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Conformational restriction receptor antagonists

The Rh-BIPHEPHOS-catalyzed cyclohydrocarbonylation has also been successfully applied to the rapid synthesis of a variety of l-azabicyclo[X.Y.O]alkane amino acids, which serve as conformationally restricted dipeptide surrogates for enzyme inhibitors and receptor antagonists, directly from dehydrodipeptide substrates (Scheme Reaction... [Pg.517]

Watanabe, M., Kazuta, Y., Hayashi, H., Yamada, S., Matsuda, A., Shuto, D. Stereochemical diversity-oriented conformational restriction strategy. Development of potent histamine H3 and/or H4 receptor antagonists with an imidazolylcyclopropane structure. J. Med. Chem. 2006,49, 5587-5596. [Pg.378]

Ohmori, Y., Yamashita, A., Tsujita, R., Yamamoto, T, Taniuchi, K., Matsuda, A., Shuto, S. A method for designing conformationally restricted analogues based on allylic strain synthesis of a novel class of noncompetitive NMDA receptor antagonists having the acrylamide structure. J. Med. Chem. 2003, 46, 5326-5333. [Pg.378]

Musicki, B., and Vevert, J.-P., Synthesis of conformationally restricted analogues of an angiotensin II receptor antagonist. General synthetic approach to functionalized imidazo[l,5-a]pyridine derivatives, Tetrahedron Lett., 35, 9391, 1994. [Pg.489]

Ono S, Ogawa K, Yamashita K, et al. Conformational analysis of the NMDA receptor antagonist (1S,2R)-1-phenyl-2-[S-1-aminopropyl]-N,N-diethylcyclopropanecarboxamide (PPDC) designed by a novel conformational restriction method based on the structural feature of cyclopropane ring. Chem Pharm Bull (Tokyo). 2002 50 966-968. [Pg.886]

Hanna PE, Ahmed AE. Conformationally restricted analogues of histamine Hi receptor antagonists, trans- and c/s-1,5-diphenyl-3-dimethylaminopyrrolidine. J Med Chem 1973 16 963-968. [Pg.1554]


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Conformation conformational restriction

Conformation conformationally restricted

Conformational restriction

Receptor conformations

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