On October 31, 1991, Shepard, Kenneth L.; Graham, Samuel L.; Hudcosky, Ronald J.; Michelson, Stuart R.; Scholz, Thomas H.; Schwam, Harvey; Smith, Anthony M.; Sondey, John M.; Strohmaier, Kim M. published an article.Name: 3-Nitro-4-chlorobenzenesulfonamide The title of the article was Topically active carbonic anhydrase inhibitors. 4. [(Hydroxyalkyl)sulfonyl]benzene and [(hydroxyalkyl)sulfonyl]thiophenesulfonamides. And the article contained the following:
For several decades a goal for the treatment of primary open-angle glaucoma has been the development of a topically active carbonic anhydrase inhibitor. (Hydroxyalkyl)sulfonyl-substituted benzene- and thiophenesulfonamides I [R = (CH2)nOH, CH2CH(OH)CH2OH, CH2CH2CMe2OH, etc., n = 2-5; R1 = H, Cl, F, NO2, CO2H, CO2Me, NH2; X = S, SO2] and II [R2 = (CH2)nOH, (CH2)mCO2Me, (CH2)3O2CCH2OMe, (CH2)3O2CCH2CHMe2, (CH2)3NHCH2CHMe2, X = S, SO2, n = 2-4, m = 2, 3] were prepared and examined for carbonic anhydrase inhibitory activity. Thus, condensation of 2-mercaptoethanol with (bromophenylsulfonyl)formamidine III gave I [R = (CH2)2OH, R1 = H, X = S]. These compounds exhibit inhibition of carbonic anhydrase II in the nanomolar range and lower intraocular pressure in the α-chymotrypsinized rabbit model of ocular hypertension after topical instillation. The inhibitory potency could be increased by converting a sulfide to the sulfone. Adding an extra methylene into the 4-substituent of benzene derivatives increases the inhibitory potency slightly more than oxidation of the sulfide. The experimental process involved the reaction of 3-Nitro-4-chlorobenzenesulfonamide(cas: 97-09-6).Name: 3-Nitro-4-chlorobenzenesulfonamide
The Article related to hydroxyalkylsulfonylbenzenesulfonamide preparation carbonic anhydrase inhibitor, hydroxyalkylsulfonylthiophenesulfonamide preparation carbonic anhydrase inhibitor, carbonic anhydrase inhibitor hydroxyalkylsulfonylbenzenesulfonamide hydroxyalkylsulfonylthiophenesulfonamide, glaucoma treatment alkylsulfonylbenzenesulfonamide thiophenesulfonamide and other aspects.Name: 3-Nitro-4-chlorobenzenesulfonamide
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