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2005
Receptor binding activity
X 0280
Tryptamine-Based Human β3-Adrenergic Receptor Agonists. Part 2. SAR of the
Derivatives. — A previously synthesized potent tryptamine-based β3-AR
15- 245 Methylene
agonist is modified by replacing the thiophene moiety in the sulfonamide part by an
aminobenzene moiety as well as by removing the chiral methyl center to simplify the
synthesis of this class of compounds. Analogue (I) shows excellent agonistic activity
for β3-AR with excellent subtype selectivity. Furthermore, sulfonamide derivative (I)
has a very strong binding constant and reveals excellent selectivity over binding to the
β1- and β2-ARs. — (SAWA*, M.; TATEISHI, H.; MIZUNO, K.; HARADA, H.; OUE,
M.; TSUJIUCHI, H.; FURUTANI, Y.; KATO, S.; Bioorg. Med. Chem. Lett. 14 (2004)
24, 5963-5966; Chem. Res. Lab., Dainippon Pharm. Co., Ltd., Suita,
Osaka 564, Japan; Eng.) — H. Hoennerscheid
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