Details

Autor(en) / Beteiligte

• Shiradkar, Mahendra Ramesh
• Murahari, Kiran Kumar
• Gangadasu, Hanimi Reddy
• Suresh, Tatikonda
• Kalyan, Chakravarthy Akula
• Panchal, Dolly
• Kaur, Ranjit
• Burange, Prashant
• Ghogare, Jyoti
• Mokale, Vinod
• Raut, Mayuresh

Titel

Synthesis of new S-derivatives of clubbed triazolyl thiazole as anti- Mycobacterium tuberculosis agents

Ist Teil von

• Bioorganic & medicinal chemistry, 2007-06, Vol.15 (12), p.3997-4008

Ort / Verlag

Oxford: Elsevier Ltd

Erscheinungsjahr

2007

Quelle

Access via ScienceDirect (Elsevier)

Beschreibungen/Notizen

• The synthesis of a new series of triazolyl-thiazole derivatives under microwave assisted organic synthesis is described. They were tested as antimycobacterial agents. It was also observed that 8f and 8g have shown promising activity, while compounds 8e and 8h have shown appreciable antimycobacterial potency. Few compounds were good inhibitors while others were inactive. In the present study, a series of N-{4-[(4-amino-5-sulfanyl-4 H-1,2,4-triazol-3-yl)methyl]-1,3-thiazol-2-yl}-2-substituted-amide ( 1a– d) derivatives were synthesized in good yields and characterized by IR, 1H NMR, mass spectral and elemental analyses. The compounds were evaluated for their preliminary in vitro antibacterial activity against Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa and Salmonella typhosa and then were screened for antitubercular activity against Mycobacterium tuberculosis H37 Rv strain by broth microdilution assay method. The antibacterial data of the tested compounds indicated that most of the synthesized compounds showed better activity against bacteria compared to reference drugs. The in vitro antitubercular activity reports of tested compounds against M. tuberculosis strain H37 Rv showed moderate to better activity.