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Background: Treating tuberculosis is a challenge due to the development of drug resistance. Hence, it is imperative to develop novel leads having high potency and efficacy to curb drug resistance. Methods: The present research work is focused on microwave-assisted synthesis of novel twenty-six 3-amino-N’-benzylidenepyrazine-2-carbohydrazide derivatives (3a-z), where, lyophilization technique was used for isolation of the major intermediate, 3-aminopyrazin-2-carbohydrazide. All synthesized compounds were subjected for anti-tubercular screening against Mycobacterium tuberculosis H37Ra by using XTT Reduction Menadione Assay (XRMA) protocol. Results: Out of 26 synthesized compounds, four N’-substitutedbenzaldehyde-3-amino-pyrazine-2- carbohydrazide derivatives viz. 3i, 3j 3v and 3z showed significant activity against M. tuberculosis H37Ra. The compounds 3i, 3j, 3v and 3z showed 99, 98, 92 and 87 % inhibition respectively as compared to 94% inhibition shown by the standard drug rifampicin. The MIC and IC50 values were in the range of 24.3-110 and 5.9-20.8 µg/ml respectively. Conclusion: A classification model called Recursive Partitioning (RP) based on binary Quantitative Structure-Activity Relationship (QSAR) was derived for the establishment of structure-activity relationship (SAR). The predictions derived on the basis of RP model were found to be in agreement with anti-tubercular screening data.

The present work involves synthesis of novel anti-fungal agents containing triazole scaffold. The newly designed compounds were synthesized on the trails of ketoconazole using the molecular hybridization approach. A series of 10 compounds having (2-((1H-1,2,4-triazol-1-yl)methyl)-2-(2,4-dichlorophenyl)-1,3-dioxolan-4-yl)methyl esters ( 4a – j ) were prepared by conventional synthetic approach. The synthesized compounds were subjected for in vitro anti-fungal screening against Aspergillus niger , Aspergillus fumigatus , Candida albicans and Penicillium notatum . Out of 10 newly synthesized compounds, six compounds ( 4b – f and j ) showed remarkable anti-fungal activity (MIC range 6.5–25 μg/ml), whereas compound 4d (MIC 6.5 μg/ml) was more potent than standard drug ketoconazole (MIC 12.5 μg/ml). These triazole hybrids can be considered as potential anti-fungal agents.