◽  
...  
Keyword(s):  
Carbonic Anhydrase ◽  
Biological Evaluation ◽  
Carbonic Anhydrase Ii ◽  
Stopped Flow ◽  
Inhibitory Potency ◽  
Standard Drug ◽  
Inhibition Constants ◽  
Synthesis And Biological Evaluation ◽  
Selective Activity

A novel series of imidazo[2,1-b]thiazole-sulfonyl piperazine conjugates (9aa-ee) has been synthesized and evaluated for carbonic anhydrase (CA, EC 4.2.1.1) inhibitory potency against four isoforms: The cytosolic isozyme hCA I, II and trans-membrane tumor-associated isoform hCA IX and hCA XII, taking acetazolamide (AAZ) as standard drug, using a stopped flow CO2 hydrase assay. The results revealed that most of the compounds showed selective activity against hCA II whereas none of them were active against hCA I, IX, XII (Ki > 100 µM). The physiologically dominant cytosolic isoform hCA II was inhibited by these molecules with inhibition constants in the range of 57.7–98.2 µM. This new derivative, thus, selectively inhibits hCA II over the hCA I, IX, XII isoforms, which may be used for further understanding the physiological roles of some of these isoforms in various pathologies.

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

Design, synthesis and biological evaluation of coumarin-3-carboxamides as selective carbonic anhydrase IX and XII inhibitors

2019 ◽  
Vol 86 ◽  
pp. 386-392 ◽  
Author(s):  
Pavitra S. Thacker ◽  
Mallika Alvala ◽  
Mohammed Arifuddin ◽  
Andrea Angeli ◽  
Claudiu T. Supuran
Keyword(s):  
Carbonic Anhydrase ◽  
Biological Evaluation ◽  
Carbonic Anhydrase Ix ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation
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