BMS-201620: a selective beta 3 agonist.
A series of N-(4-hydroxy-3-methylsulfonanilidoethanol)arylglycinamides were prepared and evaluated for their human beta3 adrenergic receptor agonist activity. SAR studies led to the identification of BMS-201620 (39), a potent beta3 full agonist (Ki = 93 nM, 93% activation). Based on its favorable safety profile, BMS-201620 was chosen for clinical evaluation.
Washburn
W N
WN
Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543, USA. william.washburn@bms.com
Sun
C-Q
CQ
Bisacchi
G
G
Wu
G
G
Cheng
P T
PT
Sher
P M
PM
Ryono
D
D
Gavai
A V
AV
Poss
K
K
Girotra
R N
RN
McCann
P J
PJ
Mikkilineni
A B
AB
Dejneka
T C
TC
Wang
T C
TC
Merchant
Z
Z
Morella
M
M
Arbeeny
C M
CM
Harper
T W
TW
Slusarchyk
D A
DA
Skwish
S
S
Russell
A D
AD
Allen
G T
GT
Tesfamariam
B
B
Frohlich
B H
BH
Abboa-Offei
B E
BE
Cap
M
M
Waldron
T L
TL
George
R J
RJ
Young
D
D
Dickinson
K E
KE
Seymour
A A
AA
D058667:Adrenergic beta-3 Receptor Agonists; D000318:Adrenergic beta-Agonists / Q000138:chemical synthesis / Q000494:pharmacology*; D000818:Animals; D004305:Dose-Response Relationship, Drug; D004353:Drug Evaluation, Preclinical; D005998:Glycine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000882:Haplorhini; D006801:Humans; D008745:Methylation; D022702:Receptors, Adrenergic, beta-3 / Q000378:metabolism; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D058667:Adrenergic beta-3 Receptor Agonists; D000318:Adrenergic beta-Agonists; C495735:BMS-201620; D022702:Receptors, Adrenergic, beta-3; C018556:glycine amide; D005998:Glycine