Abstract

A library of new 2-alkyl-2-(N-arylsulfonylindol-3-yl)-3-N-acyl-5-aryl-1,3,4-oxadiazolines was efficiently synthesized from hydrazones and anhydrides under microwave irradiation and solvent-free conditions. Compared with the traditional procedure (100 equiv. of anhydride and 1.5-4 h of reaction time), the present methodology has the advantages of short reaction time (10-20 min), and avoiding excess of anhydride (only 1.5 equiv.). Moreover, two compounds exhibited the promising anti-HIV-1 activity when evaluated for their inhibitory activity against HIV-1 replication in acutely infected C8166 cells.

Keywords: 1, 3, 4-Oxadiazoline, microwave heating, human immunodeficiency virus-1, inhibitor.