Synthesis and in-vitro antimicrobial activity of new 1,2,4-triazoles

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Abstract

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.
Original languageEnglish
Pages (from-to)267-272
Number of pages6
JournalJournal of Pharmacy and Pharmacology
Volume53
Issue number2
DOIs
Publication statusPublished - 2001

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Pyrazines
Triazoles
Aspergillus niger
Antitubercular Agents
Antifungal Agents
Staphylococcus
Mycobacterium tuberculosis
Pseudomonas aeruginosa
Agar
Staphylococcus aureus
Suspensions
Escherichia coli
Glucose
1,2,4-triazole
In Vitro Techniques

Cite this

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title = "Synthesis and in-vitro antimicrobial activity of new 1,2,4-triazoles",
abstract = "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.",
author = "A.R. Bhat and G.V. Bhat and G.G. Shenoy",
note = "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",
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Synthesis and in-vitro antimicrobial activity of new 1,2,4-triazoles. / Bhat, A.R.; Bhat, G.V.; Shenoy, G.G.

In: Journal of Pharmacy and Pharmacology, Vol. 53, No. 2, 2001, p. 267-272.

Research output: Contribution to journalArticle

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

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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

VL - 53

SP - 267

EP - 272

JO - Journal of Pharmacy and Pharmacology

JF - Journal of Pharmacy and Pharmacology

SN - 0022-3573

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ER -