Molecular sieves and Ultrasound assisted Synthesis of Novel 1,3,4-oxadiazole-2-thiones derivatives as potential antifungal Agents

Abstract

In the category of microorganism, fungi are considered as the special class of microbes responsible for opportunistic pathogenic infections in humans species. Due to the side effects of commercially available antifungal drugs and the emergence of new drug resistant fungal species in the past few years has forced the researchers to search for novel and efficient antifungal drug molecules. The 1,3,4-oxadiazoles scaffold is associated with diverse biological activities. The multipurpose use of the Mannich bases in pharmaceutical chemistry provoked us to prepare a new series of 1,3,4-oxadiazole Mannich bases derivatives, as antifungal agents.

Herein we report Molecular sieves and Ultrasound assisted synthesis of novel series of Mannich bases of the 5-substituted 1,3,4-oxadiazole-2-thiones by amino methylation with paraformaldehyde and substituted primary / secondary amines and their evaluation for antifungal activity .The structures of the newly synthesized compounds were determined by IR, NMR and Mass spectral study. The synthesized compounds exhibited interesting moderate to excellent antifungal activity against Candida albicans (NCIM 3557),Candida albicans(NCIM3471), Candida glabrata(NCIM3237), Cryptococcus neoformans (NCIM 3542),Cryptococcus neoformans(NCIM 3378),Aspergillus fumigates(NCIM 902), Aspergillus niger( NCIM 628) using Flucanazole as a standard reference drug. The synthesised compounds 6d, 6f ,6g, 6h and 6j exhibited promising antifungal activity as fungi static agents