化学
碳酸酐酶
哒嗪
药理学
磺胺
立体化学
组合化学
酶
生物化学
医学
作者
Haytham O. Tawfik,Mohamed M. Saleh,Andrea Ammara,Eman F. Khaleel,Rehab Mustafa Badi,Yomna Khater,Rabab Ahmed Rasheed,Ahmed Attia,Salma M. Hefny,Eslam B. Elkaeed,Alessio Nocentini,Claudiu T. Supuran,Wagdy M. Eldehna,Moataz A. Shaldam
标识
DOI:10.1021/acs.jmedchem.3c02279
摘要
As a progressive neuropathic condition, glaucoma can cause lifelong blindness if left untreated. Novel phenylpyridazine-tethered sulfonamides were designed as selective inhibitors for carbonic anhydrase (CA) isoform II to find effective therapeutic agents for glaucoma. Subsequently, the target inhibitors were synthesized and assessed for their inhibitory action against cytosolic CA I and II. Interestingly, the synthesized molecules poorly inhibited CA I while exhibiting low subnanomolar potency against CA II. Compound
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