1,1-Diphenyl-2-picrylhydrazyl radical scavenging activity of novel dihydropyridine derivatives

Anwar, Ayaz; Hameed, Abdul; Perveen, Shahida; Uroos, Maliha; Choudhary, Muhammad Iqbal; Basha, Fatima Zahra

doi:10.5155/eurjchem.5.1.189-191.916

Cited by 2 publications

(1 citation statement)

References 17 publications

(19 reference statements)

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“…Compound 1a had the lowest antioxidant effects because of the absence of any electron releasing groups. Anwar et al [15] synthesized dihydropyridine analogs and determined their DPPH radical scavenging activities. The IC50 values of the compounds were found to range from 127.40 ± 3.50 µM to 284.50 ± 0.66 µM.…”

Section: Antioxidant Activitymentioning

confidence: 99%

Synthesis, characterization and investigation of cholinesterase enzyme inhibition and antioxidant activities of some 4-aryl-1,4-dihydropyridine derivatives

Sellitepe¹,

Doğan²,

Eroglu³

et al. 2019

jrp

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The aim of this study is to synthesize and characterize 4-aryl-1,4-dihydropyridine derivatives and evaluate their antioxidant and cholinesterase inhibitory properties. Hantzsch reaction was used in the synthesis of compounds; the compounds were prepared by the reaction of methyl 3-acetoacetate, appropriate aromatic aldehyde, ammonia and catalyst. The reactions were carried out in the presence of copper sulfate (for Method A) and boric acid /acetic acid catalyst (for Method B). CuSO4 was used as a catalyst for the Hantzsch reaction for the first time. The structure of the synthesized compounds were characterized by IR and 1 H-NMR spectral studies. Furthermore, the enzym (acetylcholinesterase and butyrylcholinesterase) inhibition activity of the synthesized compounds was evaluated using Ellman's spectrophotometrical method as a novel approach. Antioxidant studies of the synthesized compounds were performed by measuring the 1,1-diphenyl-2-picrylhydrazyl radical scavenging assay, phosphomolibdenumreducing antioxidant power assay, and metal chelating activity test. Results showed that 4-bromo substituted derivative (1b) has the highest antioxidant activity compared to other tested compounds. Moreover, compound 1b also has higher cholinesterase inhibitory effect (34.05 ± 2.23% and 24.93 ± 0.68% at 250 µM) than other tested compounds. In this study, eight 1,4-dihydropyridine derivatives, dimethyl 4-(phenyl/substituted phenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5dicarboxylate compounds were synthesized according to the Hantzsch reaction, using CuSO4 as a catalyst, for the first time. Compared to the classical reaction conditions, the presence of catalyst has been offered several advantages such as excellent good yields and short reaction times.

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Section: Antioxidant Activitymentioning

confidence: 99%

Synthesis, characterization and investigation of cholinesterase enzyme inhibition and antioxidant activities of some 4-aryl-1,4-dihydropyridine derivatives

Sellitepe¹,

Doğan²,

Eroglu³

et al. 2019

jrp

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Synthetic Dihydropyridines as Novel Antiacanthamoebic Agents

Anwar

Siddiqui

Hameed

et al. 2020

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Background: Acanthamoeba is an opportunistic pathogen widely spread in the environment. Acanthamoeba causes excruciating keratitis which can lead to blindness. The lack of effective drugs and its ability to form highly resistant cyst are one of the foremost limitations against successful prognosis. Current treatment involves mixture of drugs at high doses but still recurrence of infection can occur due to ineffectiveness of drugs against the cyst form. Pyridine and its natural and synthetic derivatives are potential chemotherapeutic agents due to their diverse biological activities. Objective: To study the antiamoebic effects of four novel synthetic dihydropyridine (DHP) compounds against Acanthamoeba castellanii belonging to the T4 genotype. Furthermore, to evaluate their activity against amoeba-mediated host cells cytopathogenicity as well as their cytotoxicity against human cells. Method: Dihydropyridines were synthesized by cyclic dimerization of alkylidene malononitrile derivatives. Four analogues of functionally diverse DHPs were tested against Acanthamoeba castellanii by using amoebicidal, encystation and excystation assays. Moreover, Lactate dehydrogenase assays were carried out to study cytopathogenicity and cytotoxicity against human cells. Results: These compounds showed significant amoebicidal and cysticidal effects at 50 µM concentration, whereas, two of the DHP derivatives also significantly reduced Acanthamoeba-mediated host cell cytotoxicity. Moreover, these DHPs were found to have low cytotoxicity against human cells suggesting a good safety profile, and they can be employed as therapeutic agents. Conclusion: The results suggest that DHPs have potential against Acanthamoeba especially against the more resistant cyst stage and can be assessed further for drug development.

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1,1-Diphenyl-2-picrylhydrazyl radical scavenging activity of novel dihydropyridine derivatives

Cited by 2 publications

References 17 publications

Synthesis, characterization and investigation of cholinesterase enzyme inhibition and antioxidant activities of some 4-aryl-1,4-dihydropyridine derivatives

Synthesis, characterization and investigation of cholinesterase enzyme inhibition and antioxidant activities of some 4-aryl-1,4-dihydropyridine derivatives

Synthetic Dihydropyridines as Novel Antiacanthamoebic Agents

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