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Pyrazole Bearing Pyrimidine Analogues as the Privileged Scaffolds in Antimicrobial Drug Discovery: A Review

Pyrazole Bearing Pyrimidine Analogues as the Privileged Scaffolds in Antimicrobial Drug... Abstract Historically, heterocyclic compounds including N-heterocycles and their derivatives are valuable source for the identification of therapeutically active agents. Studies in the recent two decades have been reported escalating data utilizing drug optimization parameters on various pyrazole clubbed pyrimidine derivatives with numerous pharmacological activities. The present review article deals to emphasize the diverse synthetic approaches reported by researchers on pyrazole clubbed/fused pyrimidines for their antimicrobial potency. Ring variation, ring fusion, substitution variant and spacer addition strategies allied with electron withdrawing groups at active sites on pyrazole and pyrimidine are the best combination to achieve potent antimicrobial motifs. N-substituted aromatic or hetero-aromatic groups along with EWG are also good structural modifications to improve the pharmacokinetic properties in pre-clinical drug species. A new age antimicrobials can be synthesized with the next level of potency by this prospective. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Analytical Chemistry Letters Taylor & Francis

Pyrazole Bearing Pyrimidine Analogues as the Privileged Scaffolds in Antimicrobial Drug Discovery: A Review

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Pyrazole Bearing Pyrimidine Analogues as the Privileged Scaffolds in Antimicrobial Drug Discovery: A Review

Abstract

Abstract Historically, heterocyclic compounds including N-heterocycles and their derivatives are valuable source for the identification of therapeutically active agents. Studies in the recent two decades have been reported escalating data utilizing drug optimization parameters on various pyrazole clubbed pyrimidine derivatives with numerous pharmacological activities. The present review article deals to emphasize the diverse synthetic approaches reported by researchers on pyrazole...
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Publisher
Taylor & Francis
Copyright
© 2022 Har Krishan Bhalla & Sons
ISSN
2230-7532
eISSN
2229-7928
DOI
10.1080/22297928.2021.1910565
Publisher site
See Article on Publisher Site

Abstract

Abstract Historically, heterocyclic compounds including N-heterocycles and their derivatives are valuable source for the identification of therapeutically active agents. Studies in the recent two decades have been reported escalating data utilizing drug optimization parameters on various pyrazole clubbed pyrimidine derivatives with numerous pharmacological activities. The present review article deals to emphasize the diverse synthetic approaches reported by researchers on pyrazole clubbed/fused pyrimidines for their antimicrobial potency. Ring variation, ring fusion, substitution variant and spacer addition strategies allied with electron withdrawing groups at active sites on pyrazole and pyrimidine are the best combination to achieve potent antimicrobial motifs. N-substituted aromatic or hetero-aromatic groups along with EWG are also good structural modifications to improve the pharmacokinetic properties in pre-clinical drug species. A new age antimicrobials can be synthesized with the next level of potency by this prospective.

Journal

Analytical Chemistry Letters – Taylor & Francis

Published: Mar 4, 2022

Keywords: Pyrazole; Pyrimidine; Antimicrobial activity; Drug discovery

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