TY - JOUR
T1 - Synthesis and in-vitro antimicrobial activity of new 1,2,4-triazoles
AU - Bhat, A.R.
AU - Bhat, G.V.
AU - Shenoy, G.G.
N1 - Cited By :91
Export Date: 10 November 2017
CODEN: JPPMA
Correspondence Address: Shenoy, G.G.; College of Pharmaceutical Sciences, Manipal 576 119, India
Chemicals/CAS: 1,2,4-triazole, 288-88-0; Anti-Bacterial Agents; Antifungal Agents; Antitubercular Agents; Indicators and Reagents; Triazoles
References: Clayton, Y.M., Yeasts and other fungi (1978) Laboratory Methods in Antimicrobial Chemotherapy, pp. 122-123. , In: Phillips, I., Reeves, D. S., Williams, J. D., Wise, R. (eds); Cruickshank, R., Duguid, J.P., Marmion, B.P., Swain, R.H.A., Mycobacteria (1975) Medical Microbiology. 12th edn, 2, pp. 204-205. , Churchill Livingstone, New York; Stokes, E.J., Waterworth, P.M., Antibiotic sensitivity tests by diffusion methods (1972) Association of Clinical Pathologists Broadsheet, p. 55; Udupi, R.H., Studies on the synthesis of substituted azetidinones, quinazolinones and related compounds for possible antitubercular activity and other pharmacological profiles (1995), pp. 233-234. , Ph.D. Thesis, Mangalore University, India; Udupi, R.H., Bhat, A.R., Synthesis of 4-(N-pyridyl carboxamido)-5-mercapto-3-substituted 1, 2, 4-triazoles for possible antitubercular activity (1996) Indian J. Heterocyclic Chem., 1, pp. 41-44; (1998) The Double Burden: Emerging Epidemics and Persistent Problems, pp. 21-23. , The World Health Report, World Health Organisation, Geneva
PY - 2001
Y1 - 2001
N2 - We have described the synthesis of new 1,2,4-triazoles and have evaluated their antimicrobial profile. Antitubercular activity was determined in triplicate using the Lowenstein-Jensen medium. A loopful of Mycobacterium tuberculosis suspension was inoculated on the surface of each Lowenstein-Jensen media containing the test compounds (100, 10 or 1 μg mL-1). To evaluate in-vitro antibacterial activity, compounds (50, 5 or 0.5 μg) were evaluated against B. subtilis, Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus and Staphylococcus typhi by the disc diffusion method. To evaluate antifungal activity Sabourauds Dextrose agar medium was used. Some of the compounds (5, 0.5 or 0.05 μg mL-1) were screened for activity against Aspergillus niger 88 and Aspergillus niger 90 and others were screened for activity against T. rubrum TR1, T. rubrum R6, T. rubrum R7 and T. mentagrophyte M1, using the cup plate method. Our results show that the triazoles with a pyrazine moiety at position 3 were more active as antitubercular and antifungal agents compared with the triazoles which had a pyrazine moiety at position 4 of the molecule.
AB - We have described the synthesis of new 1,2,4-triazoles and have evaluated their antimicrobial profile. Antitubercular activity was determined in triplicate using the Lowenstein-Jensen medium. A loopful of Mycobacterium tuberculosis suspension was inoculated on the surface of each Lowenstein-Jensen media containing the test compounds (100, 10 or 1 μg mL-1). To evaluate in-vitro antibacterial activity, compounds (50, 5 or 0.5 μg) were evaluated against B. subtilis, Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus and Staphylococcus typhi by the disc diffusion method. To evaluate antifungal activity Sabourauds Dextrose agar medium was used. Some of the compounds (5, 0.5 or 0.05 μg mL-1) were screened for activity against Aspergillus niger 88 and Aspergillus niger 90 and others were screened for activity against T. rubrum TR1, T. rubrum R6, T. rubrum R7 and T. mentagrophyte M1, using the cup plate method. Our results show that the triazoles with a pyrazine moiety at position 3 were more active as antitubercular and antifungal agents compared with the triazoles which had a pyrazine moiety at position 4 of the molecule.
U2 - 10.1211/0022357011775307
DO - 10.1211/0022357011775307
M3 - Article
SN - 0022-3573
VL - 53
SP - 267
EP - 272
JO - Journal of Pharmacy and Pharmacology
JF - Journal of Pharmacy and Pharmacology
IS - 2
ER -