Discovery of novel antitubercular 1,5-dimethyl-2-phenyl-4-([5-(arylamino)-1,3,4-oxadiazol-2-yl]methylamino)-1,2-dihydro-3H-pyrazol-3-one analogues

Bioorganic & Medicinal Chemistry Letters
Mohamed Jawed AhsanMd Shivli Nomani

Abstract

In search of potential therapeutics for tuberculosis, we describe herewith the synthesis, characterization and antimycobacterial activity of 1,5-dimethyl-2-phenyl-4-([5-(arylamino)-1,3,4-oxadiazol-2-yl]methylamino)-1,2-dihydro-3H-pyrazol-3-one analogues. Among the synthesized compounds, 4-[(5-[(4-fluorophenylamino]-1,3,4-oxadiazol-2-yl)methylamino]-1,2-dihydro-1,5-dimethyl-2-phenylpyrazol-3-one (4a) was found to be the most promising compound active against Mycobacterium tuberculosis H(37)Rv and isoniazid resistant M. tuberculosis with minimum inhibitory concentrations, 0.78 and 3.12μg/mL, respectively, free from any cytotoxicity (>62.5μg/mL).

Citations

May 15, 2013·Expert Opinion on Therapeutic Patents·Afshin Zarghi, Zahra Hajimahdi
Jul 1, 2014·BioMed Research International·Mohamed Jawed AhsanSabina Yasmin
Jun 10, 2017·Medicinal Research Reviews·Vajinder KumarRahul Jain
Mar 4, 2017·Materials Science & Engineering. C, Materials for Biological Applications·Subramani KandhasamyParamasivan T Perumal
Mar 13, 2019·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·El Hassane AnouarAshik Mosaddik
Feb 10, 2017·Zeitschrift Für Naturforschung. C, a Journal of Biosciences·Patel NavinGildardo Rivera
Oct 9, 2020·European Journal of Medicinal Chemistry·Santosh Kumar VermaK P Rakesh
Nov 26, 2019·European Journal of Medicinal Chemistry·Zefeng ZhaoXiaohui Zheng
Dec 30, 2020·BMC Chemistry·Ankit Siwach, Prabhakar Kumar Verma

Related Concepts

Antitubercular Agents
Cercopithecus tantalus
Dose-Response Relationship, Drug
Fungus Drug Sensitivity Tests
Mycobacterium tuberculosis H37Rv
Pyrazoles
Structure-Activity Relationship
Vero Cells
Tuberculosis, Drug-Resistant
Antitubercular Agents

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