Microwave-assisted synthesis of double-headed derivatives of (4-amino-5-mercapto-4H-1,2,4-triazol-3-yl)-ethan-1-ol and study of their biological activity

The present investigation involves rapid and efficient synthesis of a series of some novel derivatives for 1,2-bis-(4-amino-5-mercapto-1,2,4-triazol-3-yl)-ethan-1-ol 5–21 using dl-malic acid under microwave (MW) irradiation. Reaction with several alkylating agents such as epichlorohydrin, 3-chloropropanol, (2-acetoxyethoxy) methyl bromide, propargyl bromide and chloroacetamide was studied. Not only higher yields but also shorter reaction times were observed in comparison with thermal procedure. Structures of the realized products have been established on the basis of their 1H/13C NMR, IR, elemental analysis and correlation experiments. It is well known that 1,2,4-triazole ring systems are famous for their antifungal activities, so the synthesized compounds were screened for their antifungal activities. The minimal inhibitory concentration (MIC) of the screened compounds exhibited prominent results against Gram (+ ve) and Gram ( − ve) and antifungal activities comparing with the standard drugs.