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 & C-13 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 mu g/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.
机构:
Univ Fed Sao Paulo, Dept Psicobiol, BR-04024002 Sao Paulo, BrazilUniv Fed Sao Paulo, Dept Psicobiol, BR-04024002 Sao Paulo, Brazil
Ferreira, Leandro
;
Galduroz Santos, Ruth Ferreia
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Univ Fed ABC, Ctr Math Computat & Cognit, Santo Andre, SP, Brazil
Univ Estadual Sao Paulo, Inst Biosci, Rio Claro, SP, BrazilUniv Fed Sao Paulo, Dept Psicobiol, BR-04024002 Sao Paulo, Brazil
Galduroz Santos, Ruth Ferreia
;
Ferri, Cleoza Pinheiro
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Univ Fed Sao Paulo, Dept Psicobiol, BR-04024002 Sao Paulo, BrazilUniv Fed Sao Paulo, Dept Psicobiol, BR-04024002 Sao Paulo, Brazil
Ferri, Cleoza Pinheiro
;
Fernandes Galduroz, Jose Carlos
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h-index: 0
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Univ Fed Sao Paulo, Dept Psicobiol, BR-04024002 Sao Paulo, BrazilUniv Fed Sao Paulo, Dept Psicobiol, BR-04024002 Sao Paulo, Brazil
机构:
Fundacao Oswaldo Cruz, Dept Pesquisa & Desenvolvimento Farmacos, Inst Tecnol Farmacos Farmanguinhos, BR-21041250 Rio De Janeiro, RJ, BrazilFundacao Oswaldo Cruz, Dept Pesquisa & Desenvolvimento Farmacos, Inst Tecnol Farmacos Farmanguinhos, BR-21041250 Rio De Janeiro, RJ, Brazil
Ferreira, Maria de Lourdes G.
;
Pinheiro, Luiz C. S.
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Fundacao Oswaldo Cruz, Dept Pesquisa & Desenvolvimento Farmacos, Inst Tecnol Farmacos Farmanguinhos, BR-21041250 Rio De Janeiro, RJ, BrazilFundacao Oswaldo Cruz, Dept Pesquisa & Desenvolvimento Farmacos, Inst Tecnol Farmacos Farmanguinhos, BR-21041250 Rio De Janeiro, RJ, Brazil
Pinheiro, Luiz C. S.
;
Santos-Filho, Osvaldo A.
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Fundacao Oswaldo Cruz, Dept Pesquisa & Desenvolvimento Farmacos, Inst Tecnol Farmacos Farmanguinhos, BR-21041250 Rio De Janeiro, RJ, BrazilFundacao Oswaldo Cruz, Dept Pesquisa & Desenvolvimento Farmacos, Inst Tecnol Farmacos Farmanguinhos, BR-21041250 Rio De Janeiro, RJ, Brazil
Santos-Filho, Osvaldo A.
;
Pecanha, Marta D. S.
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Fundacao Oswaldo Cruz, Dept Pesquisa & Desenvolvimento Farmacos, Inst Tecnol Farmacos Farmanguinhos, BR-21041250 Rio De Janeiro, RJ, BrazilFundacao Oswaldo Cruz, Dept Pesquisa & Desenvolvimento Farmacos, Inst Tecnol Farmacos Farmanguinhos, BR-21041250 Rio De Janeiro, RJ, Brazil
Pecanha, Marta D. S.
;
Sacramento, Carolina Q.
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Fundacao Oswaldo Cruz, Lab Viroses Resp, Inst Oswaldo Cruz, NIC WHO, BR-21041250 Rio De Janeiro, RJ, BrazilFundacao Oswaldo Cruz, Dept Pesquisa & Desenvolvimento Farmacos, Inst Tecnol Farmacos Farmanguinhos, BR-21041250 Rio De Janeiro, RJ, Brazil
Sacramento, Carolina Q.
;
Machado, Viviane
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Fundacao Oswaldo Cruz, Lab Viroses Resp, Inst Oswaldo Cruz, NIC WHO, BR-21041250 Rio De Janeiro, RJ, BrazilFundacao Oswaldo Cruz, Dept Pesquisa & Desenvolvimento Farmacos, Inst Tecnol Farmacos Farmanguinhos, BR-21041250 Rio De Janeiro, RJ, Brazil
Machado, Viviane
;
Ferreira, Vitor F.
