36725-34-5Relevant academic research and scientific papers
Synthesis, anti-convulsant activity and molecular docking study of novel thiazole pyridazinone hybrid analogues
Khisal, Subuhi,Mishra, Ravinesh,Partap, Sangh,Siddiqui, Aness Ahmad,Yar, Mohammad Shahar
, (2020)
Pyridazinone analogues have been known to be potential candidates for anticonvulsant agents. We have identified several pyridazinone-based anticonvulsant agents. As a continuation to our previous research, a series of hybrid pyridazinone-thiazole connected through amide linkage were designed and synthesized. Among these, compound SP-5F demonstrated significant anticonvulsant activity with median effective dose of 24.38 mg/kg (MES) and 88.23 mg/kg (scPTz). Results of GABA estimation showed a marked increase in the GABA level when compared with control. Molecular docking studies at the active site of GABA receptor, further confirmed the GABA modulatory effects of SP-5F.
6-PHENYL-4,5-DIHYDROPYRIDAZIN-3(2H)-ONE DERIVATIVES AS PDE3A AND PDE3B INHIBITORS FOR TREATING CANCER
-
Page/Page column 215, (2019/02/15)
The present invention provides 6-phenyl-4,5-dihydropyridazin-3(2H)- one derivatives of formula (I) : The present invention provides 6-phenyl-4,5-dihydropyridazin-3(2H)- one derivatives of formula (I) :
Design, Synthesis, and Pharmacological Screening of Pyridazinone Hybrids as Anticonvulsant Agents
Partap, Sangh,Yar, Mohammad Shahar,Hassan, Md. Zaheen,Akhtar, Md. Jawaid,Siddiqui, Anees A.
, (2017/10/06)
A series of new hybrid benzimidazole containing pyridazinones derivatives were designed and synthesized in accordance with the pharmacophoric requirements essential for the anticonvulsant activity. The synthesized compounds were evaluated for anticonvulsant activity on mice by the gold standard maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ)-induced seizure models. Among the compounds tested, SS-4F showed significant anticonvulsant activity in both the screens with ED50 values of 25.10 and 85.33 mg/kg in the MES and scPTZ screens, respectively. Compound SS-4F emerged as safer and effective anticonvulsant due to its several-fold higher protective indices. Further, the gamma-aminobutyric acid (GABA) estimation result showed a marked increase in the GABA level (1.7-fold) as compared to the control, which was further confirmed by good binding properties with the GABAA receptor.
Syntheses and antiinflammatory activity of some 6-aryl-2,3,4,5-tetrahydro-3-pyridazinones
Khan,Siddiqui
, p. 614 - 619 (2007/10/03)
6-Aryl-2, 3, 4, 5-tetrahydro-3-pyridazinones (2c-22c) are obtained by dehydrocyclisation of various hydrazides formed by the reaction of appropriate methyl β-aroylpropionate and hydrazine hydrate in the presence of anhydrous sodium acetate. They show promising antiinflammatory activity during their evaluation by carrageenin induced paw edema test in rats.
Substituted phenyl-1,2,4-triazolo[2,3-b]pyridazin-3(2H)ones as anti-asthma agents
-
, (2008/06/13)
Substituted phenyl-1,2,4-triazolo[4,3-b]pyridazin-3(2H)-ones, useful as anti-asthma agents.
Substituted 6-phenyl-3(2H)-pyridazinones useful as cardiotonic agents
-
, (2008/06/13)
Substituted 6-phenyl-3(2H)-pyridazinone compounds are useful as cardiotonic agents. Said compounds cause a significant increase in myocardial contractility in the anesthetized dog. Said compounds are produced by reacting substituted γ-oxobenzenebutanoic acids with suitably substituted hydrazines to provide 6-phenyl-4,5-dihydro-3(2H)-pyridazinones which are dehydrogenated to the desired product. The intermediate 6-phenyl-4,5-dihydro-3(2H)-pyridazinones are themselves useful as cardiotonic agents.
Synthesis and Anxiolytic Activity of 6-(Substituted-phenyl)-1,2,4-triazolopyridazines
Albright, J. D.,Moran, D. B.,Wright, W. B.,Collins, J. B.,Beer, B.,et al.
, p. 592 - 600 (2007/10/02)
The synthesis of a series of 6-(substituted-phenyl)-1,2,4-triazolopyridazines (VIII) is reported.Some of these derivatives show activity in tests predictive of anxiolytic activity (a) protection against pentylenetetrazole-induced convulsions; (b)
Agricultural fungicidal compositions containing 6-(substituted phenyl)-pyridazinones and said pyridazinones
-
, (2008/06/13)
Agricultural fungicidal compositions containing as an active ingredient one or more of 6-(substitutedphenyl)-3(2H)-pyridazinone compounds, salts thereof and 6-(substituted-phenyl)-4,5-dihydro-3(2H)-pyridazinone compounds, as well as new pyridazinone compo
