o-desmethyl brinzolamide

O-desmethyl Brinzolamide is an active metabolite of the carbonic anhydrase (CA) inhibitor brinzolamide .1,2It inhibits CAII and CAIV (IC50s = 0.136 and 165 nM, respectively).1 1.Huang, Q., Rui, E.Y., Cobbs, M., et al.Design, synthesis, and evaluation of NO-donor containing carbonic anhydrase inhibitors to lower intraocular pressureJ. Med. Chem.58(6)2821-2833(2015) 2.Lo Faro, A.F., Tini, A., Gottardi, M., et al.Development and validation of a fast ultra-high-performance liquid chromatography tandem mass spectrometry method for determining carbonic anhydrase inhibitors and their metabolites in urine and hairDrug Test Anal.13(8)1552-1560(2021)

O-Desmethyl Brinzolamide hydrochloride (compound 6a) 作为Brinzolamide的主要活性代谢物，具有显著的碳酸酐酶 (carbonic anhydrase(CA)) 抑制活性，其 Kd 值为 0.136 nM，对 CA IV 的 IC50 值达到 165 nM。