4773-35-7Relevant articles and documents
Alpha-amino acid derivative containing piperidine thiazole heterocycle and preparation method and application of alpha-amino acid derivative
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Paragraph 0019, (2019/02/27)
The invention discloses an alpha-amino acid derivative containing piperidine thiazole heterocycle. The alpha-amino acid derivative has a structural formula of formula I shown in the description, wherein in formula I, Ar is a phenyl group or a substituted phenyl group, a substituted group of the substituted phenyl group is one of a trifluoromethyl group, fluorine, chlorine or bromine, and R is oneof H and isopropyl. The invention further discloses a preparation method of the alpha-amino acid derivative and application of the alpha-amino acid derivative serving as an insecticide to prevention and control of armyworms. The novel alpha-amino acid derivative containing the piperidine thiazole heterocycle is simple in preparation method, can be used for prevention and control of armyworm insectpests, particularly has a good insecticidal activity against the armyworms, and provides bases for research and development of amino acid pesticides.
Peptidyl cyclopropenones: Reversible inhibitors, irreversible inhibitors, or substrates of cysteine proteases?
Cohen, Meital,Bretler, Uriel,Albeck, Amnon
, p. 788 - 799 (2013/09/02)
Peptidyl cyclopropenones were previously introduced as selective cysteine protease reversible inhibitors. In the present study we synthesized one such peptidyl cyclopropenone and investigated its interaction with papain, a prototype cysteine protease. A set of kinetics, biochemical, HPLC, MS, and 13C-NMR experiments revealed that the peptidyl cyclopropenone was an irreversible inhibitor of the enzyme, alkylating the catalytic cysteine. In parallel, this cyclopropenone also behaved as an alternative substrate of the enzyme, providing a product that was tentatively suggested to be either a spiroepoxy cyclopropanone or a gamma-lactone. Thus, a single family of compounds exhibits an unusual variety of activities, being reversible inhibitors, irreversible inhibitors and alternative substrates towards enzymes of the same family.
PIPERAZINYL DERIVATIVES USEFUL AS MODULATORS OF THE NEUROPEPTIDE Y2 RECEPTOR
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Page/Page column 138, (2009/07/18)
The present invention is directed to piperidinyl and piperazinyl derivatives of formula (II) useful as inhibitors of the NPY Y2 receptor, pharmaceutical compositions comprising said compounds, processes for the preparation of said compounds and the use of said compounds for the treatment and / or prevention of disorders, diseases and conditions mediated by the NPY Y2 receptor.