首页> 外文期刊>Journal of enzyme inhibition and medicinal chemistry. >Inhibition of human carbonic anhydrase isozymes I, II and VI with a series of bisphenol, methoxy and bromophenol compounds
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Inhibition of human carbonic anhydrase isozymes I, II and VI with a series of bisphenol, methoxy and bromophenol compounds

机译:用一系列双酚,甲氧基和溴酚化合物抑制人碳酸酐酶同工酶I,II和VI

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Carbonic anhydrase inhibitors (CAI) are valuable molecules as they have several therapeutic applications, including anti-glaucoma activity. In this study, inhibition of three human carbonic anhydrase (hCA, EC 4.2.1.1) isozymes I, II and VI with a series of bisphenol and bromophenol derivatives was investigated. Molecular docking studies of a set of such inhibitors within CA I and II were also performed. KI values of the molecules 2–9 were in the range of 10.025–892.109 μM for hCA I, 1.437–59.107 μM for hCA II and 11.143–919.182 μM for hCA VI, respectively. Reported inhibitory activities of molecules 2–9 will assist in better understanding of structure-activity relationship studies of CAI.
机译:碳酸酐酶抑制剂(CAI)是有价值的分子,因为它们具有多种治疗应用,包括抗青光眼活性。在这项研究中,研究了一系列双酚和溴酚衍生物对三种人类碳酸酐酶(hCA,EC 4.2.1.1)同工酶I,II和VI的抑制作用。还对CA I和II中的这类抑制剂进行了分子对接研究。分子2–9的K I 值在hCA I中为10.025–892.109μM,对于hCA II为1.437–59.107μM,对于hCA VI为11.143–919.182μM。报道的2-9分子的抑制活性将有助于更好地理解CAI的构效关系研究。

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