1. 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
- Author
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Habibullah Khalilullah, Mohamed Jawed Ahsan, Jeyabalan Govinda Samy, Chandra Bhushan Jain, Md. Shivli Nomani, and Kunduri Rajeswar Dutt
- Subjects
Models, Molecular ,medicine.drug_class ,Stereochemistry ,Clinical Biochemistry ,Antitubercular Agents ,Pharmaceutical Science ,Microbial Sensitivity Tests ,Antimycobacterial ,Biochemistry ,Mycobacterium tuberculosis ,Structure-Activity Relationship ,Chlorocebus aethiops ,Tuberculosis, Multidrug-Resistant ,Drug Discovery ,medicine ,Animals ,Structure–activity relationship ,Cytotoxicity ,Vero Cells ,Molecular Biology ,Dose-Response Relationship, Drug ,Molecular Structure ,biology ,Chemistry ,Organic Chemistry ,Isoniazid ,biology.organism_classification ,Pyrazoles ,Molecular Medicine ,medicine.drug - 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).
- Published
- 2012
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