Kumar Rajiv, Bua Silvia, Ram Sita, Del Prete Sonia, Capasso Clemente, Supuran Claudiu T, Sharma Pawan K
Department of Chemistry, Kurukshetra University, Kurukshetra 136119, India.
Università degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm 188, and Neurofarba Department, Sezione di Scienze Farmaceutiche, Via U. Schiff 6, I-50019 Sesto Fiorentino (Firenze), Italy.
Bioorg Med Chem. 2017 Feb 1;25(3):1286-1293. doi: 10.1016/j.bmc.2016.12.047. Epub 2016 Dec 29.
Two series of 20 novel heterocyclic compounds, imidazothiadiazoles (3a-3j) and thiazolotriazoles (4a-4j) bearing benzenesulfonamide moiety were synthesized in order to investigate the inhibition potential of both scaffolds against four selected human carbonic anhydrase isoforms (hCA I, II, IX & XII). Against human isoform hCA I, compounds 3j, 4a-4c, and 4j showed better inhibition potential (K<100nM) than the standard drug acetazolamide (AZA). Against hCA II, all the compounds showed moderate inhibition with the exception of 3a which showed nearly two fold better profile compared to AZA. Against hCA IX, all the compounds showed moderate inhibitory potential than AZA, whereas against hCA XII, compounds 3a-3c showed better inhibitory potential compared to AZA.
为了研究两种骨架对四种选定的人类碳酸酐酶同工型（hCA I、II、IX和XII）的抑制潜力，合成了带有苯磺酰胺部分的两个系列的20种新型杂环化合物，即咪唑并噻二唑（3a - 3j）和噻唑并三唑（4a - 4j）。对于人类同工型hCA I，化合物3j、4a - 4c和4j显示出比标准药物乙酰唑胺（AZA）更好的抑制潜力（K<100nM）。对于hCA II，除3a外所有化合物均表现出中等抑制作用，3a的表现比AZA好近两倍。对于hCA IX，所有化合物的抑制潜力均比AZA中等，而对于hCA XII，化合物3a - 3c比AZA表现出更好的抑制潜力。
