100757-90-2Relevant articles and documents
Aminophenone compounds as well as preparation method and application thereof
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Paragraph 0047-0050, (2021/02/06)
The invention belongs to the technical field of medicinal chemistry, and particularly relates to aminophenone compounds as well as a preparation method and application thereof. The aminophenone compounds provided by the invention have a good inhibition effect on PDE4, also have good bioavailability, can be applied to preparation of drugs for treating PDE4-related diseases, and increase the optionsof drugs for treating PDE4-related diseases; and the effect of a part of the aminophenone compounds is equivalent to the effect of positive drugs, and the aminophenone compounds have good developmentpotential.
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.
Influence of Alkyl Chain Ramification on Estradiol Receptor Binding Affinity and Intrinsic Activity of 1,2-Dialkylated 1,2-Bis(4- or 3-hydroxyphenyl)ethane Estrogens and Antiestrogens
Hartmann, Rolf W.
, p. 1668 - 1674 (2007/10/02)
The influence of a symmetrical introduction of CH3 substituents in the α or β positions of the 1,2-dialkyl-1,2-bis(4-hydroxyphenyl)ethene estrogens hexestrol (ethyl, HES) and octestrol (n-propyl, OCES) isopropyl (1), tert-butyl (2), sec-butyl (3), isobut