- New nicotinic acid-based 3,5-diphenylpyrazoles: design, synthesis and antihyperlipidemic activity with potential NPC1L1 inhibitory activity
-
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.
- Shoman, Mai E.,Aboelez, Moustafa O.,Shaykhon, Montaser Sh. A.,Ahmed, Sanaa A.,Abuo-Rahma, Gamal El-Din A.,Elhady, Omar M.
-
-
Read Online
- A one-pot and three-component synthetic approach for the preparation of asymmetric and multi-substituted 1,4-dihydropyrazines
-
An efficient, one-pot and three-component synthesis of a new series of 2-acyl-3,4,6-triaryl-1,4-dihydropyrazines is described. This two-step strategy involves treatment of phenacyl bromides and anilines to give the nucleophilic substitution intermediate f
- Peytam, Fariba,Adib, Mehdi,Shourgeshty, Reihaneh,Rahmanian-Jazi, Mahmoud,Jahani, Mehdi,Larijani, Bagher,Mahdavi, Mohammad
-
supporting information
(2019/11/11)
-
- A new synthetic strategy towards 2,4,5-trisubstituted 1H-imidazoles and highly substituted pyrrolo[1,2-c]imidazoles by use of α-azidochalcones via Michael addition-cyclization followed by Wittig reaction
-
Efficient and facile protocols for the preparation of highly functionalized 1H-imidazoles and 5H-pyrrolo[1,2-c]imidazoles are described. Heating a mixture of an α-azidochalcones and N,N,N′,N′-tetramethyl guanidine under neat conditions gave the corresponding 2,4,5-trisubstituted 1H-imidazole via Michael addition-cyclization in excellent yields. Subsequently, the prepared 1H-imidazoles undergo addition-Wittig reaction with acetylenic esters in presence of triphenylphosphine in dichloromethane to afford 5H-pyrrolo[1,2-c]imidazoles in high yields.
- Adib, Mehdi,Peytam, Fariba,Rahmanian-Jazi, Mahmoud,Bijanzadeh, Hamid Reza,Amanlou, Massoud
-
p. 6696 - 6705
(2017/10/25)
-
- New Derivatives of N-Vinyltriazoles: 1,3-Diaryl-3-(1H-1,2,4-triazol-1-yl)-2-propen-1-ones
-
We have synthesized previously unknown N-vinyltriazoles: 1,3-diaryl-3-(1H-1,2,4-triazol-1-yl)-2-propen-1-ones.We discusss a hypothesis for a probable reaction mechanism.
- Rekhter, M. A.,Grushetskaya, G. N.,Panasenko, A. A.,Krimer, M. Z.
-
p. 792 - 796
(2007/10/03)
-
- 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
-
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.
- Robert,Hassanine,Harraga,Seilles
-
p. 261 - 271
(2007/10/02)
-
- Synthesis and antimicrobial activity of 1-(4-chlorophenyl)-3-(4-methoxy/3,4-dimethoxyphenyl)propan-1,3-diones and their 2-analogs
-
The condensation of substituted acetophenones 1-5 with 4-methoxy- or 3,4-dimethoxy-benzaldehyde (6,7) in ethanolic NaOH gives the corresponding substituted 2-propen-1-ones (8-17) which on bromination yields substituted propan-1-ones (18-27).Refluxing of 1
- Singh, Rajvir,Malik, Om Parkash
-
p. 455 - 459
(2007/10/02)
-