10009-70-8Relevant articles and documents
Synthesis and RGD peptide modification of a new biodegradable copolymer: Poly(lactic acid-co-lysine)
Barrera, Denise A.,Zylstra, Eric,Lansbury Jr., Peter T.,Langer, Robert
, p. 11010 - 11011 (1993)
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Design and synthesis of potent thiol-based inhibitors of endothelin converting enzyme-1
Fink, Cynthia A.,Moskal, Michael,Firooznia, Fariborz,Hoyer, Denton,Symonsbergen, David,Wei, Dongchu,Qiao, Ying,Savage, Paula,Beil, Michael E.,Trapani, Angelo J.,Jeng, Arco Y.
, p. 2037 - 2039 (2000)
Through directed screening of compounds prepared as metalloprotease inhibitors a compound, CGS 30084, that had potent endothelin converting enzyme-1 (ECE-1) in vitro inhibitory activity (IC50=77nM) was identified. Herein we report the synthesis and optimization of ECE-1 inhibitory activity of additional analogues from this lead. Compound 3c, the thioacetate methyl ester derivative of compound 4c, was found to be a long acting inhibitor of ECE-1 activity in rats after oral administration. (C) 2000 Elsevier Science Ltd.
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Farinacci
, p. 1799,1801 (1941)
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Synthesis and screening of stereochemically diverse combinatorial libraries of peptide tertiary amides
Gao, Yu,Kodadek, Thomas
, p. 360 - 369 (2013)
Large combinatorial libraries of N-substituted peptides would be an attractive source of protein ligands, because these compounds are known to be conformationally constrained, whereas standard peptides or peptoids are conformationally mobile. Here, we report an efficient submonomer solid-phase synthetic route to these compounds and demonstrate that it can be used to create high quality libraries. A model screening experiment and analysis of the hits indicates that the rigidity afforded by the stereocenters is critical for high affinity binding.
PHARMACEUTICAL COMPOSITION CONTAINING TRICYCLIC COMPOUND HAVING SULFINYL OR SULFONYL
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Paragraph 0299, (2018/08/02)
PROBLEM TO BE SOLVED: To provide a pharmaceutical composition that has antibacterial activity against carbapenem-resistant bacteria. SOLUTION: A pharmaceutical composition contains a compound represented by formula (I), its ester body or their pharmaceutically acceptable salts, or their hydrates (W is S(=O) or S(=O)2; T is CR4AR4B or CR5AR5B-CR6AR6B; R4A, R4B, R5A, R5B, R6A and R6B independently represent halogen, hydroxy, carbonyl, alkyl, cycloalkyl, aryl or the like; R1 is a carbocycle or heterocycle; R2A and R2B independently represent H, amino, hydroxy and the like, or R2A and R2B together form methylidene, hydroxyimino and the like; R3 is H, methoxy or the like). SELECTED DRAWING: None COPYRIGHT: (C)2018,JPOandINPIT
Enantioselective protonation of α-hetero carboxylic acid-derived ketene disilyl acetals under chiral ionic Bronsted acid catalysis
Uraguchi, Daisuke,Kizu, Tomohito,Ohira, Yuki,Ooi, Takashi
supporting information, p. 13489 - 13491 (2015/01/09)
Highly enantioselective protonation of α-halo and alkoxy carboxylic acid-derived ketene disilyl acetals is achieved by using P-spiro chiral diaminodioxaphosphonium barfate as a Bronsted acid catalyst, where the enantiofacial discrimination by the catalyst mainly stems from the recognition of the electronic difference between two substituents on the ketene disilyl acetal.