10325-68-5Relevant academic research and scientific papers
New nicotinic acid-based 3,5-diphenylpyrazoles: design, synthesis and antihyperlipidemic activity with potential NPC1L1 inhibitory activity
Shoman, Mai E.,Aboelez, Moustafa O.,Shaykhon, Montaser Sh. A.,Ahmed, Sanaa A.,Abuo-Rahma, Gamal El-Din A.,Elhady, Omar M.
, p. 673 - 686 (2020/02/25)
Nicotinic acid hydrazide was incorporated into new 4,5-dihydro-5-hydroxy-3,5-diphenylpyrazol-1-yl derivatives. Compounds 6a–h were synthesized, and their antihyperlipidemic activity was evaluated in high cholesterol diet-fed rat model. Compounds 6e, 6f were found to decrease the levels of serum total cholesterol by 14–19% compared to control group. Total triglycerides were also reduced by 24–28% and LDL cholesterol by 16%. As expected from parent niacin, compounds 6e and 6f caused an elevation of HDL cholesterol by 33–41%. Docking study supported the ability of designed compounds to block NPC1L1 active site in a manner similar to that observed with ezetimibe.
Modular access to 1,2-allenyl ketones based on a photoredox-catalysed radical-polar crossover process
Du, Chan,Fang, Jianghua,Fang, Yewen,Lei, Wan,Li, Yan,Liu, Yongjun
, p. 8502 - 8506 (2021/10/20)
Herein, a new protocol dealing with the preparation of 1,2-allenyl ketones has been successfully developedviathe reactions of enynes with radicals enabled by dual photoredox/copper catalysis. Based on the results of a deuteration experiment and the competition reaction between cyclopropanation and allenation, the mechanism based on a photoredox-neutral-catalysed radical-polar crossover process has been proposed. Synthetic applications of allenes have also been demonstrated.
Microwave-assisted dehalogenation of α-haloketones by zinc and ammonium chloride in alcohol
Li, Jian,Ye, Deju,Liu, Hong,Luo, Xiaoming,Jiang, Hualiang
, p. 567 - 575 (2008/04/12)
The treatment of α-haloketones with 1.5 equiv. of Zn and 1 equiv. of NH4Cl in ethanol for 0.5αmin gave the corresponding ketones with excellent yields under microwave irradiation. Vic-dibromides and 2,2-dibromoacetophenone can be efficiently debrominated to alkenes and acetophenones, respectively. Copyright Taylor & Francis Group, LLC.
Imidazo[2,1-b]thiazole derivatives XII. Synthesis and immunoactivity in vitro on human T lymphocyte of several 3-aroylmethyl and 2-aroyl-3-methyl(aryl)-5,6-dihydroimidazo[2,1-b]thiazoles
Robert,Hassanine,Harraga,Seilles
, p. 261 - 271 (2007/10/02)
To estimate the influence of aryl group position on the immunostimulant properties of imidazo[2,1-b]thiazole derivatives, several compounds were obtained and tested, versus tetramisole hydrochloride, on the mobilisation of CD2 receptor by human T lymphocyte. The synthesis use the action of monobrominated β-diketones on the 2-mercaptoimidazoline. So, 1-aryl-4-bromobutane-1,3-diones lead to 3-aroylmethyl-5,6-dihydroimidazo[2,1-b]thiazoles 4. Same, 1-aryl-2-bromobutane-1,3-diones and 1,3-diaryl-2-bromopentane-1,3-diones give respectively 3-aroyl-2-methyl-5,6-dihydroimidazo[2,1-b]thiazoles 5 and 3-aroyl-2-aryl-5,6-dihydroimidazo[2,1-b]thiazoles 6. Better yields are obtained when the reaction presents two steps. The first one, realized in acetone at room temperature, leads to an intermediate S-substituted 4,5-dihydroimidazole which, in second step, is cyclized in imidazo[2,1-b]thiazole compound via an unisolated carbinolamine. This one explains the univocal formation of 5 derivatives and the feasible blending in case of 6. The immunoactivity of several imidazothiazoles 4, 5 and 6 is lower that them of 6-aryl substituted compounds and particularly that the levamisole which is the reference product in this series.
A Convenient Synthesis of β-(1-Imidazoyl)enones from α,β-Dibromoketones
Kashima, C.,Shimizu, M.,Tajima, T.
, p. 961 - 964 (2007/10/02)
As the convenient preparative method of β-(substituted)-phenyl-β-(1-imidazolyl)enones, we succeeded in the preparation of β-aryl-β-(1-imidazolyl)enones from α,β-dibromo-β-arylketones with imidazole in the presence of triethylamine.
