Synthesis and SAR of potent and orally bioavailable tert-butylpyrrolidine archetype derived melanocortin subtype-4 receptor modulators.
Discovery of a series of tert-butyl pyrrolidine derived, potent and orally bioavailable melanocortin receptor subtype-4 (MC4R) selective modulators is disclosed.
Guo
Liangqin
L
Department of Medicinal Chemistry, Merck Research Laboratories, 126 E. Lincoln Avenue, PO Box 2000, RY 50G-332, Rahway, NJ 07065, USA. liangqin_guo@merck.com
Ye
Zhixiong
Z
Ujjainwalla
Feroze
F
Sings
Heather L
HL
Sebhat
Iyassu K
IK
Huber
John
J
Weinberg
David H
DH
Tang
Rui
R
MacNeil
Tanya
T
Tamvakopoulos
Constantin
C
Peng
Qianping
Q
MacIntyre
Euan
E
van der Ploeg
Lex H T
LH
Goulet
Mark T
MT
Wyvratt
Matthew J
MJ
Nargund
Ravi P
RP
D000284:Administration, Oral; D006801:Humans; D015394:Molecular Structure; D011759:Pyrrolidines / Q000138:chemical synthesis* / Q000493:pharmacokinetics*; D044105:Receptor, Melanocortin, Type 4 / Q000819:agonists*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D019098:Telomerase
D011759:Pyrrolidines; D044105:Receptor, Melanocortin, Type 4; C509186:TERT protein, human; D019098:Telomerase