53623-37-3Relevant articles and documents
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.
AMIDE COMPOUND
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Page/Page column 76-77, (2008/06/13)
Disclosed is a compound represented by the formula (I) or (II) below, or a salt thereof. [In the formulae, ring A represents an optionally substituted ring (which is not a pyrrolidine, piperidine or piperazine); ring B represents an optionally substituted aromatic ring; ring D represents an optionally substituted ring; R1 and R2 independently represent a hydrogen atom or a substituent; R3 represents a hydrogen atom or a C1-6 alkyl group, or alternatively it combines with the ring A to form a non-aromatic ring; ring Aa represents an optionally substituted aromatic hydrocarbon; Y represents CH or N; Ra1 represents an optionally substituted hydrocarbon group; and Ra2 and Ra3 independently represent a hydrogen atom or a substituent.] The compound has a DGAT inhibitory effect and is useful for treatment or improvement of diseases or conditions caused by high expression or high activation of DGAT.
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.