40871-01-0Relevant academic research and scientific papers
Iodine-alumina catalyzed Aza- michael addition under solvent free conditions
Saikia, Monmi,Kakati, Dwipen,Joseph, Maria Stalin,Sarma, Jadab Chandra
experimental part, p. 654 - 658 (2010/06/15)
An efficient aza-Michael addition of amines to a variety of activated olefins was carried out under solvent free conditions using iodine-alumina as a catalyst at room temperature or under microwave irradiation (in case of solid) in high yield. 2009 Bentham Science Publishers Ltd.
N-, α-, and β-substituted 3-aminopropionic acids: Design, syntheses and antiseizure activities
Tan,Wainman,Weaver
, p. 113 - 121 (2007/10/03)
A treatment for epilepsy is proposed based on analogues of 3-aminopropionic acid (β-alanine), a putative neurotransmitter in the central nervous system (CNS). A model three point pharmacophore was proposed based on modelling data obtained from the study of antagonists for both the glial γ-aminobutyric acid (GABA)-uptake site and the glycine co-agonist site of N-methyl-D-aspartate (NMDA) receptor. Three series of 3-aminopropionic acids containing, N-, α-, and β-substituents, were designed and synthesized to probe the position and the size of a lipophilic binding pocket within the proposed pharmacophore. These analogues were tested in vivo for both their antiseizure activities and their neurologic toxicities. Among the fourteen novel 3-aminopropionic acids synthesized, eight were found to have promising antiseizure activity. This study shows that substitution on the N-terminus confers the greatest antiseizure activity, particularly against pilocarpine-induced seizures.
Peptidomimetics of efflux pump inhibitors potentiate the activity of levofloxacin in Pseudomonas aeruginosa
Renau, Thomas E.,Leger, Roger,Yen, Rose,She, Miles W.,Flamme, Eric M.,Sangalang, Joan,Gannon, Carla L.,Chamberland, Suzanne,Lomovskaya, Olga,Lee, Ving J.
, p. 763 - 766 (2007/10/03)
Several classes of peptidomimetics of the efflux pump inhibitor D-ornithine-D-homophenylalanine-3-aminoquinoline (MC-02,595) have been prepared and evaluated for their ability to potentiate the activity of the fluoroquinolone levofloxacin in Pseudomonas a
Design and synthesis of potent and selective inhibitors of integrin VLA-4
Wattanasin, Sompong,Weidmann, Beat,Roche, Didier,Myers, Stewart,Xing, Amy,Guo, Qin,Sabio, Michael,Von Matt, Peter,Hugo, Ronald,Maida, Susan,Lake, Philip,Weetall, Marla
, p. 2955 - 2958 (2007/10/03)
The synthesis and identification of a novel series of inhibitors of integrin VLA-4 are described. Their in vitro activity and selectivity against closely related integrins are also presented.
The synthesis of lactam analogues of fentanyl
Micovic, Ivan V.,Roglic, Goran M.,Ivanovic,Dosen-Micovic, Ljiljana,Kiricojevic, Vesna D.,Popovic, Jelena B.
, p. 2041 - 2050 (2007/10/03)
Fentanyl, sufentanil and alfentanil are clinically widely used anaesthetics and are structurally related to drugs with entirely different pharmacological activity such as droperidol, loperamide and lorcainide, etc. Therefore, in order to test their pharma
3-(1,3-dithiol-2-ylidene)-2,4-dioxopyrrolidines, -piperidines, and -hexahydroazepines and use thereof against hepatic diseases
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, (2008/06/13)
Novel thioketene derivatives of the formula: STR1 wherein R1 is hydrogen atom, an alkyl group, a lower alkenyl group, a phenyl group or a group of the formula: --B--Y; Y is a nitrogen-containing monocyclic heterocyclic group or a substituted or unsubstituted phenyl group; B is a straight or branched lower alkylene group; R2 and R3 are both a lower alkyl group or are combined together to form a group of the formula: --CH2 CH2 -- or --CH=CH--; R4 is hydrogen atom, a lower alkyl group or a (lower alkoxy)carbonyl group; A is a group of the formula: --(CH2)n -- or --CH(COOR5)--; n is an integer of 0, 1 or 2 and R5 is a lower alkyl group, are disclosed. The compound (I) is useful as an agent for treating and protecting various liver diseases.
