53623-37-3Relevant academic research and scientific papers
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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, (2008/06/13)
The present invention relate to a compound represented by the formula (I) or (II) wherein ring A is an optionally substituted ring (the ring should not be pyrrolidine, piperidine and piperazine), ring B is an optionally substituted aromatic ring, ring D is an optionally substituted ring, R1 and R2 are each independently a hydrogen atom or a substituent, R3 is a hydrogen atom or a C1-6 alkyl group, or R3 is bonded to ring A to form a non-aromatic ring, ring Aa is an optionally substituted aromatic hydrocarbon, Y is CH or N, Ra1 is an optionally substituted hydrocarbon group, and Ra2 and Ra3 are each independently a hydrogen atom or a substituent, or a salt thereof. The present invention provides a compound having a DGAT inhibitory activity, which is useful for the treatment or amelioration of diseases or pathologies caused by high expression or high activation of DGAT.
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.
Kinetics and mechanism of oxidation of beta benzoylpropionic acids by pyridinium fluorochromate in aqueous acetic acid medium
Kavitha,Pandurangan,Alphonse
, p. 715 - 718 (2007/10/03)
The kinetics of oxidation of beta benzoylpropionic acid and para substituted beta benzoylpropionic acids(KA) by pyridinium fluorochromate(PFC) has been studied in aqueous acetic acid medium in the presence of perchloric acid. The reaction follows first order kinetics each with respect to [PFC], [KA] and [H+]. Electron withdrawing substituents are found to retard the reaction and electron releasing substituents are found to increase the rate of reaction and the rate data obey the Hammett relationship. The products of the oxidation are the corresponding acids. The activation enthalpies and entropies are calculated and the possible mechanism for oxidation reaction is discussed.
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.
