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Computationally Designed Carbonic Anhydrase Inhibitors Derived from Sulfonamides for Treatment of Glaucoma

Caruso, D. J.; Connolly, M. P.; Nguyen, T. Q.; Siegel, J. B.

2023-02-27 pharmacology and toxicology
10.1101/2023.02.25.529947 bioRxiv
Show abstract

Glaucoma is a known contributor to blindness in adults. This disease occurs as a result of overactivity of the carbonic anhydrase II (CAII) enzyme. Several of the commonly used sulfonamide drugs have been used to treat the symptoms of glaucoma but have been found to have low potency. To develop a more effective drug for the treatment of glaucoma, two novel CAII inhibitor drugs were designed through bioisoteric replacement and chemical intuition. This research discusses the development of these CAII inhibitor drugs from the existing glaucoma drug known as dichlorphenamide. The drugs created in this research were found to have a better docking score within the CAII binding site than that of dichlorphenamide. The drugs proposed in this paper would need to undergo further research to determine laboratory synthesis and potential clinical trialing.

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