447461-03-2Relevant articles and documents
Synthesis of the southern tripeptide (C1-N12) of sanglifehrins using asymmetric organocatalysis
Radhika, Laghuvarapu,Chandrasekhar, Srivari
, p. 3602 - 3609 (2015/08/11)
The tripeptide southern region of the novel cyclophilin binding natural product macrolides, namely sanglifehrins, is synthesized involving asymmetric organocatalysis as chirality-inducing step. List's asymmetric α-amination was used in the synthesis of th
Macrocyclic BACE-1 inhibitors acutely reduce Aβ in brain after po application
Lerchner, Andreas,Machauer, Rainer,Betschart, Claudia,Veenstra, Siem,Rueeger, Heinrich,McCarthy, Clive,Tintelnot-Blomley, Marina,Jaton, Anne-Lise,Rabe, Sabine,Desrayaud, Sandrine,Enz, Albert,Staufenbiel, Matthias,Paganetti, Paolo,Rondeau, Jean-Michel,Neumann, Ulf
scheme or table, p. 603 - 607 (2010/06/19)
A series of macrocyclic peptidic BACE-1 inhibitors was designed. While potency on BACE-1 was rather high, the first set of compounds showed poor brain permeation and high efflux in the MDRI-MDCK assay. The replacement of the secondary benzylamino group wi
Macrocyclic Compounds Useful as Bace Inhibitors
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Page/Page column 44-45, (2008/12/05)
The invention relates to novel macrocyclic compounds of the formula (I), in which all of the variables are as defined in the specification, the number of ring atoms included in the macrocyclic ring being 14, 15, 16 or 17, in free base form or in acid addition salt form, to their preparation, to their use as medicaments and to medicaments comprising them.
Thiol-based angiotensin-converting enzyme 2 inhibitors: P1′ modifications for the exploration of the S1′ subsite
Deaton, David N.,Graham, Kevin P.,Gross, Jeffrey W.,Miller, Aaron B.
, p. 1681 - 1687 (2008/12/22)
Explorations of the S1′ subsite of ACE2 via modifications of the P1′ methylene biphenyl moiety of thiol-based metalloprotease inhibitors led to improvements in ACE2 selectivity versus ACE and NEP, while maintaining potent ACE2 inhibi
MACROCYCLIC COMPOUNDS USEFUL AS BACE INHIBITORS
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Page/Page column 87, (2008/06/13)
The invention relates to novel macrocyclic compounds of the formula (I), in which all of the variables are as defined in the specification, in free base form or in acid addition salt form, to their preparation, to their use as medicaments and to medicaments comprising them.
MACROCYCLIC COMPOUNDS AND COMPOSITIONS USEFUL AS BACE INHIBITORS
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Page/Page column 23-24, (2008/06/13)
The invention relates to novel macrocyclic compounds of the formula in which R1, R3, V1, V2, X1, X2, Y, Z, Ar, AA and n are as defined in the specification, the number of ring atoms include
Practical, asymmetric synthesis of aromatic-substituted bulky and hydrophobic tryptophan and phenylalanine derivatives
Wang, Wei,Xiong, Chiyi,Zhang, Junyi,Hruby, Victor J
, p. 3101 - 3110 (2007/10/03)
Aromatic ring substituted tryptophans and phenylalanines can provide valuable tools in developing highly potent and selective peptide ligands with specific structural features in addition to providing a large lipophilic surface for binding to receptors and for crossing membrane barriers. An efficient method for the synthesis of these novel amino acids has been developed. In the approach, asymmetric hydrogenations of α-enamides using Burk's DuPHOS-based Rh (I) catalysts generated high enantiomerically pure α-amino acid derivatives, which subsequently underwent Suzuki cross couplings with boronic acid derivatives to afford these aromatic substituted amino acids in high yields and high enantioselectivity. The method can allow for the preparation of such amino acids in large scales for extensive structure-activity studies.
