53985-53-8Relevant academic research and scientific papers
Discovery of 5-substituent-N-arylbenzamide derivatives as potent, selective and orally bioavailable LRRK2 inhibitors
Ding, Xiao,Dai, Xuedong,Long, Kai,Peng, Cheng,Andreotti, Daniele,Bamborough, Paul,Eatherton, Andrew J.,Edge, Colin,Jandu, Karamjit S.,Nichols, Paula L.,Philps, Oliver J.,Stasi, Luigi Piero,Wan, Zehong,Xiang, Jia-Ning,Dong, Kelly,Dossang, Pamela,Ho, Ming-Hsun,Li, Yi,Mensah, Lucy,Guan, Xiaoming,Reith, Alastair D.,Ren, Feng
, p. 4034 - 4038 (2017/08/23)
Leucine-rich repeat kinase 2 (LRRK2) has been suggested as a potential therapeutic target for Parkinson's disease. Herein we report the discovery of 5-substituent-N-arylbenzamide derivatives as novel LRRK2 inhibitors. Extensive SAR study led to the discovery of compounds 8e, which demonstrated potent LRRK2 inhibition activity, high selectivity across the kinome, good brain exposure, and high oral bioavailability.
NOVEL COMPOUNDS
-
, (2011/04/25)
The present invention discloses novel compounds inhibiting LRRK2 kinase activity, the preparation processes thereof, the compositions containing them, as well as the use in treating diseases characterized by LRRK2 kinase activity, particularly Parkinson's disease and Alzheimer's disease.
N-H Insertion reactions of rhodium carbenoids. Part 5: A convenient route to 1,3-azoles
Davies, James R.,Kane, Peter D.,Moody, Christopher J.
, p. 3967 - 3977 (2007/10/03)
Dirhodium(II) carboxylate catalysed reaction of diazocarbonyl compounds 2 in the presence of primary amides 1 results in the formation of α-acylaminoketones 3 (12 examples) by N-H insertion reaction of the intermediate rhodium carbene. The 1,4-dicarbonyl
Total synthesis of amamistatin A, an antiproliferative linear peptide from an actinomycete
Yokokawa, Fumiaki,Izumi, Kentaro,Omata, Junko,Shioiri, Takayuki
, p. 3027 - 3034 (2007/10/03)
Amamistatin A, a linear lipopeptide and a growth inhibitor of human tumor cell lines from an actinomycete, was efficiently synthesized by a convergent approach. The asymmetric synthesis of β-hydroxy acid fragment was achieved by using chiral oxazaborolidinone mediated aldol reaction. The oxazole ring was constructed from N-acylthreonine via side-chain oxidation and cyclodehydration. The synthesis of the linear peptide was carded out in a stepwise manner from the cyclic hydroxamic acid fragment, and the final deprotection provided amamistatin A. (C) 2000 Elsevier Science Ltd.
Substituted benzoic acid hypolipemic agents
-
, (2008/06/13)
Polysubstituted benzoic acids, and their use in mammals as hypolipemic agents.
