Abstract
Synthesis, characterization and investigation of antibacterial and antifungal activities of twelve camphor based 2,4-disubstituted 1,3-thiazoles is presented. Their structures were determined using NMR, IR, FAB MS and HRMS analyses. Among the derivatives, 3i and 5 were found to exhibit antifungal and antibacterial activities comparable to that of fluconazole and ciprofloxacin against yeast belonging to Candida spp., MIC 0.12-0.98 μg/ml and Gram-positive bacteria including both pathogenic S. aureus and opportunistic S. epidermidis, MIC 0.98-7.81 μg/ml, B. subtilis and B. cereus, MIC 3.91-31.25 μg/ml, and M. luteus, MIC 0.98 μg/ml species, respectively. Molecular docking studies of all compounds into the active sites of microbial enzymes indicated a possible targets SAP and NMT, thiazoles 3a-j, 4, 5 showed more favourable affinity than the native ligand.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Anti-Bacterial Agents / chemical synthesis*
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Anti-Bacterial Agents / chemistry
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Anti-Bacterial Agents / pharmacology
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Antifungal Agents / chemical synthesis*
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Antifungal Agents / chemistry
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Antifungal Agents / pharmacology
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Bacterial Proteins / chemistry
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Bacterial Proteins / metabolism
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Binding Sites
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Camphor / chemistry*
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Camphor / pharmacology
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Candida / drug effects
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Candida / enzymology
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Candida / growth & development
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Fungal Proteins / chemistry
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Fungal Proteins / metabolism
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Gram-Positive Bacteria / drug effects
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Gram-Positive Bacteria / enzymology
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Gram-Positive Bacteria / growth & development
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Ligands
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Microbial Sensitivity Tests
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Molecular Docking Simulation
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Molecular Structure
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Thiazoles / chemical synthesis*
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Thiazoles / chemistry
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Thiazoles / pharmacology
Substances
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Anti-Bacterial Agents
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Antifungal Agents
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Bacterial Proteins
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Fungal Proteins
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Ligands
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Thiazoles
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Camphor