title: Synthesis and biological screening of novel 2-morpholinoquinoline nucleus clubbed with 1,2,4-oxadiazole motifs.
abstract: 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.
authors.affiliation: Department of Chemistry, Sardar Patel University, Vallabh Vidyanagar 388 120, Gujarat, India. Electronic address: krdsharad1126@gmail.com.
authors.forename: Sharad C
authors.initials: SC
authors.lastname: Karad
authors.affiliation: Department of Chemistry, Sardar Patel University, Vallabh Vidyanagar 388 120, Gujarat, India.
authors.forename: Vishal B
authors.initials: VB
authors.lastname: Purohit
authors.affiliation: Department of Chemistry, Sardar Patel University, Vallabh Vidyanagar 388 120, Gujarat, India.
authors.forename: Rahul P
authors.initials: RP
authors.lastname: Thummar
authors.affiliation: Department of Chemistry, Sardar Patel University, Vallabh Vidyanagar 388 120, Gujarat, India.
authors.forename: Beena K
authors.initials: BK
authors.lastname: Vaghasiya
authors.affiliation: Department of Chemistry, Sardar Patel University, Vallabh Vidyanagar 388 120, Gujarat, India.
authors.forename: Ronak D
authors.initials: RD
authors.lastname: Kamani
authors.affiliation: B. R. Doshi School of Biosciences, Sardar Patel Maidan, Bakrol-Vadtal Road,Satellite Campus, Sardar Patel University, Vallabh Vidyanagar 388120, Gujarat India.
authors.forename: Parth
authors.initials: P
authors.lastname: Thakor
authors.affiliation: B. R. Doshi School of Biosciences, Sardar Patel Maidan, Bakrol-Vadtal Road,Satellite Campus, Sardar Patel University, Vallabh Vidyanagar 388120, Gujarat India.
authors.forename: Vasudev R
authors.initials: VR
authors.lastname: Thakkar
authors.affiliation: Department of Advanced Organic Chemistry, P. D. Patel Institute of Applied Sciences (PDPIAS), Charotar University of Science & Technology (CHARUSAT), Changa 388421, Gujarat, India.
authors.forename: Sampark S
authors.initials: SS
authors.lastname: Thakkar
authors.affiliation: Department of Advanced Organic Chemistry, P. D. Patel Institute of Applied Sciences (PDPIAS), Charotar University of Science & Technology (CHARUSAT), Changa 388421, Gujarat, India.
authors.forename: Arabinda
authors.initials: A
authors.lastname: Ray
authors.affiliation: Department of Chemistry, Sardar Patel University, Vallabh Vidyanagar 388 120, Gujarat, India. Electronic address: dipanalka@yahoo.com.
authors.forename: Dipak K
authors.initials: DK
authors.lastname: Raval
mesh_terms: D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects; D001426:Bacterial Proteins / Q000737:chemistry / Q000378:metabolism; D020134:Catalytic Domain; D060326:Chemistry Techniques, Synthetic; D004353:Drug Evaluation, Preclinical; D005658:Fungi / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D062105:Molecular Docking Simulation; D010069:Oxadiazoles / Q000737:chemistry*; D011804:Quinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000890:Anti-Infective Agents; D001426:Bacterial Proteins; D010069:Oxadiazoles; D011804:Quinolines
keywords: 2-morpholinoquinoline based 1,2,4-oxadiazole; Antimicrobial activity; Cytotoxicity; Molecular docking; Pharmacokinetic study