Literature DB >> 16725324

Synthesis and in vitro antimycobacterial activity of N1-nicotinoyl-3-(4'-hydroxy-3'-methyl phenyl)-5-[(sub)phenyl]-2-pyrazolines.

Mohammad Shaharyar1, Anees Ahamed Siddiqui, Mohamed Ashraf Ali, Dharmarajan Sriram, Perumal Yogeeswari.   

Abstract

A series of N1-nicotinoyl-3- (4'-hydroxy-3'-methyl phenyl)-5-(substituted phenyl)-2-pyrazolines were synthesized by the reaction between isoniazid (INH) and chalcones and were tested for their antimycobacterial activity in vitro against Mycobacterium tuberculosis H37Rv (MTB) and INH-resistant M. tuberculosis (INHR-MTB) using the agar dilution method. Among the synthesized compounds, compound (i) N1-nicotinyl-3-(4'-hydroxy-3'-methyl phenyl)-5-(1''-chlorophenyl)-2-pyrazoline was found to be the most active agent against MTB and INHR-MTB, with minimum inhibitory concentration of 0.26 microm. When compared to INH-compound i was found to be 2.8- and 43.7-fold more active against MTB and INHR-MTB, respectively.

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Year:  2006        PMID： 16725324     DOI： 10.1016/j.bmcl.2006.05.024

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  6 in total

1.  Nitric oxide functionalized molybdenum(0) pyrazolone Schiff base complexes: thermal and biochemical study.

Authors:  Jan Mohammad Mir; Ram Charitra Maurya
Journal:  RSC Adv       Date:  2018-10-16       Impact factor: 4.036

2.  Synthesis, biological evaluation and 2D-QSAR study of halophenyl bis-hydrazones as antimicrobial and antitubercular agents.

Authors:  Hatem A Abdel-Aziz; Wagdy M Eldehna; Mohamed Fares; Sara T A Al-Rashood; Khalid A Al-Rashood; Marwa M Abdel-Aziz; Dalia H Soliman
Journal:  Int J Mol Sci       Date:  2015-04-20       Impact factor: 5.923

3.  2-pyrazoline derivatives in neuropharmacology: Synthesis, ADME prediction, molecular docking and in vivo biological evaluation.

Authors:  Savita Upadhyay; Avinash C Tripathi; Sarvesh Paliwal; Shailendra K Saraf
Journal:  EXCLI J       Date:  2017-05-08       Impact factor: 4.068

Review 4.  Recent advances in the therapeutic applications of pyrazolines.

Authors:  Mohamed R Shaaban; Abdelrahman S Mayhoub; Ahmad M Farag
Journal:  Expert Opin Ther Pat       Date:  2012-03-08       Impact factor: 6.674

5.  5''-(2,4-Dichloro-benzyl-idene)-1'-(2,4-dichloro-phen-yl)-1''-methyl-1',2',3',5',6',7',8',8a'-octa-hydro-dispiro-[acenaphthyl-ene-1,3'-indolizine-2',3''-piperidine]-2,4''(1H)-dione.

Authors:  J Suresh; R Vishnupriya; R Ranjith Kumar; S Sivakumar; P L Nilantha Lakshman
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2012-09-08

6.  Synthesis and Characterization of Some New Bis-Pyrazolyl-Thiazoles Incorporating the Thiophene Moiety as Potent Anti-Tumor Agents.

Authors:  Sobhi M Gomha; Mastoura M Edrees; Farag M A Altalbawy
Journal:  Int J Mol Sci       Date:  2016-09-07       Impact factor: 5.923
  6 in total

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