Das Mahapatra, AmarjyotiAmarjyotiDas MahapatraQueen, AarfaAarfaQueenYousuf, MohdMohdYousufKhan, ParvezParvezKhanHussain, AfzalAfzalHussainRehman, Md TabishMd TabishRehmanAlajmi, Mohamed F.Mohamed F.AlajmiDatta, BhaskarBhaskarDattaHassan, Md ImtaiyazMd ImtaiyazHassan2025-08-312025-08-312022-01-0110.1080/07391102.2020.18458032-s2.0-85096100829https://repository.iitgn.ac.in/handle/IITG2025/2371233183174Inhibitors of carbonic anhydrase (CAIs) hold promise for addressing various diseases, including cancer, diabetes, and other metabolic syndromes. CAV is the only isoform present in the mitochondria and is considered a potential drug target for obesity. In this work, we have developed C2, and C4 substituted oxazole-5(4H)-one derivatives as a new scaffold for the selective inhibition of human carbonic anhydrase VA (hCAVA). Synthesized compounds were characterized by ¹H NMR, ¹³C NMR, and LC-MS mass spectrometry and subsequently evaluated for in vitro hCAVA inhibition. Two compounds, 4 and 5 showed a considerably higher binding affinity for hCAVA in comparison to the hCAII. Further, cell-based studies showed that these compounds decrease the expression of CAVA and GLUT4 in adipocytes and non-toxic to HEK293 cells. The present work opens a platform for the use of oxazole-5(4H)-ones and holds promise for further refinement of potent and selective hCAVA inhibitors. Communicated by Ramaswamy H. Sarma.en-USfalseCarbonic anhydrase inhibitors | carbonic anhydrase VA | drug discovery | obesity | oxazolone derivativesArticle153802543144-315420221012WOS:000588826300001