Literature DB >> 16303302

Synthesis and in vitro antitubercular activity of some 1-[(4-sub)phenyl]-3-(4-{1-[(pyridine-4-carbonyl)hydrazono]ethyl}phenyl)thiourea.

Dharmarajan Sriram1, Perumal Yogeeswari, Kasinathan Madhu.   

Abstract

Various isonicotinyl hydrazones were prepared by reacting isonicotinyl hydrazide [INH] with 1-(4-acetylphenyl)-3-[(4-sub)phenyl]thiourea and were tested for their antimycobacterial activity in vitro against Mycobacterium tuberculosis H37Rv and INH-resistant M. tuberculosis using the BACTEC 460 radiometric system. Among the synthesized compounds, 1-(4-fluorophenyl)-3-(4-{1-[(pyridine-4-carbonyl)-hydrazono]ethyl}phenyl)thiourea (4d) was found to be the most potent compound with a minimum inhibitory concentration of 0.49 microM against M. tuberculosis H37Rv and INH-resistant M. tuberculosis. When compared to INH, 4d was found to be 3 and 185 times more active against M. tuberculosis H37Rv and INH-resistant M. tuberculosis, respectively, with a selectivity index of >300.

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Year:  2005        PMID： 16303302     DOI： 10.1016/j.bmcl.2005.11.004

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


  7 in total

1.  High pressure liquid chromatographic analysis of in vivo metabolites of N-(substituted phenyl)-N'-(1,3,5-trimethyl pyrazole-4-yl)thioureas in rats.

Authors:  Bedia Kocyigit-Kaymakcioglu; Ufuk Yilmaz; Feyza Aricioglu
Journal:  Eur J Drug Metab Pharmacokinet       Date:  2007 Oct-Dec       Impact factor: 2.441

2.  Synthesis, X-ray crystal structure elucidation and Hirshfeld surface analysis of N-((4-(1H-benzo[d]imidazole-2-yl)phenyl)carbamothioyl)benzamide: investigations for elastase inhibition, antioxidant and DNA binding potentials for biological applications.

Authors:  Nasima Arshad; Mamoona Rafiq; Rabail Ujan; Aamer Saeed; Shahid I Farooqi; Fouzia Perveen; Pervaiz Ali Channar; Saba Ashraf; Qamar Abbas; Ashfaq Ahmed; Tuncer Hokelek; Manpreet Kaur; Jerry P Jasinski
Journal:  RSC Adv       Date:  2020-06-02       Impact factor: 4.036

Review 3.  Pyridine: the scaffolds with significant clinical diversity.

Authors:  Sourav De; Ashok Kumar S K; Suraj Kumar Shah; Sabnaz Kazi; Nandan Sarkar; Subhasis Banerjee; Sanjay Dey
Journal:  RSC Adv       Date:  2022-05-20       Impact factor: 4.036

Review 4.  Biological activities of hydrazone derivatives.

Authors:  Sevim Rollas; S Güniz Küçükgüzel
Journal:  Molecules       Date:  2007-08-17       Impact factor: 4.411

5.  Synthesis, docking study and biological evaluation of some new thiourea derivatives bearing benzenesulfonamide moiety.

Authors:  Mostafa M Ghorab; Mohamed S A El-Gaby; Aiten M Soliman; Mansour S Alsaid; Marwa M Abdel-Aziz; Mahmoud M Elaasser
Journal:  Chem Cent J       Date:  2017-05-19       Impact factor: 4.215

6.  2-(1,3-Dioxoisoindolin-2-yl)acetic acid-N'-[(E)-2-meth-oxy-benzyl-idene]pyridine-4-carbohydrazide (1/1).

Authors:  Shaaban K Mohamed; Muhammad Akhyar Farrukh; Mehmet Akkurt; Mustafa R Albayati; Antar A Abdelhamid
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2012-07-14

7.  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
  7 in total

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