139397-08-3Relevant academic research and scientific papers
Synthesis and biological evaluations of novel endomorphin analogues containing α-hydroxy-β-phenylalanine (AHPBA) displaying mixed μ/δ opioid receptor agonist and δ opioid receptor antagonist activities
Hu, Miao,Giulianotti, Marc A.,McLaughlin, Jay P.,Shao, Jiaan,Debevec, Ginamarie,Maida, Laura E.,Geer, Phaedra,Cazares, Margaret,Misler, Jaime,Li, Ling,Dooley, Colette,Ganno, Michelle L.,Eans, Shainnel O.,Mizrachi, Elisa,Santos, Radleigh G.,Yongye, Austin B.,Houghten, Richard A.,Yu, Yongping
, p. 270 - 281 (2015)
A novel series of endomorphin-1 (EM-1) and endomorphin-2 (EM-2) analogues was synthesized, incorporating chiral α-hydroxy-β-phenylalanine (AHPBA), and/or Dmt1-Tic2 at different positions. Pharmacological activity and metabolic stabil
Novel multifunctional peptidase inhibitors, especially for medical use
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, (2011/04/18)
The invention relates to compounds of the general formula (1) or the acid addition salts thereof with organic and/or inorganic acids; as well as to the use of the compounds of the general formula (1) in medicine.
NOVEL MULTIFUNCTIONAL PEPTIDASE INHIBITORS, ESPECIALLY FOR MEDICAL USE
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, (2011/04/14)
The invention relates to compounds of the general formula (1) or the acid addition salts thereof with organic and/or inorganic acids; as well as to the use of the compounds of the general formula (1) in medicine.
Enantiospecific formation of 3,6-dihydro-1H-pyridin-2-ones: Low-pressure palladium-catalysed decarboxylative carbonylation of 3-tosyl-5-vinyloxazolidin- 2-ones
Knight, Julian G.,Lawson, Iain M.,Johnson, Christopher N.
, p. 227 - 230 (2007/10/03)
Palladium-catalysed decarboxylative carbonylation of 3-tosyl-5- vinyloxazolidin-2-ones 5 occurs at atmospheric pressure to give 1-tosyl-3,6-dihydro-1H-pyridin-2-ones 6. The reaction proceeds with no loss of enantiopurity and detosylation with sodium napht
Allosteric regulation of the conformational dynamics of a cavitand receptor
Yan, Zhiqing,Chang, Yuning,Mayo, Dennis,Maslak, Veselin,Xia, Shijing,Badjic, Jovica D.
, p. 3697 - 3700 (2007/10/03)
Inspired by allostery in nature, we synthesized cavitand 1 and investigated regulation of its conformational dynamics. Quantitative 1H NMR studies have revealed that the rate of the conformational isomerization of 1 can be modulated using the e
A stereocontrolled synthesis of hapalosin
Oshitari, Tetsuta,Saiyinbilige,Mandai, Tadakatsu
, p. 185 - 190 (2007/10/03)
A facile synthetic method for two components of hapalosin, that is, β-hydroxy-γ-amino acid and β-hydroxy acid, has been established by utilizing chiral building blocks efficiently resolved in a lipase-catalyzed transesterification. Furthermore, the synthe
Regiospecific ring-opening reactions of β-aziridinyl ct, β-enoates with acids: Application to the stereoselective synthesis of a couple of diastereoisomeric (Zi)-alkene dipeptide isosteres from a single β-aziridinyl a, β-enoate and to the convenient preparation of amino alcohols bearing a, β-unsaturated ester groups
Tamamura, Hirokazu,Yamashita, Masaki,Nakajima, Yutaka,Sakano, Kyoko,Otaka, Akira,Ohno, Hiroaki,Ibuka, Toshiro,Fujii, Nobutaka
, p. 2983 - 2996 (2007/10/03)
Regio- and stereo-selective ring-opening reactions of N-(2, 4, 6-trimethylphenylsulfonyl)-γ, δ-cis- or trans-γ, δ-epimino (E)-α, β-enoates with acids such as methanesulfonic acid (MSA) or trifluoroacetic acid (TFA) have been found. These ring-opening reactions are useful for the stereoselective synthesis of a couple of diastereomeric (£)-alkene dipeptide isosteres from a single substrate of γ, δ-epimino (E)-α, β-enoate, and for the convenient preparation of δ-aminated γ-hydroxy α, β-enoates. The Royal Society of Chemistry 1999.
Inactivation of serine protease, α-chymotrypsin by fluorinated phenylalanine analogues
Ohba, Tsuyoshi,Ikeda, Eitatsu,Takei, Hisashi
, p. 1875 - 1880 (2007/10/03)
Fluorinated phenylalanine analogues were found to be slow-binding or reversible competitive inhibitors of α-chymotrypsin. A series of these compounds were designed to inactivate α-chymotrypsin as a result of the formation of hydrogen-bonding between fluorine atom of the inhibitors and the amide protons known as oxy-anion hole in the active-site of serine and cysteine proteases.
Tuftsin derivatives
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, (2008/06/13)
Linear or cyclic tetra peptide derivatives of tuftsin which activate immunocompetent cells, i.e., macrophages and polymorphonuclear leukocyte, provide a host-mediated inhibition of the growth of tumors, provide protective effects for infectious diseases s
