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4-((8-hydroxyquinolin-7-yl)(2-nitrophenyl)methylamino)-1,5-dimethyl-2-phenyl-1,2-dihydro-3h-pyrazol-3-one

Development stage
Preclinical
Lead developer
Milind College of Science
Modality
Small Molecules
01

Overview

4-((8-hydroxyquinolin-7-yl)(2-nitrophenyl)methylamino)-1,5-dimethyl-2-phenyl-1,2-dihydro-3H-pyrazol-3-one, also referred to as compound 4b, is a small molecule synthesized through a Betti-type reaction involving the one-pot condensation of 2-nitrobenzaldehyde, 4-aminoantipyrine, and 8-hydroxyquinoline. Developed by researchers at the Milind College of Science, this compound has been evaluated for its anthelmintic and anti-inflammatory properties. It acts as an inhibitor of cyclooxygenase (COX) isoenzymes, which prevents the synthesis of prostanoids involved in inflammation and parasite survival. In in-vitro studies, the compound demonstrated potent anthelmintic activity, with efficacy in inducing paralysis and death in helminth parasites comparable to the reference drug albendazole. Furthermore, compound 4b satisfies Lipinski's rule of five, suggesting favorable pharmacokinetic properties for potential oral development.

Other names
4-((8-hydroxyquinolin-7-yl)(2-nitrophenyl)methylamino)-1,5-dimethyl-2-phenyl-1,2-dihydro-3H-pyrazol-3-one
02

Targets

COX

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