145784-33-4Relevant articles and documents
CuBr-promoted formal hydroacylation of 1-alkynes with glyoxal derivatives: An unexpected synthesis of 1,2-dicarbonyl-3-enes
Chen, Shufeng,Li, Xiaojie,Zhao, Haiying,Li, Baoguo
, p. 4137 - 4141 (2014/05/20)
An efficient and concise protocol has been developed for the highly regio- and stereoselective synthesis of E-1,2-dicarbonyl-3-ene derivatives by a copper-promoted reaction of 1-alkynes with α-carbonyl aldehydes in the presence of morpholine. The products obtained are believed as the formal hydroacylation of the triple bond.
Design and synthesis of 2,4-disubstituted polyhydroquinolines as prospective antihyperglycemic and lipid modulating agents
Kumar, Atul,Sharma, Siddharth,Tripathi, Vishwa Deepak,Maurya, Ram Awatar,Srivastava, Swayam Prakash,Bhatia, Gitika,Tamrakar,Srivastava, Arvind Kumar
experimental part, p. 4138 - 4148 (2010/08/06)
A series of 2,4-disubstituted polyhydroquinoline were synthesized and evaluated for their in vivo antihyperglycemic as well as antidyslipidemic activities. Several synthesized compounds have exhibited promising in vivo antihyperglycemic in SLM, STZ-S, and db/db mice model along with significant lipid and TG modulating activity. All these compounds were evaluated in various in vitro models of diabetes to know the possible mechanism of their antihyperglycemic action. Interestingly, compounds 3a-r (diaryl substitution) have exhibited promising protein-tyrosine phosphatase 1B (PTP1B) inhibitory activity whereas, compounds 5a-d (acid substituted) have shown significant glycogen phosphorylase activity.
Diaryl dihydropyrazole-3-carboxamides with significant in vivo antiobesity activity related to CB1 receptor antagonism: Synthesis, biological evaluation, and molecular modeling in the homology model
Srivastava, Brijesh Kumar,Joharapurkar, Amit,Raval, Saurin,Patel, Jayendra Z.,Soni, Rina,Raval, Preeti,Gite, Archana,Goswami, Amitgiri,Sadhwani, Nisha,Gandhi, Neha,Patel, Harilal,Mishra, Bhupendra,Solanki, Manish,Pandey, Bipin,Jain, Mukul R.,Patel, Pankaj R.
, p. 5951 - 5966 (2008/04/12)
A number of analogues of diaryl dihydropyrazole-3-carboxamides have been synthesized. Their activities were evaluated for appetite suppression and body weight reduction in animal models. Depending on the chemical modification of the selected dihydropyrazole scaffold, the lead compounds - the bisulfate salt of (±)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4,5-dihydro-1H-pyrazole-3- carboxylic acid morpholin-4-ylamide 26 and the bisulfate salt of (-)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4,5-dihydro-1H-pyrazole-3- carboxylic acid morpholin-4-ylamide 30-showed significant body weight reduction in vivo, which is attributed to their CB1 antagonistic activity and exhibited a favorable pharmacokinetic profile. The molecular modeling studies also showed interactions of two isomers of (±)-5-(4-chlorophenyl)-1-(2,4- dichlorophenyl)-4,5-dihydro-1H-pyrazole-3-carboxylic acid morpholin-4-ylamide 9 with CB1 receptor in the homology model similar to those of N-piperidino-5-(4- chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-3-pyrazole-carboxamide (rimonabant) 1 and 4S-(-)-3-(4-chlorophenyl)-N-methyl-N′-[(4-chlorophenyl) -sulfonyl]-4-phenyl-4,5-dihydro-1H-pyrazole-1-carboxamidine (SLV-319) 2.
