Synthesis and analgesic effects of N-[3-[(hydroxyamino) carbonyl]-1-oxo-2 (R)-benzylpropyl]-L-isoleucyl-L-leucine, a new potent inhibitor of multiple neurotensin/ …

…, M Rodriguez, F Vecchini, H Fulcrand…

文献索引：Doulut, Sylvie; Dubuc, Isabelle; Rodriguez, M.; Vecchini, F.; Fulcrand, H.; et al. Journal of Medicinal Chemistry, 1993 , vol. 36, # 10 p. 1369 - 1379

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被引用次数: 30

摘要

The synthesis of N-[3-[(hydroxyamino) carbonyll-1-oxo-2 (R)-benzylpropyll-L-isoleucyl-L- leucine (JMV-390-1, 6a), a multipeptidase inhibitor based on the C-terminal sequence common to neurotensin (NT) and neuromedin N (NN), is described. This compound behaves as a full inhibitor of the major NT/NN degrading enzymes in vitro, eg endopeptidase 24.16, endopeptidase 24.15, endopeptidase 24.11, and leucine ...