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Synthesis and Evaluation of Some Hydroxyproline-Derived Peptidomimetics as Isoprenyltransferase Inhibitors.
作者:Celeste E. O'CONNELL、Ceryl A. ROWELL、Karen ACKERMANN、Ana Maria GARCIA、Michael D. LEWIS、James J. KOWALCZYK
DOI:10.1248/cpb.48.740
日期:——
CA1A2X peptidomimetics containing a modified proline at position A2 were prepared and evaluated for their ability to inhibit farnesyltransferase (FTase) and geranylgeranyltransferase I (GGTase I) in enzymatic and cellbased assays. These compounds inhibited farnesylation of H-ras in vitro in the high nanomolar to low micromolar IC50 range.
含有位置A2处修饰脯氨酸的CA1A2X肽模拟物被制备并评估了它们抑制法尼基转移酶(FTase)和香叶香叶基转移酶I(GGTase I)的能力,通过酶学和细胞基础检测。这些化合物在体外抑制H-ras的法尼基化,IC50值在高达数百纳摩尔至低微摩尔范围内。
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[EN] DISUBTITUTED AZETIDINES, PYRROLIDINES, PIPERIDINES AND AZEPANES AS INHIBITORS OF MONOAMINE OXIDASE B FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES<br/>[FR] AZÉTIDINES, PYRROLIDINES, PIPÉRIDINES ET AZÉPANES DI-SUBSTITUÉS EN TANT QU'INHIBITEURS DE MONOAMINE OXYDASE B POUR LE TRAITEMENT DE MALADIES NEURODÉGÉNÉRATIVES
申请人:UNIV OF LJUBLJANA
公开号:WO2018055096A1
公开(公告)日:2018-03-29
This invention relates to new inhibitors of MAO-Bwith the general formula I, where substituents are described in patent description. Compounds can be in the form of pure enantiomers or as racemic mixtures, or in the form of pharmaceutically acceptable salts. The present invention relates to the use of these inhibitors for the alleviation of symptoms and treatment of acute and chronic neurological disorders, cognitive and neurodegenerative diseases.
这项发明涉及具有一般式I的新MAO-B抑制剂,其中取代基在专利描述中有描述。化合物可以是纯对映体的形式,也可以是消旋混合物的形式,或者是药用盐的形式。本发明涉及利用这些抑制剂缓解症状和治疗急性和慢性神经疾病、认知和神经退行性疾病。
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Bandmann, Heinz; Bartik, Tamas; Bauckloh, Sylvia, Zeitschrift fur Chemie, 1990, vol. 30, # 6, p. 193 - 204
作者:Bandmann, Heinz、Bartik, Tamas、Bauckloh, Sylvia、Behler, Ansgar、Brille, Frank、et al.
DOI:——
日期:——
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Bindra,A.P. et al., Australian Journal of Chemistry, 1971, vol. 24, p. 1721 - 1726
作者:Bindra,A.P. et al.
DOI:——
日期:——
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Vig, O. P.; Vig, R.; Dua, D. M., Indian Journal of Chemistry - Section B Organic and Medicinal Chemistry, 1984, vol. 23, # 3, p. 274 - 275
作者:Vig, O. P.、Vig, R.、Dua, D. M.、Rani, Veena
DOI:——
日期:——