51631-50-6Relevant academic research and scientific papers
Synthesis and characterization of chrysanthemic acid esters
Ding, Qingwei,Li, Yonghong,Zhang, Mingang
experimental part, p. 2881 - 2883 (2012/08/29)
A short and convenient synthesis for a series of novel chrysanthemic acid esters from aldehyde and chrysanthemic acid is reported.
A mild and general one-pot preparation of cyanoethyl-protected tetrazoles
Kennedy, Lawrence J.
experimental part, p. 2010 - 2013 (2010/06/14)
Described herein is a mild and general one-pot procedure for the conversion of cyanoethyl amides to cyanoethyl-protected tetrazoles with azidotrimethylsilane via the intermediacy of imidoyl chlorides generated in situ with phosphorus pentachloride. This s
Discovery of 2-[1-(4-Chlorophenyl)cyclopropyl]-3-hydroxy-8- (trifluoromethyl)quinoline-4-carboxylic acid (PSI-421), a P-selectin inhibitor with improved pharmacokinetic properties and oral efficacy in models of vascular injury
Huang, Adrian,Moretto, Alessandro,Janz, Kristin,Lowe, Michael,Bedard, Patricia W.,Tam, Steve,Di, Li,Clerin, Valerie,Sushkova, Natalia,Tchernychev, Boris,Tsao, Desiree H. H.,Keith Jr., James C.,Shaw, Gray D.,Schaub, Robert G.,Wang, Qin,Kaila, Neelu
supporting information; experimental part, p. 6003 - 6017 (2010/11/19)
Previously, we reported the discovery of PSI-697 (1a), a C-2 benzyl substituted quinoline salicylic acid-based P-selectin inhibitor. It is active in a variety of animal models of cardiovascular disease. Compound 1a has also been shown to be well tolerated and safe in healthy volunteers at doses of up to 1200 mg in a phase 1 single ascending dose study. However, its oral bioavailability was low. Our goal was to identify a back up compound with equal potency, increased solubility, and increased exposure. We expanded our structure-activity studies in this series by branching at the α position of the C-2 benzyl side chain and through modification of substituents on the carboxylic A-ring of the quinoline. This resulted in discovery of PSI-421 with marked improvement in aqueous solubility and pharmacokinetic properties. This compound has shown oral efficacy in animal models of arterial and venous injury and was selected as a preclinical development compound for potential treatment of such diseases as atherosclerosis and deep vein thrombosis.
Synthesis and evaluation of a new series of substituted acyl(thio)urea and thiadiazolo [2,3-a] pyrimidine derivatives as potent inhibitors of influenza virus neuraminidase
Sun, Chuanwen,Zhang, Xiaodong,Huang, Hai,Zhou, Pei
, p. 8574 - 8581 (2008/02/07)
A series of substituted acyl(thio)urea and 2H-1,2,4-thiadiazolo [2,3-a] pyrimidine derivatives were prepared and both of their cell culture and enzymatic activity toward influenza virus were tested. Their in vitro neuraminidase inhibitory activities were in good agreement with the corresponding activities in cultured cells and they were evaluated as potent neuraminidase inhibitors. Of the analogues that demonstrated IC50s 0.1 μM, 16 and 60 were further investigated as candidates with the most potential for future development. The molecular docking work of the representative compound was described to provide more insight into their mechanism of action and further rationalize the observations of this new series herein, which represents a novel class of highly potent and selective inhibitors of influenza virus.
Process for producing an optically active α-isopropyl-p-chlorophenylacetic acid
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, (2008/06/13)
A process for producing an optically active α-isopropyl-p-chlorophenylacetic acid (ICPA) of the formula: STR1 wherein the symbol * stands for an asymmetric carbon atom.
Oxadiazoline-1,3,4 one-5s
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, (2008/06/13)
Novel 1,3,4-oxadiazoline-5-one derivatives, their preparation and the insecticidal compositions in which they are present are disclosed. The novel 1,3,4-oxadiazoline-5-one derivatives correspond to the formula: STR1 in which: X represents a halogen atom,
