title: Synthesis and pharmacological characterization of 1-benzyl-4-aminoindole-based thyroid hormone receptor β agonists.
abstract: A series of 1-benzylindole-based TRβ agonists were prepared and evaluated. Compounds 11b' and 11c' were found to have cholesterol-lowering in a rat model with marginal effects on cardiac function and HPT axis. The present work illustrates the potential use of indoles as inner ring isosteres.
authors.affiliation: Drug Discovery Laboratories, Sanwa Kagaku Kenkyusho Co., Ltd, 363 Shiosaki, Hokusei-cho, Inabe-city, Mie 511-0406, Japan.
authors.forename: Naoki
authors.initials: N
authors.lastname: Takahashi
authors.affiliation: Drug Discovery Laboratories, Sanwa Kagaku Kenkyusho Co., Ltd, 363 Shiosaki, Hokusei-cho, Inabe-city, Mie 511-0406, Japan.
authors.forename: Koji
authors.initials: K
authors.lastname: Maeda
authors.affiliation: Product Planning II, R&D Planning Department, R&D Strategy Center, Sanwa Kagaku Kenkyusho Co., Ltd, 35 Higashisotobori-cho, Higashi-ku, Nagoya 461-8631, Japan.
authors.forename: Yukiyasu
authors.initials: Y
authors.lastname: Asano
authors.affiliation: Drug Discovery Laboratories, Sanwa Kagaku Kenkyusho Co., Ltd, 363 Shiosaki, Hokusei-cho, Inabe-city, Mie 511-0406, Japan. Electronic address: no_watanabe@skk-net.com.
authors.forename: Nobuhide
authors.initials: N
authors.lastname: Watanabe
mesh_terms: D000818:Animals; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D037042:Thyroid Hormone Receptors beta / Q000819:agonists / Q000187:drug effects*
chemical_list: D007211:Indoles; D037042:Thyroid Hormone Receptors beta; C000164:1-benzylindole
keywords: Dyslipidemia; Hypothalamic/pituitary/thyroid axis; Thyroid hormone receptor β agonists; Thyroid stimulating hormone