Design and synthesis of pyridazinone-based 5-HT2C agonists

Allerton, Charlotte; Andrews, M. D.; Blagg, Julian; Ellis, David; E, Evrard; Green, Martin P.; Liu, Kevin K.‐C.; McMurray, Gordon; Ralph, Michael J.; Sanderson, Vivienne; Ward, Robin V.; Watson, Lesa

doi:10.1016/j.bmcl.2009.07.136

Cited by 31 publications

(12 citation statements)

References 17 publications

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“…The pyridazinone-based as 5-HT(2C) agonists [7]. Pyridazinone derived compound with excellent levels of 5-HT(2C) functional agonism and selectivity over 5-HT(2A) and 5-HT(2B) and exhibited good efficacy in stress urinary incontinence [110]. Diaryl pyridazine-3-ones evaluated as aldose reductase inhibitory activity [111].…”

Section: Miscellenous Activitiesmentioning

confidence: 99%

Pharmacological activities of pyridazines and pyridazinone Derivatives: A Review on biologically active scaffold

Abida¹,

Alam²,

Asif³

2019

SARJPS

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Pyridazine and pyridazinone derivatives compounds are biologically important compounds. Pyridazinone has carbonyl group on third carbon on pyridazine ring. Pyridazine and pyridazinone is a wonder nucleus because their derivatives give amost all types of biological activities such as such as analgesic, antiinflammatory, antimicrobial, antisecretory, antiulcer, antidepressants, neuroleptics, anxiolytics, sedative, hypnotic, tranquillizer, anticonvulsant, antiplatelet, antithrombotics, anticancer, antihistamine, cardiotonics, vasodilatators, antiarrhythmics, antidiabetic, antihypertensive, antitubercular and various other types of activities. These compounds are synthesized with the aim of novel agents those possess interesting biological activities. The present review has been focused on the pyridazine and pyridazinone derivatives with potential pharmacologica activities.

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Section: Miscellenous Activitiesmentioning

confidence: 99%

Pharmacological activities of pyridazines and pyridazinone Derivatives: A Review on biologically active scaffold

Abida¹,

Alam²,

Asif³

2019

SARJPS

View full text Add to dashboard Cite

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“…The SAR of a series of pyridazinone derived 5-HT(2C) agonists has been explored and resulted in identification of a compound with excellent levels of 5-HT(2C) functional agonism and selectivity over 5-HT(2A) and 5-HT(2B). This compound showed good in vivo efficacy in pre-clinical models of stress urinary incontinence, despite having physiochemical properties commensurate with impaired CNS penetration (Allerton at al., 2009). Synthesis and vasodilatory activity of some amide derivatives of 6-(4-carboxymethyloxyphenyl)-4,5-dihydro-3(2H)pyridazinone (23) are reported.…”

Section: Biological Activitiesmentioning

confidence: 99%

Diverse chemical and biological potentials of various pyridazine and pyridazinone derivatives

Int¹

2019

Preprint

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A series of heterocyclic compounds incorporating pyridazine moiety were for diverse biological activities. Pyridazines and pyridazinones derivatives showed wide spectrum of biological activities such as vasodialator, cardiotonic, anticonvulsant, antihypertensive, antimicrobial, anti-inflammatory, analgesic, anti-feedant, herbicidal, and various other biological, agrochemical and industrial chemical activities. The results illustrated that the synthesized pyridazine/pyridazine compounds have diverse and significant biological activities. Mechanistic insights into the biological properties of pyridazinone derivatives and various synthetic techniques used for their synthesis are also described.

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“…In view of above facts, there is an ongoing research on pyridazine compounds, particularly in relation to microbial infections. [9][10][11] Tuberculosis an Overview TB is a chronic infectious disease caused by mycobacterium species of the "TB complex", including primarily M. tuberculosis, that divides every 16-20 h, an extremely slow rate compared with other bacteria, which usually divide in less than an hour, but M. bovis, M. africanum, M. canetti, and M. microti can also cause TB, but these species do not usually infect healthy adults. TB is an air-borne communicable disease caused by transmission of aerosolized droplets of M. tuberculosis.…”

Section: Introductionmentioning

confidence: 99%

Development of structurally diverse antitubercular molecules with pyridazine ring

2013

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There has been considerable interest in the development of new molecule with antibacterial activities particularly against tuberculosis because mycobacterium species have developed resistance against currently used drugs, their toxic effect, and longer duration of therapy. The pyridazine derivatives are an important class of compound for new drugs research and development. Therefore, many researchers have synthesized these compounds as target structures and evaluated their antitubercular activity. These observations have been guiding in the development of new molecules that possess potent antitubercular activity with minimum side effects or effective against multidrug-resistant, extensively drug-resistant mycobacterium strains, and also in patient co-infected with HIV/AIDS.

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Design and synthesis of pyridazinone-based 5-HT2C agonists

Cited by 31 publications

References 17 publications

Pharmacological activities of pyridazines and pyridazinone Derivatives: A Review on biologically active scaffold

Pharmacological activities of pyridazines and pyridazinone Derivatives: A Review on biologically active scaffold

Diverse chemical and biological potentials of various pyridazine and pyridazinone derivatives

Development of structurally diverse antitubercular molecules with pyridazine ring

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