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Synthesis of 2,3,6-trideoxy sugar triazole hybrids as potential new broad spectrum antimicrobial agents.
Sharma, Smriti; Saquib, Mohammad; Verma, Saroj; Mishra, Nripendra N; Shukla, Praveen K; Srivastava, Ranjana; Prabhakar, Yenamandra S; Shaw, Arun K.
Afiliação
  • Sharma S; Division of Medicinal & Process Chemistry, CSIR-Central Drug Research Institute, Sector-10 Jankipuram Extension, Sitapur Road, Lucknow 226031, India.
  • Saquib M; Division of Medicinal & Process Chemistry, CSIR-Central Drug Research Institute, Sector-10 Jankipuram Extension, Sitapur Road, Lucknow 226031, India.
  • Verma S; Division of Medicinal & Process Chemistry, CSIR-Central Drug Research Institute, Sector-10 Jankipuram Extension, Sitapur Road, Lucknow 226031, India.
  • Mishra NN; Medical Mycology Lab, Division of Fermentation Technology, CSIR-Central Drug Research Institute, Sector-10 Jankipuram Extension, Sitapur Road, Lucknow 226031, India.
  • Shukla PK; Medical Mycology Lab, Division of Fermentation Technology, CSIR-Central Drug Research Institute, Sector-10 Jankipuram Extension, Sitapur Road, Lucknow 226031, India. Electronic address: pk_shukla@cdri.res.in.
  • Srivastava R; Division of Microbiology, CSIR-Central Drug Research Institute, Sector-10 Jankipuram Extension, Sitapur Road, Lucknow 226031, India.
  • Prabhakar YS; Division of Medicinal & Process Chemistry, CSIR-Central Drug Research Institute, Sector-10 Jankipuram Extension, Sitapur Road, Lucknow 226031, India. Electronic address: yenpra@yahoo.com.
  • Shaw AK; Division of Medicinal & Process Chemistry, CSIR-Central Drug Research Institute, Sector-10 Jankipuram Extension, Sitapur Road, Lucknow 226031, India. Electronic address: akshaw55@yahoo.com.
Eur J Med Chem ; 83: 474-89, 2014 Aug 18.
Article em En | MEDLINE | ID: mdl-24992075
Here, we describe a molecular hybridization inspired design and synthesis of novel 6-triazolyl 2,3,6-trideoxy sugars as promising new broad-spectrum antimicrobial agents using click chemistry in key step. These compounds showed MIC between 0.39 and 50 µg/mL against different native and resistant bacteria and fungi with no toxicity. Among them, compound 29 was the most active molecule with MIC 0.78 µg/mL against Staphylococcus aureus and Klebsiella pneumoniae and 3.12 µg/mL against methicillin- and vancomycin-resistant S. aureus. Compound 26 was the most potent anti-fungal candidate with MIC 0.39 µg/mL against Trichophyton mentagrophytes. Compound 46 was found to be promising with broad-spectrum activity against both bacterial and fungal strains. The bioinformatic studies involving bacteria's protein co-crystals prompted penicillin binding protein-2 as the most likely target of these compounds.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Triazóis / Carboidratos / Desenho de Fármacos / Anti-Infecciosos Idioma: En Ano de publicação: 2014 Tipo de documento: Article

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Triazóis / Carboidratos / Desenho de Fármacos / Anti-Infecciosos Idioma: En Ano de publicação: 2014 Tipo de documento: Article