51095-47-7Relevant academic research and scientific papers
Kurasoins a and b, new protein farnesyltransferase inhibitors produced by Paecilomyces sp. FO-3684. II. Structure elucidation and total synthesis
Uchida, Ryuji,Shiomi, Kazuro,Sunazuka, Toshiaki,Inokoshi, Junji,Nishizawa,Hirose, Tomoyasu,Tanaka, Haruo,Iwai, Yuzuru,Omura, Satoshi
, p. 886 - 889 (1996)
The structures of new protein farnesyltransferase inhibitors, kurasoins A and B, were elucidated by NMR study. Kurasoins A and B are acyloin compounds having in common a 3-hydroxy-1-phenyl-2-butanone moiety, to which β-hydroxyphenyl and 3-indolyl moieties
BENZO- OR PYRIDO-IMIDAZOLE DERIVATIVE
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Paragraph 0656; 0657, (2013/04/25)
The present invention addresses the problem of finding a compound having both PPAR activation activity and angiotensin receptor antagonistic activity. The present invention is a benzo- or pyrido-imidazole derivative represented by general formula (I), a pharmaceutically acceptable salt thereof, or a ester or amide thereof (where A is biphenyl methyl-imidazolyl, biphenyl methyl-benzimidazolyl, or the like, B is divalent benzimidazolyl or the like, C is carboxyl or the like, E is divalent phenyl, naphthyl, or the like, G is a dangling bond, oxygen, or the like, Q is oxygen or sulfur, n is an integer from 1 to 6, p is an integer from 1 to 6, V is a dangling bond, oxygen, or the like, and R is hydrogen, alkyl, or the like).
THYROID RECEPTOR AGONISTS
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Page/Page column 62-63, (2010/02/14)
The invention provides compounds of formula (I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt. The invention also provides the use of such compounds in the treatment or prophylaxis of a condition mediated by a thyroid receptor. Formula (I), wherein R1, R2, n, Y, Y', R3, R4, W and R5 are as defined in the specification.
NOVEL PHARMACEUTICAL COMPOSITIONS
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Page/Page column 51, (2010/02/14)
The invention provides compounds of formula (I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt, for use in the treatment or prophylaxis of condition mediated by an androgen receptor.
Non-thiazolidinedione antihyperglycaemic agents. Part 3: The effects of stereochemistry on the potency of α-methoxy-β-phenylpropanoic acids
Haigh, David,Allen, Graham,Birrell, Helen C.,Buckle, Derek R.,Cantello, Barrie C. C.,Eggleston, Drake S.,Haltiwanger, R. Curtis,Holder, Julie C.,Lister, Carolyn A.,Pinto, Ivan L.,Rami, Harshad K.,Sime, John T.,Smith, Stephen A.,Sweeney, John D.
, p. 821 - 830 (2007/10/03)
Rhizopus delemar lipase catalysed ester hydrolysis of the α-methoxy-β-phenylpropanoate 1 affords the (R)-(+) and (S)-(-) isomers in >84% enantiomeric excess. Absolute stereochemistry was determined by a single crystal X-ray analysis of a related synthetic analogue. The activity of these two enantiomers on glucose transport in vitro and as anti-diabetic agents in vivo is reported and their unexpected equivalence attributed to an enzyme-mediated stereospecific isomerisation of the (R)-(+) isomer. Binding studies using recombinant human PPARγ (peroxisomal proliferator activated receptor γ), now established as a molecular target for this compound class, indicate a 20-fold higher binding affinity for the (S) antipode relative to the (R) antipode. Copyright (C) 1999 Elsevier Science Ltd.
Syntheses and novel bioactivities of artificial leaf-opening substances of Lespedeza cuneata G. Don, designed for the bioorganic studies of nyctinasty
Ueda, Minoru,Sawai, Yoshiyuki,Yamamura, Shosuke
, p. 10925 - 10936 (2007/10/03)
Potassium lespedezate (1) is the leaf-opening substance of a nyctinastic plant, Lespedeza cuneata G. Don. We have synthesized two sugar-derivatives of 1, potassium galactolespedezate (4) and mannolespedezate (6). Both 4 and 6 were quite effective for the leaf-opening of Cassia. mimosoides at 8 x 10-7 M, as strong as 1. However, 1 kept the leaf open only for a few days; on the other hand, 4 and 6 kept the leaf open after a week at that concentration. Additionally, remarkable difference was observed in the rate of enzymatic hydrolysis of natural and artificial leaf-opening sustance by using commercially available β-glucosidase. Therefore, 4 and 6 would not be hydrolized in the plant body, and are potentially useful molecular probes for the studies of the control of the nyctinastic leaf-movement by a biological clock.
Heterocyclic compounds as pharmaceutical
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, (2008/06/13)
Compounds of Formula (I) or a tautomeric form thereof and/or a pharmaceutically acceptable salt thereof, and/or a pharmaceutically acceptable solvate thereof, wherein A1, A2, A3, R2, X, Y and n are as define
Selectivity and Specificity in Substrate Binding to Proteases: Novel Hydrolytic Reactions Catalysed by α-Chymotrypsin Suspended in Organic Solvents with Low Water Content and Mediated by Ammonium Hydrogen Carbonate
Ricca, Jean-Marc,Crout, David H. G.
, p. 1225 - 1234 (2007/10/02)
α-Chymotrypsin suspended in organic solvents with low water content catalysed hydrolytic reactions in the presence of ammonium hydrogen carbonate.Molecular modelling studies were carried out and structure-reactivity relationships were established by studying the hydrolysis of amino acid derivatives and analogues.The enzyme was found to be stereoselective with respect to the hydrolysis of L-amino acid derivatives, but no stereoselectivity was observed when α-hydroxy esters were used as substrates.A general procedure for the resolution of aromatic amino acid esters is given.The results are interpreted in terms of molecular modelling based on X-ray crystallographic data and literature data.
