Analgesic, Anti-Inflammatory, and Antiplatelet Profile of Hydrazones Containing Synthetic Molecules

Asif, Mohammad; Husain, Asif

doi:10.1155/2013/247203

Cited by 53 publications

(30 citation statements)

References 44 publications

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“…Hydrazones (―CO―NH―N═CH―) are members of the Schiff bases family and can be a good option in drug development due to their pharmacological properties. They show a wide range of activities including antibacterial, anticancer, antioxidant, antifungal, analgesic, anti‐inflammatory, anticonvulsant, antimalarial, and antitubercular activities.…”

Section: Introductionmentioning

confidence: 99%

Novel fluorine‐containing chiral hydrazide‐hydrazones: Design, synthesis, structural elucidation, antioxidant and anticholinesterase activity, andin silicostudies

et al. 2019

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In this study, a series of fluorine‐containing chiral hydrazide‐hydrazone derivatives [III‐XII] from ʟ‐cysteine ethyl ester hydrochloride was synthesized as new antioxidant and anticholinesterase agents. The antioxidant activity of these derivatives was evaluated by ABTS+· and DPPH· scavenging and CUPRAC assays and the anticholinesterase activity by the Ellman method spectrophotometrically. The results of the antioxidant assay showed that compounds V, IX, and X exhibited higher activity than BHT and α‐tocopherol used as positive standards. Among the synthesized derivatives, compound IX (IC50: 2.3 ± 1.6 μM) exhibited higher acetylcholinesterase inhibitory activity than galantamine (IC50: 4.5 ± 0.8 μM). Compounds XI (IC50: 9.6 ± 1.0 μM), IX (IC50: 12.5 ± 1.6 μM), III (IC50: 16.0 ± 1.6 μM), X (IC50: 17.2 ± 1.8 μM), VI (IC50: 20.2 ± 0.8 μM), XII (IC50: 21.5 ± 1.0 μM), and VII (IC50: 24.6 ± 0.6 μM) displayed better butyrylcholinesterase inhibitory activity than galantamine (IC50: 46.03 ± 0.14 μM). ADME‐Tox analysis was used to probe the drug‐like properties of the compounds. Molecular docking studies were also applied to understand the interactions between compounds and targets. The docking calculations were supported by the experimental data. In particular, compound IX, having better activity than galantamine against acetylcholinesterase and butyrylcholinesterase enzymes, was visualized using molecular docking.

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Section: Introductionmentioning

confidence: 99%

Novel fluorine‐containing chiral hydrazide‐hydrazones: Design, synthesis, structural elucidation, antioxidant and anticholinesterase activity, andin silicostudies

et al. 2019

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“…This concept has been widely used in the literature for the design of kinase-protein and serine-protease inhibitors, and ligands of G-protein coupled receptors (GPCR) and ionic channels [ 1 ]. Recently, based on several works with bioactive N -acylhydrazone (NAH) derivatives [ 2 , 3 , 4 , 5 , 6 , 7 ], the privileged structure nature of this bioactive framework was proposed [ 5 ].…”

Section: Introductionmentioning

confidence: 99%

Novel Orally Active Analgesic and Anti-Inflammatory Cyclohexyl-N-Acylhydrazone Derivatives

et al. 2015

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The N-acylhydrazone (NAH) moiety is considered a privileged structure, being present in many compounds with diverse pharmacological activities. Among the activities attributed to NAH derivatives anti-inflammatory and analgesic ones are recurrent. As part of a research program aiming at the design of new analgesic and anti-inflammatory lead-candidates, a series of cyclohexyl-N-acylhydrazones 10–26 were structurally designed from molecular modification on the prototype LASSBio-294, representing a new class of cycloalkyl analogues. Compounds 10–26 and their conformationally restricted analogue 9 were synthetized and evaluated as analgesic and anti-inflammatory agents in classical pharmacologic protocols. The cyclohexyl-N-acylhydrazones 10–26 and the cyclohexenyl analogue 9 showed great anti-inflammatory and/or analgesic activities, but compound 13 stood out as a new prototype to treat acute and chronic painful states due to its important analgesic activity in a neuropathic pain model.

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“…Hydrazones constitute another important class of pharmacologically active drug molecules which has attracted the attention of medicinal chemists due to their diverse biological activities such as analgesic, anthelmintic, anticonvulsant, antidepressant, anti-inflammatory, antimalarial, anticancer, antiviral, and antibacterial [24]. Some commercially available antibacterial drugs such as furacilin, furazolidone, ftivazide, nifuroxazide, nirofurazone, and nitrofurantoin are known to contain hydrazone group [25][26][27].…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Characterization and in Vitro Antimicrobial Evaluation of Some Novel Benzimidazole Derivatives Bearing Hydrazone Moiety

Sarma

Singh

Gupta

et al. 2017

Asian J Pharm Clin Res

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Objective: The synthesis of novel benzimidazole-hydrazone derivatives has been carried out based on the previous findings that both these pharmacophores possess potent antimicrobial activities. The antibacterial properties of synthesized derivatives were screened against both Grampositive and Gram-negative bacteria.Methods: O-phenylenediamine on condensation with substituted aromatic acids in polyphosphoric acid gave benzimidazole nucleus which on reaction with ethyl chloroacetate and hydrazine hydrate in two different steps resulted in the formation of substituted acetohydrazides. The targeted compounds 6a-l were synthesized by reaction of substituted acetohydrazides with aromatic aldehydes and screened for their antibacterial potential by cup-plate method. Results:The synthesized benzimidazole-hydrazones exhibited moderate to strong antibacterial activities against Staphylococcus aureus, Bacillus subtilis, Escherichia coli, and Pseudomonas aeruginosa. The compounds 6a-6f were found to be most effective against S. aureus, E. coli, and P. aeruginosa. Among all the synthesized compounds, the zone of inhibition of 6f in highest concentration, i.e., 100 µg/ml were found to be >31 mm against all the stains of bacteria. Conclusion:The antibacterial results revealed that the synthetized derivatives have significant antimicrobial properties and further structure activity relationship studies may develop more potent and less toxic molecules.

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Analgesic, Anti-Inflammatory, and Antiplatelet Profile of Hydrazones Containing Synthetic Molecules

Cited by 53 publications

References 44 publications

Novel fluorine‐containing chiral hydrazide‐hydrazones: Design, synthesis, structural elucidation, antioxidant and anticholinesterase activity, andin silicostudies

Novel fluorine‐containing chiral hydrazide‐hydrazones: Design, synthesis, structural elucidation, antioxidant and anticholinesterase activity, andin silicostudies

Novel Orally Active Analgesic and Anti-Inflammatory Cyclohexyl-N-Acylhydrazone Derivatives

Synthesis, Characterization and in Vitro Antimicrobial Evaluation of Some Novel Benzimidazole Derivatives Bearing Hydrazone Moiety

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