article · Journal of Medicinal Chemistry
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 <b>7c</b> disclosed the most potent activity (IC<sub>50</sub> = 0.63 nM) with high selectivity against CA II (605-fold than acetazolamide selectivity). Moreover, compound <b>7c</b> also showed significant in vivo IOP-reducing properties in the in vivo model of glaucoma. Furthermore, the binding of compound <b>7c</b> to CA II was assessed at the molecular level, exploiting the molecular docking approach.
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DOI: 10.1021/acs.jmedchem.3c02279
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