121489-29-0Relevant academic research and scientific papers
Discovery of a novel series of benzoic acid derivatives as potent and selective human β3 adrenergic receptor agonists with good oral bioavailability. 3. Phenylethanolaminotetraline (PEAT) skeleton containing biphenyl or biphenyl ether moiety
Imanishi, Masashi,Nakajima, Yutaka,Tomishima, Yasuyo,Hamashima, Hitoshi,Washizuka, Kenichi,Sakurai, Minora,Matsui, Shigeo,Imamura, Emiko,Ueshima, Koji,Yamamoto, Takao,Yamamoto, Nobuhiro,Ishikawa, Hirofumi,Nakano, Keiko,Unami, Naoko,Hamada, Kaori,Matsumura, Yasuhiro,Takamura, Fujiko,Hattori, Kouji
, p. 4804 - 4822 (2009/07/11)
We designed a series of benzoic acid derivatives containing the biphenyl ether or biphenyl template on the RHS and a phenylethanolaminotetraline (PEAT) skeleton, which was prepared by highly stereoselective synthesis, to generate two structurally different lead compounds (10c, 10m) with a good balance of potency, selectivity, and pharmacokinetic profile. Further optimization of the two lead compounds to improve potency led to several potential candidates (i.e., 11f, 11l, 11o, 12b). In particular, biphenyl analogue 12b exhibited an excellent balance of high potency (EC50 = 0.38 nM) for β3, high selectivity over β1 and β2, and good pharmacokinetic properties in rats, dogs, and monkeys.
Synthesis and β-adrenergic activity of atypical β-adrenergic phenylethanolaminotetralin stereoisomers
Cecchi, R.,Croci, T.,Boigegrain, R.,Boveri, S.,Baroni, M.,et al.
, p. 259 - 268 (2007/10/02)
A series of substituted phenylethanolaminotetralins were synthesized as pure stereoisomers and their ability to stimulate atypical β-adrenoceptors selectively was evaluated.The compounds in vitro relative potencies were assessed using the atypical β respo
