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

نویسندگان

  • P B Mohite
  • V H Bhaskar
چکیده

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.

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

منابع مشابه

Synthesis of 1,5 and 2,5-disubstituted tetrazoles using NiO nanoparticles and their evaluation as antimicrobial agents

Treatments of tetrazolate salts prepared in situ from various aldehyde; malononitrile and sodium azide in the presence of NiO nanoparticles with benzyl bromide gave the corresponding 1,5- and 2,‌5-disubstituted tetrazoles. Reaction of tetrazolate salts with 2,4′-dibromoacetophenone in the presence of NiO nanoparticles provided the corresponding 2,5-disubstituted derivatives as an only isomer. T...

متن کامل

Synthesis of Novel Fluorene Bisamide Derivatives via Ugi Reaction and Evaluation their Biological Activity against Mycobacterium species

A series of new fluorene bisamide derivatives were synthesized through multi-component Ugi reaction and tested for their in vitro anti-mycobacterial activity. The structures of the products 5a-w were deduced from their IR, 1H NMR, and 13C NMR spectra. Elemental analyses (CHN) for novel compounds (5a, 5d, 5f, 5h, 5k, 5l, 5p, 5s, 5t, 5v, 5w) was done to. These compounds were evaluated as anti-bac...

متن کامل

Synthesis of Novel Fluorene Bisamide Derivatives via Ugi Reaction and Evaluation their Biological Activity against Mycobacterium species

A series of new fluorene bisamide derivatives were synthesized through multi-component Ugi reaction and tested for their in vitro anti-mycobacterial activity. The structures of the products 5a-w were deduced from their IR, 1H NMR, and 13C NMR spectra. Elemental analyses (CHN) for novel compounds (5a, 5d, 5f, 5h, 5k, 5l, 5p, 5s, 5t, 5v, 5w) was done to. These compounds were evaluated as anti-bac...

متن کامل

Evaluation of Novel α-(Acyloxy)-α-(Quinolin-4-yl) Acetamides as Antiplasmodial Agents

Because of expanding resistance to efficient and affordable antimalarial drugs likechloroquine, the search is continuing for more effective drugs against this disease. In-vitroantiplasmodial activity and cytotoxicity of α-(acyloxy)-α-(quinolin-4-yl) acetamides onPlasmodium falciparum and structure-activity relationships of this new class of Passeriniadducts is described. The in-vitro antiplasmo...

متن کامل

Evaluation of Novel α-(Acyloxy)-α-(Quinolin-4-yl) Acetamides as Antiplasmodial Agents

Because of expanding resistance to efficient and affordable antimalarial drugs likechloroquine, the search is continuing for more effective drugs against this disease. In-vitroantiplasmodial activity and cytotoxicity of α-(acyloxy)-α-(quinolin-4-yl) acetamides onPlasmodium falciparum and structure-activity relationships of this new class of Passeriniadducts is described. The in-vitro antiplasmo...

متن کامل

ذخیره در منابع من


  با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

عنوان ژورنال:
  • Advanced pharmaceutical bulletin

دوره 2 1  شماره 

صفحات  -

تاریخ انتشار 2012