Synthesis and antitubercular activity of 3-aryl substituted-2-[1H(2H)benzotriazol-1(2)-yl]acrylonitriles

A series of 22 3-aryl substituted-2-(1H(2H)-benzotriazol-1(2)-yl)acrylonitriles was synthesized for a preliminary in vitro evaluation of antitubercular activity according to an international program with the Tuberculosis Antimicrobial Acquisition & Coordinating Facility (TAACF). This work report...

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Bibliographic Details
Published in:European journal of medicinal chemistry 2000-05, Vol.35 (5), p.535
Main Authors: Sanna, P, Carta, A, Nikookar, M E
Format: Article
Language:English
Subjects:
Acrylonitrile - analogs & derivatives
Acrylonitrile - chemical synthesis
Acrylonitrile - chemistry
Acrylonitrile - pharmacology
Antitubercular Agents - chemical synthesis
Antitubercular Agents - pharmacology
Magnetic Resonance Spectroscopy
Molecular Structure
Mycobacterium tuberculosis - drug effects
Mycobacterium tuberculosis - pathogenicity
Nitriles - chemical synthesis
Nitriles - pharmacology
Spectrophotometry
Triazoles - chemical synthesis
Triazoles - chemistry
Triazoles - pharmacology
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Summary:A series of 22 3-aryl substituted-2-(1H(2H)-benzotriazol-1(2)-yl)acrylonitriles was synthesized for a preliminary in vitro evaluation of antitubercular activity according to an international program with the Tuberculosis Antimicrobial Acquisition & Coordinating Facility (TAACF). This work reports the synthetic approach and analytical and spectroscopic characterization (UV, IR, 1H- and 13C-NMR) of all compounds synthesized. Several compounds showed an interesting activity in the preliminary screening with a percent growth inhibition of the virulent Mycobacterium tuberculosis between 40 and 99% at the concentration of 12.5 microg/mL. The most effective derivatives E-5a and E-5e were also tested against M. avium in vitro.
ISSN:0223-5234