Synthesis and pharmacological evaluation of clubbed isopropylthiazole derived triazolothiadiazoles, triazolothiadiazines and mannich bases as potential antimicrobial and antitubercular agents.
A series of novel clubbed Isopropylthiazole derivatives triazolothiadiazines 2a-g, dihydro triazolothiadiazoles 3a-g, thioxotriazoles 4a-d, triazolothiadiazole 5, arylideneamino triazolethiones 7a-h and oxadiazolethiones 11a-b were synthesized and characterized by IR, (1)H NMR, (13)C NMR, elemental and mass spectral analysis. These compounds were evaluated for their preliminary in vitro antibacterial, antifungal and antitubercular activity against Mycobacterium tuberculosis H(37)Rv strain by broth dilution assay method. All the compounds exhibited moderate to significant antibacterial and antifungal activities. Results of the antitubercular screening against M. tuberculosis H(37)Rv showed compounds 7c and 7d exhibited good antitubercular activity (MIC 4 and 8 μg/mL) respectively, when compared with first line drug such as isoniazid (0.25 μg/mL).
Suresh Kumar
G V
GV
St Johns Pharmacy College, Department of Medicinal Chemistry, 6, 2nd stage Vijaynagar, R.P.C. Layout, Bangalore 560040, Karnataka, India. gvsureshkumar@yahoo.com
Rajendra Prasad
Y
Y
Mallikarjuna
B P
BP
Chandrashekar
S M
SM
D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D000995:Antitubercular Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects; D005658:Fungi / Q000187:drug effects; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects; D013055:Spectrophotometry, Infrared; D013844:Thiazoles / Q000138:chemical synthesis* / Q000494:pharmacology*
D000890:Anti-Infective Agents; D000995:Antitubercular Agents; D013844:Thiazoles