Literature DB >> 24312768

In vitro evaluation of tetrazoles as a novel class of Antimycobacterium tuberculosis agents.

P B Mohite1, V H Bhaskar.   

Abstract

PURPOSE: We report here the antimycobacterial activity of some already synthesized tetrazole derivatives containing tetrazole against Mycobacterium tuberculosis strain H37Rv.
METHODS: In vitro evaluation of the antitubercular activity was carried out within the Tuberculosis Antimicrobial Acquisition & Coordinating Facility (TAACF) screening program for the discovery of novel drugs for the treatment of tuberculosis. Under the direction of the US National Institute of Allergy and Infectious Diseases (NIAID), Southern Research Institute that coordinates the overall program. The method of TAACF was followed for evaluation of activity.
RESULTS: This new structural class of compounds showed high activity against the bacilli. The activity depends on the substituent's present in azatidinone core. Compounds having a 4-MeOC6H4 4-N(CH3)2C6H4 group as the substituent on β-lactam ring were active. The highest activity was registered for compounds having 4-MeOC6H4 as substituent.
CONCLUSION: The new compounds showed high potency and promising antitubercular activity and should be regarded as new hits for further development as a novel class of Antimycobacterium tuberculosis agents.

Entities:  

Keywords:  Antimycobacterial activity; Azatidinones; TAACF; Tetrazole

Year:  2012        PMID: 24312768      PMCID: PMC3846022          DOI: 10.5681/apb.2012.005

Source DB:  PubMed          Journal:  Adv Pharm Bull        ISSN: 2228-5881


  16 in total

1.  Synthesis of novel substituted tetrazoles having antifungal activity.

Authors:  Ram Shankar Upadhayaya; Sanjay Jain; Neelima Sinha; Nawal Kishore; Ramesh Chandra; Sudershan K Arora
Journal:  Eur J Med Chem       Date:  2004-07       Impact factor: 6.514

2.  Recent advances in antituberculous drug development and novel drug targets.

Authors:  Haruaki Tomioka; Yutaka Tatano; Ko Yasumoto; Toshiaki Shimizu
Journal:  Expert Rev Respir Med       Date:  2008-08       Impact factor: 3.772

3.  Microplate alamar blue assay versus BACTEC 460 system for high-throughput screening of compounds against Mycobacterium tuberculosis and Mycobacterium avium.

Authors:  L Collins; S G Franzblau
Journal:  Antimicrob Agents Chemother       Date:  1997-05       Impact factor: 5.191

4.  Synthesis and antinociceptive activity of some substituted-{5-[2-(1,2,3,4-tetrahydrocarbazol-9-yl)ethyl]tetrazol-1-yl}alkanones.

Authors:  A Rajasekaran; P P Thampi
Journal:  Eur J Med Chem       Date:  2005-09-15       Impact factor: 6.514

Review 5.  Recent advances in new structural classes of anti-tuberculosis agents.

Authors:  Amit Nayyar; Rahul Jain
Journal:  Curr Med Chem       Date:  2005       Impact factor: 4.530

Review 6.  Emerging drugs for active tuberculosis.

Authors:  Ann M Ginsberg
Journal:  Semin Respir Crit Care Med       Date:  2008-09-22       Impact factor: 3.119

7.  Synthesis of chloro and bromo substituted 5-(indan-1'-yl)tetrazoles and 5-(indan-1'-yl)methyltetrazoles as possible analgesic agents.

Authors:  S C Bachar; S C Lahiri
Journal:  Pharmazie       Date:  2004-06       Impact factor: 1.267

8.  Programs to facilitate tuberculosis drug discovery: the tuberculosis antimicrobial acquisition and coordinating facility.

Authors:  R C Goldman; B E Laughon; R C Reynolds; J A Secrist; J A Maddry; M-A Guié; A C Poffenberger; C A Kwong; S Ananthan
Journal:  Infect Disord Drug Targets       Date:  2007-06

Review 9.  Overview of anti-tuberculosis (TB) drugs and their resistance mechanisms.

Authors:  Ruiru Shi; Nobunori Itagaki; Isamu Sugawara
Journal:  Mini Rev Med Chem       Date:  2007-11       Impact factor: 3.862

Review 10.  New tuberculosis drugs in development.

Authors:  Barbara E Laughon
Journal:  Curr Top Med Chem       Date:  2007       Impact factor: 3.295

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  4 in total

1.  Synthesis, Cytotoxic Analysis, and Molecular Docking Studies of Tetrazole Derivatives via N-Mannich Base Condensation as Potential Antimicrobials.

Authors:  Ashraf Atef Hatamleh; Dunia Al Farraj; Sarah Salah Al-Saif; SathishKumar Chidambaram; Surendrakumar Radhakrishnan; Idhayadhulla Akbar
Journal:  Drug Des Devel Ther       Date:  2020-10-23       Impact factor: 4.162

Review 2.  Tetrazolium compounds: synthesis and applications in medicine.

Authors:  Cheng-Xi Wei; Ming Bian; Guo-Hua Gong
Journal:  Molecules       Date:  2015-03-27       Impact factor: 4.411

3.  Novel tetrazole and cyanamide derivatives as inhibitors of cyclooxygenase-2 enzyme: design, synthesis, anti-inflammatory evaluation, ulcerogenic liability and docking study.

Authors:  Phoebe F Lamie; John N Philoppes; Amany A Azouz; Nesreen M Safwat
Journal:  J Enzyme Inhib Med Chem       Date:  2017-12       Impact factor: 5.051

4.  New endoperoxides highly active in vivo and in vitro against artemisinin-resistant Plasmodium falciparum.

Authors:  Lis Lobo; Lília I L Cabral; Maria Inês Sena; Bruno Guerreiro; António Sebastião Rodrigues; Valter Ferreira de Andrade-Neto; Maria L S Cristiano; Fatima Nogueira
Journal:  Malar J       Date:  2018-04-03       Impact factor: 2.979

  4 in total

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