Structure-activity relationship of human carbonic anhydrase-II inhibitors: Detailed insight for future development as anti-glaucoma agents.

Structure-activity relationship of human carbonic anhydrase-II inhibitors: Detailed insight for future development as anti-glaucoma agents. Bioorg Chem. 2019 Dec 27;95:103557 Authors: Ghorai S, Pulya S, Ghosh K, Panda P, Ghosh B, Gayen S Abstract Human carbonic anhydrase-II (hCA-II) is the most dominant physiologic isoform amongst the sixteen reported hCA isoforms. Because of its high availability in the different anatomical, and cellular sites of the eye like retina and lens, it plays a more prominent role in the regulation of intraocular pressure than the other twelve catalytically active hCA isoforms. This isoform is also located in the brain, kidney, gastric mucosa, osteoclasts, RBCs, skeletal muscle, testes, pancreas, lungs, etc. Earlier, hCA-II inhibitors were designed based on the sulfonamides e.g. acetazolamide, dichlorphenamide, methazolamide, ethoxzolamide, etc. and they were used systemically in antiglaucoma therapy. Many successful attempts have been made by the researchers in order to design more potent and effective inhibitors by incorporating various moieties in sulphonamides. Some novel scaffolds like chalcones, thiophenes, organotellurium compounds, dithiocarbamate, selenide, and 2-benzylpyrazine, etc. were also designed as hCA-II inhibitors and their inhibitory efficacy was proved in the nanomolar range. In order to obtain relevant information from the insights of their structure-activity relationship, the reported ...
Source: Bioorganic Chemistry - Category: Chemistry Authors: Tags: Bioorg Chem Source Type: research