Topic
Bicyclic molecule
About: Bicyclic molecule is a research topic. Over the lifetime, 29587 publications have been published within this topic receiving 451252 citations. The topic is also known as: bicyclic molecule.
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21 Jul 1997TL;DR: In this article, the authors defined compounds of formula (I) as corticotropin releasing factor (hormone) CRF (CRH) antagonists, and the pharmaceutically acceptable salts of such compounds.
Abstract: This invention relates to compounds of formula (I), wherein A, B, D, E, K, G, R?3 and R5? are defined as in the specification, and to the pharmaceutically acceptable salts of such compounds. Compounds (I) are corticotropin releasing factor (hormone) CRF (CRH) antagonists.
79 citations
TL;DR: Bromo and chloro polyimines react with trimethylsilyacetylene in the presence of Pd(PPh3)2Cl2/CuI and diisopropylamine as discussed by the authors.
79 citations
TL;DR: The search for photoresponsive conformational transitions accompanied by changes in physicochemical and biological properties led to the design of small cyclic peptides containing azobenzene moieties in the backbone, suggesting that restricted conformational freedom was already present in the monocyclic form.
Abstract: The search for photoresponsive conformational transitions accompanied by changes in physicochemical and biological properties led us to the design of small cyclic peptides containing azobenzene moieties in the backbone. For this purpose, (4-aminomethyl)phenylazobenzoic acid (H-AMPB-OH) and (4-amino)phenylazobenzoic acid (H-APB-OH) were synthesized and used to cyclize a bis-cysteinyl-octapeptide giving monocyclic derivatives in which additional conformational restriction could be introduced by conversion to bicyclic structures with a disulphide bridge. While synthesis with H-AMPB-OH proceeded smoothly on a chlorotrityl-resin with Fmoc/tBu chemistry, the poor nucleophilicity of the arylamino group of H-APB-OH required special chemistry for satisfactory incorporation into the peptide chain. Additional difficulties were encountered in the reductive cleavage of the S-tert-butylthio group from the cysteine residues since concomitant reduction of the azobenzene moiety took place at competing rates. This difficulty was eventually bypassed by using the S-trityl protection. Side-chain cyclization of the APB-peptide proved to be difficult, suggesting that restricted conformational freedom was already present in the monocyclic form, a fact that was fully confirmed by NMR structural analysis. Conversely, the methylene spacer in the AMPB moiety introduced sufficient flexibility for facile and quantitative side-chain cyclization to the bicyclic form. Both of the monocyclic peptides and both of the bicyclic peptides are photoresponsive molecules which undergo cis/trans isomerization reversibly.
79 citations
TL;DR: N-Protection d'imidazoles substitues en 4(S), du benzimidaxole, de l'IMidazo [4,5b] pyridine and du bi-idazolyle-1,1' par action de SEMCl (chloromethyl trimethylsilyl-2 ethyl ether) sur les derives N-non substitues; deprotection par une solution acide diluee.
Abstract: N-Protection d'imidazoles substitues en 4(S), du benzimidazole, de l'imidazo [4,5-b] pyridine et du biimidazolyle-1,1' par action de SEMCl (chloromethyl trimethylsilyl-2 ethyl ether) sur les derives N-non substitues; deprotection par une solution acide diluee
79 citations