220875-99-0Relevant academic research and scientific papers
Allylamine derivative as well as preparation method and application thereof
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, (2021/06/02)
The invention relates to an allylamine derivative as well as a preparation method and application thereof, and in particular, relates to a compound represented by a formula I, or a stereoisomer, a tautomer, a polymorphic substance, a solvate, an N-oxide, an isotope labeled compound, a metabolite, a prodrug or ester thereof, or a pharmaceutically acceptable salt thereof. The compound has a higher inhibitory activity against vascular adhesion protein 1/semicarbazide sensitive amine oxidase, a good selectivity against monoamine oxidase and diamine oxidase; and additionally, in some embodiments, the mixture has a high in vivo bioavailability as well as safety.
N-Cycloalkanoyl-L-phenylalanine derivatives as VCAM/VLA-4 antagonists.
Sidduri, Achyutharao,Tilley, Jefferson W,Hull, Kenneth,Lou, Jian Ping,Kaplan, Gerry,Sheffron, Allen,Chen,Campbell, Robert,Guthrie, Robert,Huang, Tai-Nan,Huby, Nicholas,Rowan, Karen,Schwinge, Virginia,Renzetti, Louis M
, p. 2475 - 2478 (2007/10/03)
A systematic structure-activity relationship investigation of the lead compound 1 resulted the identification of several N-[(substituted alkyl)cycloalkanoyl]-4-[((2,6-dichlorophenyl)carbonyl)amino]-L-phenylalanine derivatives as potent VCAM/VLA-4 antagonists. The data are consistent with a model of these compounds in which these alkanoylphenylalanines reside in a compact gauche (-) bioactive conformation.
