Identification and characterization of amino-piperidinequinolones and quinazolinones as MCHr1 antagonists.
Several potent, functionally active MCHr1 antagonists derived from quinolin-2(1H)-ones and quinazoline-2(1H)-ones have been synthesized and evaluated. Pyridylmethyl substitution at the quinolone 1-position results in derivatives with low-nM binding potency and good selectivity with respect to hERG binding.
Blackburn
Christopher
C
Millennium Pharmaceuticals, Inc., 40 Landsdowne St. Cambridge, MA 02139, USA. chris.blackburn@mpi.com
LaMarche
Matthew J
MJ
Brown
James
J
Che
Jennifer Lee
JL
Cullis
Courtney A
CA
Lai
Sujen
S
Maguire
Martin
M
Marsilje
Thomas
T
Geddes
Bradley
B
Govek
Elizabeth
E
Kadambi
Vivek
V
Doherty
Colleen
C
Dayton
Brian
B
Brodjian
Sevan
S
Marsh
Kennan C
KC
Collins
Christine A
CA
Kym
Philip R
PR
D000818:Animals; D051379:Mice; D011799:Quinazolines / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology*; D015363:Quinolones / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology*; D011979:Receptors, Pituitary Hormone / Q000037:antagonists & inhibitors*
D011799:Quinazolines; D015363:Quinolones; D011979:Receptors, Pituitary Hormone; C092274:melanin-concentrating hormone receptor