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Univ Fed Fluminense, Dept Quim Organ, Inst Quim, BR-24210141 Niteroi, RJ, BrazilFundacao Oswaldo Cruz, Dept Pesquisa & Desenvolvimento Farmacos, Inst Tecnol Farmacos Farmanguinhos, BR-21041250 Rio De Janeiro, RJ, Brazil
Ferreira, Vitor F.
;
Souza, Thiago Moreno L.
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Fundacao Oswaldo Cruz, Lab Viroses Resp, Inst Oswaldo Cruz, NIC WHO, BR-21041250 Rio De Janeiro, RJ, BrazilFundacao Oswaldo Cruz, Dept Pesquisa & Desenvolvimento Farmacos, Inst Tecnol Farmacos Farmanguinhos, BR-21041250 Rio De Janeiro, RJ, Brazil
Souza, Thiago Moreno L.
;
Boechat, Nubia
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Fundacao Oswaldo Cruz, Dept Pesquisa & Desenvolvimento Farmacos, Inst Tecnol Farmacos Farmanguinhos, BR-21041250 Rio De Janeiro, RJ, BrazilFundacao Oswaldo Cruz, Dept Pesquisa & Desenvolvimento Farmacos, Inst Tecnol Farmacos Farmanguinhos, BR-21041250 Rio De Janeiro, RJ, Brazil
机构:
Qilu Univ Technol, Shandong Acad Sci, State Key Lab Biobased Mat & Green Papermaking LB, Jinan, Shandong, Peoples R ChinaQilu Univ Technol, Shandong Acad Sci, State Key Lab Biobased Mat & Green Papermaking LB, Jinan, Shandong, Peoples R China
机构:
Univ Fed Sao Paulo, Dept Psicobiol, BR-04024002 Sao Paulo, BrazilUniv Fed Sao Paulo, Dept Psicobiol, BR-04024002 Sao Paulo, Brazil
Ferreira, Leandro
;
Galduroz Santos, Ruth Ferreia
论文数: 0引用数: 0
h-index: 0
机构:
Univ Fed ABC, Ctr Math Computat & Cognit, Santo Andre, SP, Brazil
Univ Estadual Sao Paulo, Inst Biosci, Rio Claro, SP, BrazilUniv Fed Sao Paulo, Dept Psicobiol, BR-04024002 Sao Paulo, Brazil
Galduroz Santos, Ruth Ferreia
;
Ferri, Cleoza Pinheiro
论文数: 0引用数: 0
h-index: 0
机构:
Univ Fed Sao Paulo, Dept Psicobiol, BR-04024002 Sao Paulo, BrazilUniv Fed Sao Paulo, Dept Psicobiol, BR-04024002 Sao Paulo, Brazil
Ferri, Cleoza Pinheiro
;
Fernandes Galduroz, Jose Carlos
论文数: 0引用数: 0
h-index: 0
机构:
Univ Fed Sao Paulo, Dept Psicobiol, BR-04024002 Sao Paulo, BrazilUniv Fed Sao Paulo, Dept Psicobiol, BR-04024002 Sao Paulo, Brazil
机构:
Fundacao Oswaldo Cruz, Dept Pesquisa & Desenvolvimento Farmacos, Inst Tecnol Farmacos Farmanguinhos, BR-21041250 Rio De Janeiro, RJ, BrazilFundacao Oswaldo Cruz, Dept Pesquisa & Desenvolvimento Farmacos, Inst Tecnol Farmacos Farmanguinhos, BR-21041250 Rio De Janeiro, RJ, Brazil
Ferreira, Maria de Lourdes G.
;
Pinheiro, Luiz C. S.
论文数: 0引用数: 0
h-index: 0
机构:
Fundacao Oswaldo Cruz, Dept Pesquisa & Desenvolvimento Farmacos, Inst Tecnol Farmacos Farmanguinhos, BR-21041250 Rio De Janeiro, RJ, BrazilFundacao Oswaldo Cruz, Dept Pesquisa & Desenvolvimento Farmacos, Inst Tecnol Farmacos Farmanguinhos, BR-21041250 Rio De Janeiro, RJ, Brazil
Pinheiro, Luiz C. S.
