29776-78-1Relevant academic research and scientific papers
Investigation of the active turn geometry for the labour delaying activity of indolizidinone and azapeptide modulators of the prostaglandin F2α receptor
Boukanoun, Meriem K.,Hou, Xin,Nikolajev, Ljiljana,Ratni, Sara,Olson, David,Claing, Audrey,Laporte, Stéphane A.,Chemtob, Sylvain,Lubell, William D.
, p. 7750 - 7761 (2015)
On pursuing molecules that delay labour, so-called tocolytics, the prostaglandin F2α receptor (FP) was targeted, because of its role in the stimulation of uterine contractions leading to birth and preterm birth. Previously, both the indolizidin
The Study of Stability of Proline-Containing Derivatives of Dopamine and Serotonin in the Biological Media in Vitro Experiments
Andreeva, L. A.,Myasoedov, N. F.,Nagaev, I. Yu.,Shevchenko, K. V.,Shevchenko, V. P.
, p. 150 - 158 (2020/05/28)
Abstract—: The peptides Boc-Gly-Pro-DP, Z-Gly-Pro-DP, LA-Gly-Pro-DP, Boc-Gly-Pro-Srt, Z-Gly-Pro-Srt have been synthesized for the first time. The study of their stability in the presence of leucine aminopeptidase, carboxypeptidase Y, carboxypeptidase B, and proline endopeptidase (PEP) has shown that the synthesized peptides are stable in the presence of aminopeptidases and carboxypeptidases. In the presence of PEP, dopamine (DP) and serotonin (Srt) have been cleaved from these substances. Thus, the originally synthesized proline derivatives of Srt and DP may be considered as the resources, from which Srt and DP can be gradually released. This creates the possibility of a prolonged action of these biologically active compounds on cells and, consequently, on the whole body.
5,5-FUSED ARYLENE OR HETEROARYLENE HEPATITIS C VIRUS INHIBITORS
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Paragraph 0234; 0235; 0236; 0282; 0284, (2018/08/20)
Provided herein are 5,5-fused heteroarylene hepatitis C virus inhibitor compounds, for example, of Formula I, IA, or IB, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.
Structural-functional study of glycine-and-proline-containing peptides (Glyprolines) as potential neuroprotectors
Martynova,Andreeva,Klimova,Kirillova, Yu. G.,Shevchenko,Nagaev, I. Yu.,Shram,Shvets,Myasoedov
experimental part, p. 150 - 156 (2010/04/29)
A synthetic scheme for preparation of (Gly-Pro) n, (Pro-Gly) n (n = 2, 3), and (Pro-Gly-Pro) n (n = 1, 2) peptides was elaborated. The effect of the synthesized peptides and the Gly-Pro and Pro-Gly dipeptides on survival of cultured cells of PC12 rat pheochromocytoma was studied under the conditions of oxidative stress induced by brief incubation of the cells with hydrogen peroxide. Peptides of the general formula (Gly-Pro) n and the Pro-Gly-Pro peptide at a concentration of 0.2-100 μM were shown to decrease the number of damaged cells. The Gly-Pro peptide was the most active and decreased the number of damaged cells by 49% on average at a concentration of 100 μM.
Molecular design and structure - Activity relationships leading to the potent, selective, and orally active thrombin active site inhibitor BMS-189664
Das, Jagabandhu,Kimball,Hall, Steven E.,Han, Wen-Ching,Iwanowicz, Edwin,Lin, James,Moquin, Robert V.,Reid, Joyce A.,Sack, John S.,Malley, Mary F.,Chang, Chiehying Y.,Chong, Saeho,Wang-Iverson, David B.,Roberts, Daniel G.M.,Seiler, Steven M.,Schumacher, William A.,Ogletree, Martin L.
, p. 45 - 49 (2007/10/03)
A series of structurally novel small molecule inhibitors of human α-thrombin was prepared to elucidate their structure-activity relationships (SARs), selectivity and activity in vivo. BMS-189664 (3) is identified as a potent, selective, and orally active reversible inhibitor of human α-thrombin which is efficacious in vivo in a mouse lethality model, and at inhibiting both arterial and venous thrombosis in cynomolgus monkey models.
Design of a gag pentapeptide analogue that binds human cyclophilin a more efficiently than the entire capsid protein: New insights for the development of novel anti-HIV-1 drugs
Li, Quan,Moutiez, Mireille,Charbonnier, Jean-Baptiste,Vaudry, Karine,Ménez, André,Quéméneur, Eric,Dugave, Christophe
, p. 1770 - 1779 (2007/10/03)
Cyclophilin A (hCyp-18), a ubiquitous cytoplasmic peptidyl-prolyl cis/trans isomerase (PPIase), orchestrates HIV-1 core packaging, hCyp-18, incorporated into the virion, enables core uncoating and RNA release and consequently plays a critical role in the
Conformational studies of cyclo(L-Phe-L-Pro-Gly-L-Pro)2 by 1H- and 13C-nuclear magnetic resonance spectroscopy, and its enantioface-differentiating ability
Ishizu,Fujii,Noguchi
, p. 235 - 238 (2007/10/02)
Analyses of the 1H- and 13C-nuclear magnetic resonance (1H- and 13C-NMR) spectra of the cyclooctapeptide cyclo (L-Phe-L-Pro-Gly-L-Pro)2 (3) in CDCl3 with the aid of the C-H correlated spectroscopy (C-H COSY) two-dimensional NMR spectrum (Fig. 2) suggested that two kinds of C2-symmetric conformation with all trans and cis-trans-trans-trans forms coexist. When 0.5 eq of CsSCN or 1 eq of D- and L-PheOMe · HCl (D/L ratio = 1/2) was added to a solution of the cyclooctapeptide (3) in CDCl3, the 1H- and 13C-NMR spectra (Fig. 3) suggested the presence of only one C2-symmetric conformation (all trans), resulting from the formation of complexes with CsSCN or D- and L-PheOMe · HCl. The 13C-NMR spectra of the complexes of the cyclooctapeptide (3 or 4) with D- and L-PheOMe · HCl displayed separate resonances for each carbon atom of D-PheOMe · HCl and L-PheOMe · HCl. Furthermore, the ability of 3 to distinguish the D from the L enantiomer, is superior to that of 4 (Table II).
Amino acid derivatives, methods of preparing said derivatives and antihypertensive drugs containing them
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, (2008/06/13)
The present invention relates to an amino acid derivative represented by the formula STR1 wherein R1 and R2 represent hydroxyl, alkyloxy, aryloxy, arylkyloxy, alkyl, aryl, or aralkyl; R3, R5, R8 and R
