Synthesis and biological screening of novel 2-morpholinoquinoline nucleus clubbed with 1,2,4-oxadiazole motifs
| Autor: | Sampark S. Thakkar, Arabinda Ray, Vishal B. Purohit, Dipak K. Raval, Rahul P. Thummar, Vasudev R. Thakkar, Ronak D. Kamani, Sharad C. Karad, Parth Thakor, Beena K. Vaghasiya |
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| Rok vydání: | 2017 |
| Předmět: |
Stereochemistry
Drug Evaluation Preclinical Oxadiazole Chemistry Techniques Synthetic Microbial Sensitivity Tests 010402 general chemistry 01 natural sciences Structure-Activity Relationship chemistry.chemical_compound Anti-Infective Agents Bacterial Proteins Catalytic Domain Drug Discovery medicine Bioassay Cytotoxicity Norfloxacin Pharmacology Oxadiazoles Bacteria biology 010405 organic chemistry Chemistry Organic Chemistry Fungi General Medicine biology.organism_classification Antimicrobial Griseofulvin Combinatorial chemistry 0104 chemical sciences Molecular Docking Simulation Quinolines Agarose medicine.drug |
| Zdroj: | European Journal of Medicinal Chemistry. 126:894-909 |
| ISSN: | 0223-5234 |
| DOI: | 10.1016/j.ejmech.2016.12.016 |
| Popis: | Novel series of 2-morpholinoquinoline scaffolds (6a-n), containing the 1,2,4-oxadiazole and moiety, was designed and synthesized in good yield (76–86%). The synthesized compounds were screened for their preliminary in vitro antimicrobial activity against a panel of pathogenic strains of bacteria and fungi. Molecular docking and pharmacokinetic study were carried out for the prepared compounds. The cytotoxicity of the synthesized compounds was tested at different concentrations using bioassay of S. pombe cells at the cellular level. The effect of synthesized compounds on the DNA integrity of S. pombe was observed on agarose gel. Compounds 6d, 6e, 6g, 6h, 6j and 6n exhibited excellent antimicrobial potency as compared to the standard drugs (i.e Ampicillin, Norfloxacin, Chloramphenicol, Ciprofloxacin). Compounds 6d, 6e, 6g, 6k and 6n were found to have significant antifungal activity as compared to griseofulvin. Compounds 6f, 6i, 6k, 6l were found very less cytotoxic, while compounds 6d, 6e, 6g, 6h were found to exhibit maximum toxicity. The rest of the synthesized compounds were found to be moderately toxic. |
| Databáze: | OpenAIRE |
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