53878-12-9Relevant academic research and scientific papers
Ultrasound assisted synthesis of coumarin thioglycopyranoside derivatives
Yu, Lei,Gao, Jian-Fang,Cao, Ling-Hua
, p. 1175 - 1179 (2009)
Themethyl coumarins reacted with N-bromo-succinimide gave compounds (a~c) which on further reacted with various peracetyl sulfhydryl glycose (1~3) afforded a series of novel coumarin thioglycopyranoside compounds (1a~1c, 2a~2c, 3a~3c). And when used ultra
Synthesis of new heterocyclic and polycyclic aromatic retinals and their bacteriorhodopsin analogues
Ivanova, Diana,Kolev, Vilen,Lazarova, Tzvetana,Padros, Esteve
, p. 2645 - 2648 (1999)
New heterocyclic and polycyclic aromatic retinal analogues (Fig. 1) were synthesised and their recombination with bacterioopsin was studied.
3-(2-Aminocarbonylphenyl)propanoic acid analogs as potent and selective EP3 receptor antagonists. Part 2: Optimization of the side chains to improve in vitro and in vivo potencies
Asada, Masaki,Iwahashi, Maki,Obitsu, Tetsuo,Kinoshita, Atsushi,Nakai, Yoshihiko,Onoda, Takahiro,Nagase, Toshihiko,Tanaka, Motoyuki,Yamaura, Yoshiyuki,Takizawa, Hiroya,Yoshikawa, Ken,Sato, Kazutoyo,Narita, Masami,Ohuchida, Shuichi,Nakai, Hisao,Toda, Masaaki
experimental part, p. 1641 - 1658 (2010/04/29)
A series of 3-[2-{[(3-methyl-1-phenylbutyl)amino]carbonyl}-4-(phenoxymethyl)phenyl]propanoic acid analogs were synthesized and evaluated for their in vitro potency. In most cases, introduction of one or two substituents into the two phenyl moieties resulted in the tendency of an increase or retention of in vitro activities. Several compounds, which showed excellent subtype selectivity, were evaluated for their inhibitory effect against PGE2-induced uterine contraction in pregnant rats, which is thought to be mediated by the EP3 receptor subtype. The structure-activity relationships (SARs) are also discussed.
Discovery of novel N-acylsulfonamide analogs as potent and selective EP3 receptor antagonists
Asada, Masaki,Obitsu, Tetsuo,Kinoshita, Atsushi,Nakai, Yoshihiko,Nagase, Toshihiko,Sugimoto, Isamu,Tanaka, Motoyuki,Takizawa, Hiroya,Yoshikawa, Ken,Sato, Kazutoyo,Narita, Masami,Ohuchida, Shuichi,Nakai, Hisao,Toda, Masaaki
scheme or table, p. 2639 - 2643 (2010/07/05)
A series of novel N-acylsulfonamide analogs were synthesized and evaluated for their binding affinity and antagonist activity for the EP3 receptor subtype. Representative compounds were also evaluated for their inhibitory effect on PGE2-induced
CARBOXAMIDE COMPOUNDS AND THEIR USE AS ANTAGONISTS OF THE CHEMOKINE CCR2 RECEPTOR
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Page/Page column 65, (2009/07/17)
Chemokine receptor antagonists, in particular, compounds of Formula (I) that act as antagonists of the chemokine CCR2 receptor, including pharmaceutical compositions and uses thereof to treat or prevent diseases associated with monocyte accumulation, lymphocyte accumulation or leukocyte accumulation are described; wherein (B/A) is an optionally substituted fused aromatic or partially aromatic bicyclic ring containing at least one nitrogen atom.
THERAPEUTIC AGENT FOR PSYCHONEUROTIC DISEASE
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Page/Page column 25, (2008/06/13)
The present invention relates to a preventive and/or therapeutic agent for psychoneurotic diseases, comprising an EP3 antagonist represented by the general formula (I): (wherein the meanings of characters are defined in the description). This compound has an antagonistic potency against EP3 and exhibits efficacy through unusual action mechanism as a preventive and/or therapeutic agent for psychoneurotic disorder, psychosomatic disorder, anxiety disorder, depression and disorder caused by stress.
CARBOXYLIC ACID COMPOUNDS
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Page/Page column 20, (2008/06/13)
The present invention relates to a carboxylic acid compound of formula (I): wherein R1 is H, alkyl; m is 2, 3; n is 0-2; R2 is phenyl, naphthyl, benzofuran, benzothiophene; Q is -CH2-O-Cycl, -CH2-Cyc2, -L-Cyc3; R3a and R3b each independently is hydrogen, alkyl or taken together form tetrahydro-2H-pyran; a pharmaceutically acceptable salt thereof, a method for producing a process of the preparation thereof and a pharmaceutical agent comprising the same as an active ingredient. The compound of formula (I) have an antagonizing activity against PGE2 receptor, specifically EP3 receptor which is subtype thereof, and are useful for the prevention and/or treatment of itching, pain, urinary disturbance or stress disease.
Antagonists of melanin concentrating hormone effects on the melanin concentrating hormone receptor
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Page/Page column 44, (2010/02/14)
The present invention is directed to compounds of formula (I), which antagonize of the effects of melanin-concentrating hormone (MCH) through the melanin concentrating hormone receptor which is useful for the prevention or treatment of eating disorders, weight gain, obesity, abnormalities in reproduction and sexual behavior, thyroid hormone secretion, diuresis and water/electrolyte homeostasis, sensory processing, memory, sleeping, arousal, anxiety, depression, seizures, neurodegeneration and psychiatric disorders.
Design, synthesis, and 3D QSAR of novel potent and selective aromatase inhibitors
Leonetti, Francesco,Favia, Angelo,Rao, Angela,Aliano, Rosaria,Paluszcak, Anja,Hartmann, Rolf W.,Carotti, Angelo
, p. 6792 - 6803 (2007/10/03)
The design, synthesis, and biological evaluation of a series of new aromatase inhibitors bearing an imidazole or triazole ring linked to a fluorene (A), indenodiazine (B), or coumarin scaffold (C) are reported. Properly substituted coumarin derivatives di
Non-nucleosidic coumarin derivatives as polynucleotide-crosslinking agents
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Page column 18, (2010/02/08)
Novel coumarin derivatives comprising a coumarin moiety linked to a non-nucleosidic backbone moiety are disclosed. The resulting molecules are typically used as photoactivate crosslinking groups when incorporated into polynucleotides as replacements for o
