89144-77-4Relevant academic research and scientific papers
Anticonvulsant activity of a combined pharmacophore of pyrazolo-pyridines with lesser toxicity in mice
Siddiqui, Nadeem,Ahsan, Waquar,Alam, M. Shamsher,Ali, Ruhi,Srivastava, Kamna,Ahmed, Sharique
, p. 576 - 582 (2011/12/03)
Various 2-amino-6-[3-(substituted phenyl)-5-phenyl-4,5-dihydropyrazol-1-yl] -4-(substituted phenyl)nicotinonitriles (3a-t) were designed and synthesized by clubbing two active anticonvulsant pharmacophores pyrazole and pyridine. All the synthesized compounds possessed the pharmacophoric elements essential for good anticonvulsant activity. The anticonvulsant screening was performed by maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole (scPTZ) tests. Two compounds 3i and 3s showed significant anticonvulsant activity in both the screens with ED50 values 17.5 mg/kg and 22.6 mg/kg respectively in MES screen and 154.1 mg/kg and 242.6 mg/kg respectively in scPTZ screen. They were also found to have no acute toxic effects in mice when tested at elevated doses.
Design, synthesis, and structure-activity relationships of pyrazole derivatives as potential FabH inhibitors
Lv, Peng-Cheng,Sun, Juan,Luo, Yin,Yang, Ying,Zhu, Hai-Liang
scheme or table, p. 4657 - 4660 (2010/09/16)
Fatty acid biosynthesis is essential for bacterial survival. FabH, β-ketoacyl-acyl carrier protein (ACP) synthase III, is a particularly attractive target, since it is central to the initiation of fatty acid biosynthesis and is highly conserved among Gram-positive and -negative bacteria. Fifty-six 1-acetyl-3,5-diphenyl-4,5-dihydro-(1H)-pyrazole derivatives were synthesized and developed as potent inhibitors of FabH. This inhibitor class demonstrates strong antibacterial activity. Escherichia coli FabH inhibitory assay and docking simulation indicated that the compounds 1-(5-(4-fluorophenyl)- 3-(4-methoxyphenyl)-4,5-dihydro-1H-pyrazol-1-yl)ethanone (12) and 1-(5-(4-chlorophenyl)-3-(4-methoxyphenyl)-4,5-dihydro-1H-pyrazol-1-yl)ethanone (13) were potent inhibitors of E. coli FabH.
Kinesin spindle protein (KSP) inhibitors. Part 1: The discovery of 3,5-diaryl-4,5-dihydropyrazoles as potent and selective inhibitors of the mitotic kinesin KSP
Cox, Christopher D.,Breslin, Michael J.,Mariano, Brenda J.,Coleman, Paul J.,Buser, Carolyn A.,Walsh, Eileen S.,Hamilton, Kelly,Huber, Hans E.,Kohl, Nancy E.,Torrent, Maricel,Yan, Youwei,Kuo, Laurence C.,Hartman, George D.
, p. 2041 - 2045 (2007/10/03)
Optimization of high-throughput screening (HTS) hits resulted in the discovery of 3,5-diaryl-4,5-dihydropyrazoles as potent and selective inhibitors of KSP. Dihydropyrazole 15 is a potent, cell-active KSP inhibitor that induces apoptosis and generates aberrant mitotic spindles in human ovarian carcinoma cells at low nanomolar concentrations. X-ray crystallographic evidence is presented which demonstrates that these inhibitors bind in an allosteric pocket of KSP distant from the nucleotide and microtubule binding sites.
Synthesis and reactions of 4-[3-oxo-1-phenyl-3-(p-substituted phenyl)-propyl]-1-4-chloro-phenyl-2-(3-methyl-5-oxo-2-pyrazolin-1-yl) thiazole
Hamad,Said,Amer,Yassin,El-Gendy
, p. 27 - 30 (2007/10/03)
Compounds 4-[3-oxo-1-phenyl-3-(p-chloro or p-methoxyphenyl)-propyl]-1-[4-chlorophenyl)-2-(3-methyl-5-oxo-2-pyrazolin-1-yl)] -thiazole (II a-b) have been prepared. The reactions of compounds (II a-b) with hydrazines in ethanol and in acetic acid, hydroxylamine hydrochloride, aromatic aldehydes, zinc dust, Grignard reagents, P2S5 and polyphosphoric acid have been investigated.
Heterocycles. 3. Synthesis and Spectral Data of Some 2-Pyrazolines
El-Rayyes, Nizar R.,Hovakeemian, George H.,Hmoud, Hayat S.
, p. 225 - 229 (2007/10/02)
The reaction of 1,3-diaryl-2-propen-1-ones (Ia-o) with hydrazine and methyl- and phenylhydrazine produced different substituted 2-pyrazolines (III).The structures of these products were evident from their chemical and spectroscopic analysis.
