Synthesis and pharmacological evaluation of novel heterotricyclic acylhydrazone derivatives, designed as PAF antagonists

Fraga, Aline Guerra Manssour; Rodrigues, Carlos Rangel; Miranda, Ana Luísa P.; Barreiro, Eliezer J.; Fraga, Carlos A. M.

doi:10.1016/s0928-0987(00)00102-0

Cited by 39 publications

(20 citation statements)

References 16 publications

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“…Benzylidene-/ 4′-bromobenzylidene 3-hydroxy-8-methyl-6-phenylpyrazolo [3,4-b]thieno-[2,3-d]pyridine-2-carbohydrazide were evaluated at 10 μM, presenting, respectively, 10.4 and 13.6% of inhibition of the PAF-induced platelet aggregation [24].…”

Section: Analgesic Antiinflammatory and Antiplatelet Activitymentioning

confidence: 99%

Biological Activities of Hydrazone Derivatives

2007

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There has been considerable interest in the development of novel compounds with anticonvulsant, antidepressant, analgesic, antiinflammatory, antiplatelet, antimalarial, antimicrobial, antimycobacterial, antitumoral, vasodilator, antiviral and antischistosomiasis activities. Hydrazones possessing an azometine -NHN=CH-proton constitute an important class of compounds for new drug development. Therefore, many researchers have synthesized these compounds as target structures and evaluated their biological activities. These observations have been guiding for the development of new hydrazones that possess varied biological activities.

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Section: Analgesic Antiinflammatory and Antiplatelet Activitymentioning

confidence: 99%

Biological Activities of Hydrazone Derivatives

2007

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“…The evaluation of platelet antiaggregating profile let to the identification of a new potent prototype of antiplatelet derivative, that is, benzylidene 10H-phenothiazine-1-carbohydrazide (IC 50 = 2.3 M), which acts in the AA pathway probably by the inhibition of platelet COX-1 enzyme. Additionally, the change in para-substituent group of acylhydrazone framework permitted to identify a hydrophilic carboxylate derivative and a hydrophobic bromo derivative as two new analgesics that are more potent than dipyrone, possessing selective peripheral or central mechanism of action [47]. The evaluation of platelet antiaggregating profile let to the identification of a new potent prototype, that is, benzylidene 10H-phenothiazine-1-carbohydrazide (IC 50 = 2.3 M) (12), which acts in the arachidonic acid (AA) pathway probably by the inhibition of platelet COX-1 enzyme.…”

Section: Antiplatelet Activitymentioning

confidence: 99%

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

Asif

Husain

2013

Journal of Applied Chemistry

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Hydrazones are present in many of the bioactive compounds with wide interest because of their diverse pharmacological applications. Hydrazones possess wide variety of biological activities such as anticonvulsant, antidepressant, analgesic, anti-inflammatory, antiplatelet, antimicrobial, anticancer, antihypertensive, anthelmintic, antidiabetic, antiparasitic, and other anticipated activities. This created an interest for researchers towards synthesized variety of hydrazone derivatives for different biological activities. Therefore many researchers have synthesized hydrazone derivatives as target structures for their biological activities. This is paper focuses on the analgesic, anti-inflammatory, and antiplatelet activities of hydrazones.

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“…The antiplatelet activity of novel tricyclic acylhydrazone derivatives was evaluated by their ability to inhibit platelet aggregation of rabbit platelet-rich plasma (16). The arylhydrazone chelator 2-hydroxy-1-naphthylaldehyde isonicotinoyl hydrazone showed greater antimalarial agent activity than did desferrioxamine against chloroquine-resistant and -sensitive parasites (17).…”

Section: Introductionmentioning

confidence: 99%