Antimicrobial, anticoagulant, and cytotoxic evaluation of multidrug resistance of new 1,4-dihydropyridine derivatives
| Autor: | Akbar Idhayadhulla, Ibrahim A. Arif, Anis Ahamed, Radhakrishnan Surendra Kumar, Mohammed Mateen |
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| Jazyk: | angličtina |
| Rok vydání: | 2018 |
| Předmět: |
Prothrombin time
biology medicine.diagnostic_test 010405 organic chemistry Chemistry Clotrimazole Pharmacology 010402 general chemistry biology.organism_classification Antimicrobial 01 natural sciences Article 0104 chemical sciences Multiple drug resistance HeLa lcsh:Biology (General) medicine Anticoagulant Agent General Agricultural and Biological Sciences Candida albicans lcsh:QH301-705.5 Partial thromboplastin time medicine.drug |
| Zdroj: | Saudi Journal of Biological Sciences, Vol 25, Iss 6, Pp 1227-1235 (2018) |
| Popis: | A new series of 1,4-dihydropyridine derivatives (2a–h, 3a–e, and 4a–e) were systematically designed and synthesized via ultrasound irradiation methods with easy work-up and good yields. Compounds structures were confirmed by IR, 1H NMR, 13C NMR, and mass spectra. The synthesized compounds were screened for both antimicrobial and anticoagulant activities. Compound 2e (MIC: 0.25 μg/mL) was highly active against Escherichia coli and compound 2c (MIC: 0.5 μg/mL) was also highly active against Pseudomonas aeruginosa compared with ciprofloxacin. (MIC: 1 μg/mL) The antifungal activity of 2c (MIC: 0.5 μg/mL) against Candida albicans was high relative to that of clotrimazole (MIC: 1 μg/mL). Anticoagulant activity was determined by activated partial thromboplastin time (APTT) and prothrombin time (PT) coagulation assays. Compound 4-(4-hydroxyphenyl)-2,6-dimethyl-N3,N5-bis(5-phenyl-1,3,4-thiadiazol-2-yl)-1,4-dihydropyridine-3,5-dicarboxamide 3d (>1000 s in APTT assays) was highly active in anticoagulant screening compared with the reference of heparin.Cytotoxicity was evaluated using HepG2 (liver), HeLa (cervical), and MCF-7 (breast) cancer cell lines, with high toxicities observed for 2c (GI50 = 0.02 μm) against HeLa cell line and 2e (GI50 = 0.03 μm) equipotant against MCF-7 cell line. Therefore, the compounds 2e, 2c and 3d can serve as lead molecules for the development of new classes of antimicrobial and anticoagulant agent. Keywords: Ultrasound irradiation, 1,4-Dihydropyridine derivatives, Anticoagulant activity, Antimicrobial activity, Structure activity relationship |
| Databáze: | OpenAIRE |
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