Drug intelligence / Profile preview

5-(2,4-dichlorophenylsulfonamido)-1,3,4-thiadiazole-2-sulfonamide

Development stage
Preclinical
Lead developer
Università degli Studi di Firenze
Modality
Small Molecules
Administration
Topical, Ophthalmic
01

Overview

5-(2,4-dichlorophenylsulfonamido)-1,3,4-thiadiazole-2-sulfonamide is a small molecule carbonic anhydrase inhibitor developed through a collaboration between the Università degli Studi di Firenze and the University of Florida. It is designed to treat glaucoma by inhibiting the isozymes Carbonic Anhydrase II (CA II) and Carbonic Anhydrase IV (CA IV), which are primarily responsible for the production of aqueous humor in the eye. Although the compound itself possesses potent inhibitory activity, its high lipophilicity and very low water solubility initially rendered it ineffective as a topical agent. However, when formulated as a complex with cyclodextrins (such as beta-cyclodextrin or hydroxypropyl-beta-cyclodextrin), the drug's solubility and corneal penetration are significantly enhanced, resulting in a potent and long-lasting reduction of intraocular pressure (IOP) in animal models of glaucoma.

Other names
5-(2,4-dichlorophenylsulfonamido)-1,3,4-thiadiazole-2-sulfonamide cyclodextrin complex
02

Targets

CA2 (Carbonic Anhydrase 2)CA4 (Carbonic anhydrase 4)CA7 (Carbonic anhydrase VII)CA1 (Carbonic anhydrase 1)

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