volume 41 pages 128004

Design and synthesis, biological evaluation of bis-(1,2,3- and 1,2,4)-triazole derivatives as potential antimicrobial and antifungal agents

Publication typeJournal Article
Publication date2021-06-01
scimago Q2
wos Q2
SJR0.472
CiteScore5.1
Impact factor2.2
ISSN0960894X, 14643405
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Pharmaceutical Science
Clinical Biochemistry
Molecular Medicine
Abstract
A new series of bis-1,2,3- and 1,2,4-triazoles (10a-m) were designed and efficiently synthesized using methyl salicylate as potential antimicrobial agents. All compounds were characterized by their proton & 13C NMR, IR, Mass spectral data, and elemental analysis. The final compounds 10a-m were in vitro screened for antimicrobial and antifungal activity against gram negative Pseudomonas aeruginosa, Escherichia coli, gram positive Bacillus subtilis, Staphylococcus aureus strains and Aspergillus niger & Saccharomyces cerevisiae. Majority of the synthesized compounds exhibited potent antimicrobial activity (MIC 3.9 µg/mL) and promising antifungal activity with the zone of inhibition (ZOI) 1.5–8.2 mm. Compounds like 10d and 10f exhibited best antimicrobial activity against S. aureus. The molecular docking analysis revealed that all the synthesized derivatives shown better binding affinities. Among all, compound 10f exhibited best scores. Hence, there was an assumption that introduction of para-chloro and bromo-phenyl aromatic groups on triazole moiety could result excellent antimicrobial activity. This substantial growth inhibitory activity of bis-1,2,3- and 1,2,4-triazole derivatives suggested these compounds could assist a new way in the development of lead molecules against microbial infection and antimicrobial resistance investigations.
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GOST Copy
Bitla S. et al. Design and synthesis, biological evaluation of bis-(1,2,3- and 1,2,4)-triazole derivatives as potential antimicrobial and antifungal agents // Bioorganic and Medicinal Chemistry Letters. 2021. Vol. 41. p. 128004.
GOST all authors (up to 50) Copy
Bitla S., Gayatri A. A., Puchakayala M. R., Kumar Bhukya V., Jagadeshwar V., Dhanavath R., Bhaskar K., Kothula D., Sagurthi S. R., Atcha K. R. Design and synthesis, biological evaluation of bis-(1,2,3- and 1,2,4)-triazole derivatives as potential antimicrobial and antifungal agents // Bioorganic and Medicinal Chemistry Letters. 2021. Vol. 41. p. 128004.
RIS |
Cite this
RIS Copy
TY - JOUR
DO - 10.1016/j.bmcl.2021.128004
UR - https://doi.org/10.1016/j.bmcl.2021.128004
TI - Design and synthesis, biological evaluation of bis-(1,2,3- and 1,2,4)-triazole derivatives as potential antimicrobial and antifungal agents
T2 - Bioorganic and Medicinal Chemistry Letters
AU - Bitla, Sampath
AU - Gayatri, Akkiraju Anjini
AU - Puchakayala, Muralidhar Reddy
AU - Kumar Bhukya, Vijaya
AU - Jagadeshwar, Vannada
AU - Dhanavath, Ramulu
AU - Bhaskar, Kuthati
AU - Kothula, Devender
AU - Sagurthi, S. R.
AU - Atcha, Krisham Raju
PY - 2021
DA - 2021/06/01
PB - Elsevier
SP - 128004
VL - 41
PMID - 33811989
SN - 0960-894X
SN - 1464-3405
ER -
BibTex
Cite this
BibTex (up to 50 authors) Copy
@article{2021_Bitla,
author = {Sampath Bitla and Akkiraju Anjini Gayatri and Muralidhar Reddy Puchakayala and Vijaya Kumar Bhukya and Vannada Jagadeshwar and Ramulu Dhanavath and Kuthati Bhaskar and Devender Kothula and S. R. Sagurthi and Krisham Raju Atcha},
title = {Design and synthesis, biological evaluation of bis-(1,2,3- and 1,2,4)-triazole derivatives as potential antimicrobial and antifungal agents},
journal = {Bioorganic and Medicinal Chemistry Letters},
year = {2021},
volume = {41},
publisher = {Elsevier},
month = {jun},
url = {https://doi.org/10.1016/j.bmcl.2021.128004},
pages = {128004},
doi = {10.1016/j.bmcl.2021.128004}
}