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Design and synthesis of novel benzenesulfonamide containing 1,2,3-triazoles as potent human carbonic anhydrase isoforms I, II, IV and IX inhibitors by Kumar, Rajiv; Vats, Lalit; Bua, Silvia; Supuran, Claudiu T.; Sharma, Pawan K. is a Chemistry article available to read on EtoBox.

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In a quest to discover new biologically active compounds, a series of twenty novel heterocyclic derivatives substituted at position 5 with -H (7a-7j) or -CF (8a-8j), bearing benzenesulfonamide at N-1 position and various aroyl groups at position 4 of the 1,2,3-triazole ring was synthesized and screened for their carbonic anhydrase (CA, EC 4.2.1.1) inhibition potential against four human (h) isoforms hCA I, II, IV and IX. All the compounds (7a-7j and 8a-8j) were synthesized via [3+2] cycloaddition reaction from 4-azidobenzenesulfonamide. Interestingly, compounds 7a-7j were prepared in one pot manner via enaminone intermediate using novel methodology. All the newly synthesized compounds (7a-7j &8a-8j) were found to be excellent inhibitors of edema related isoform hCA I with their inhibition constant (K) ranging from 30.1 to 86.8 nM as compared to standard drug acetazolamide (AAZ) with K = 250 nM. Further it was found that most of tested compounds were weaker inhibitors of isoform, hCA II although compounds 7b, 7d-7e, 8a, 8d-8f, 8i (mostly with electron withdrawing substituents) have shown better inhibition potential (K < 50 nM). Against glaucoma associated hCA IV, compound 7d was fou

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Author

Kumar, Rajiv; Vats, Lalit; Bua, Silvia; Supuran, Claudiu T.; Sharma, Pawan K.

Publisher

Elsevier Science; Elsevier ; Elsevier BV (ISSN 0223-5234)

Published

2018

Language

EN

Field

Chemistry (Physical Sciences)