Study on Synthesis and Appraisal of Some 2,5-Disubstituted-1,3,4-Thiadiazoles as Diuretic Agents

Abstract

Acetazolamide and Methazolamide are well known 1,3,4-thiadiazole derivatives exhibiting diuretic activity. Therefore, some newer 2,5-disubstituted-1,3,4-thiadiazoles were prepared and screened for diuretic activity. A few of the compounds namely IVa1, IVb2 and IVc2 showed good diuretic activity comparable with the standard drug acetazolamide. Properties of the synthesized compounds were calculated by using the software Osiris property explorer (peo). Morphilino analogs (IVa3 – IVd3) showed higher Druglikeness and Drug Score as compared to other analogs. Among morphilino analogs IVa3 is the most active compound therefore selected for bioisosteric approach for newer analog design using molopt software.