3-Substituted thieno [2, 3-b][1, 4] thiazine-6-sulfonamides. A novel class of topically active carbonic anhydrase inhibitors

…, PJ Mallorga, SR Michelson, H Schwam…

Index: Hunt; Mallorga; Michelson; Schwam; Sondey; Smith; Sugrue; Shepard Journal of Medicinal Chemistry, 1994 , vol. 37, # 2 p. 240 - 247

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Citation Number: 21

Abstract

3-Aminoalkyl derivatives of thieno [2, 3-b][1, 41 thiazine-6-sulfonamide were prepared for evaluation as topically active ocular hypotensive agents. The compounds described were found to be excellent in vitro inhibitors of carbonic anhydrase I1 and in vivo to lower intraocular pressure in three rabbit models of ocular hypertension. Compounds 20A, 20B, and 20C metthe requirement of formulation as a 1% solution at pH 5.2, but none of the ...