Synthesis, characterisation, evaluation of antimicrobial & antifungal activity of novel pyrazolopyrimidine & pyrazolopyridine derivatives

Abstract

A new series of substituted PyrazoloPyrimidine & Pyrazolopyridine were designed to meet the structural requirement of antimicrobial ,Analgesic & antifungal drugs which has been known to possess a broad spectrum of biological activities such as analgesic,antimicrobial antifungal etc .(1) The therapeutic importance of these rings prompted us to develop selective molecules. The starting material of 1-{1-phenyl-3-(substituted phenyl)-1H-pyrazol-4-yl}-3-phenyl-1-propen-3-one (Chalcone) (3a-c) prepared from by claisen schmidt reaction from respective 1-phenyl-3-(substituted phenyl)-1H-pyrazoles-4-carboxaldehyde (Vilsmeier-Haack Reaction) ( 2a-c). 1-{1-phenyl-3-(substituted phenyl)-1H-pyrazol-4-yl}-3-phenyl-1-propen-3-one (Chalcone) (3a-c) further treated with thiourea ,3amino-s-triazole,ethylcyanoacetate, cynothioacetamideto produced 1,2,3,4 tetrahydropyrimidine (4 a-c),triazolopyrimidine (5 a,b),cynophenylpyridine(6 a-c) & phenyl pyridine thione derivatives.The structures of newly Synthesised compounds were characterized by spectral data & studied for their antimicrobial & Antifungal activities. Compounds 4a, 4c, 5a, 6c, 7c showed high antimicrobial activity using disc diffusion method with reference to using Amoxicillin as standard drug active active against Bacillus substillus, staphylococcus aureus, Proteus vulgaris.and pseudomonas.Similary compound 4c&7c showed maximum antifungal activity against fungal species candida albicans