Antimicrobial, anticoagulant, and cytotoxic evaluation of multidrug resistance of new 1,4-dihydropyridine derivatives

Saudi Journal of Biological Sciences
Anis AhamedAkbar Idhayadhulla

Abstract

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 (G...Continue Reading

Citations

Dec 19, 2019·Pharmaceutics·Andrés GonzálezÁngel Lanas
Nov 19, 2019·Mini Reviews in Medicinal Chemistry·Abhinav Prasoon MishraAwani Kumar Rai
Nov 6, 2020·European Journal of Medicinal Chemistry·Yichao WanZilong Tang
Jan 1, 2021·Environmental Pollution·Hannan Safiyyah Tan Sian Hui AbdullahPoh Wai Chia
Dec 24, 2019·ACS Omega·Sandeep V H S BhaskaruniSreekantha B Jonnalagadda

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Methods Mentioned

BETA
NMR
ELISA

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