;
Santos-Filho, Osvaldo A.
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机构:
Fundacao Oswaldo Cruz, Dept Pesquisa & Desenvolvimento Farmacos, Inst Tecnol Farmacos Farmanguinhos, BR-21041250 Rio De Janeiro, RJ, BrazilFundacao Oswaldo Cruz, Dept Pesquisa & Desenvolvimento Farmacos, Inst Tecnol Farmacos Farmanguinhos, BR-21041250 Rio De Janeiro, RJ, Brazil
Santos-Filho, Osvaldo A.
;
Pecanha, Marta D. S.
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机构:
Fundacao Oswaldo Cruz, Dept Pesquisa & Desenvolvimento Farmacos, Inst Tecnol Farmacos Farmanguinhos, BR-21041250 Rio De Janeiro, RJ, BrazilFundacao Oswaldo Cruz, Dept Pesquisa & Desenvolvimento Farmacos, Inst Tecnol Farmacos Farmanguinhos, BR-21041250 Rio De Janeiro, RJ, Brazil
Pecanha, Marta D. S.
;
Sacramento, Carolina Q.
论文数: 0引用数: 0
h-index: 0
机构:
Fundacao Oswaldo Cruz, Lab Viroses Resp, Inst Oswaldo Cruz, NIC WHO, BR-21041250 Rio De Janeiro, RJ, BrazilFundacao Oswaldo Cruz, Dept Pesquisa & Desenvolvimento Farmacos, Inst Tecnol Farmacos Farmanguinhos, BR-21041250 Rio De Janeiro, RJ, Brazil
Sacramento, Carolina Q.
;
Machado, Viviane
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机构:
Fundacao Oswaldo Cruz, Lab Viroses Resp, Inst Oswaldo Cruz, NIC WHO, BR-21041250 Rio De Janeiro, RJ, BrazilFundacao Oswaldo Cruz, Dept Pesquisa & Desenvolvimento Farmacos, Inst Tecnol Farmacos Farmanguinhos, BR-21041250 Rio De Janeiro, RJ, Brazil
Machado, Viviane
;
Ferreira, Vitor F.
论文数: 0引用数: 0
h-index: 0
机构:
Univ Fed Fluminense, Dept Quim Organ, Inst Quim, BR-24210141 Niteroi, RJ, BrazilFundacao Oswaldo Cruz, Dept Pesquisa & Desenvolvimento Farmacos, Inst Tecnol Farmacos Farmanguinhos, BR-21041250 Rio De Janeiro, RJ, Brazil
Ferreira, Vitor F.
;
Souza, Thiago Moreno L.
论文数: 0引用数: 0
h-index: 0
机构:
Fundacao Oswaldo Cruz, Lab Viroses Resp, Inst Oswaldo Cruz, NIC WHO, BR-21041250 Rio De Janeiro, RJ, BrazilFundacao Oswaldo Cruz, Dept Pesquisa & Desenvolvimento Farmacos, Inst Tecnol Farmacos Farmanguinhos, BR-21041250 Rio De Janeiro, RJ, Brazil
Souza, Thiago Moreno L.
;
Boechat, Nubia
论文数: 0引用数: 0
h-index: 0
机构:
Fundacao Oswaldo Cruz, Dept Pesquisa & Desenvolvimento Farmacos, Inst Tecnol Farmacos Farmanguinhos, BR-21041250 Rio De Janeiro, RJ, BrazilFundacao Oswaldo Cruz, Dept Pesquisa & Desenvolvimento Farmacos, Inst Tecnol Farmacos Farmanguinhos, BR-21041250 Rio De Janeiro, RJ, Brazil
机构:
Qilu Univ Technol, Shandong Acad Sci, State Key Lab Biobased Mat & Green Papermaking LB, Jinan, Shandong, Peoples R ChinaQilu Univ Technol, Shandong Acad Sci, State Key Lab Biobased Mat & Green Papermaking LB, Jinan, Shandong, Peoples R China