Non-imidazole heterocyclic histamine H3 receptor antagonists.
Continued exploration of the SAR around the lead imidazopyridine histamine H(3) antagonist 1 has led to the discovery of several related series of heterocyclic histamine H(3) antagonists. The synthesis and SAR of indolizine, indole and pyrazolopyridine based compounds are now described.
Johnson & Johnson Pharmaceutical Research and Development L. L. C., 3210 Merryfield Row, San Diego, CA 92121, USA. wchai@prdus.jnj.com
Wenying
W
Chai
J Guy
JG
Breitenbucher
Annette
A
Kwok
Xiaobing
X
Li
Victoria
V
Wong
Nicholas I
NI
Carruthers
Timothy W
TW
Lovenberg
Curt
C
Mazur
Sandy J
SJ
Wilson
Frank U
FU
Axe
Todd K
TK
Jones
D000818:Animals; D001711:Biotransformation; D002460:Cell Line; D002463:Cell Membrane Permeability; D004355:Drug Stability; D006576:Heterocyclic Compounds, 4 or More Rings / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D006633:Histamine Antagonists / Q000138:chemical synthesis* / Q000493:pharmacokinetics* / Q000494:pharmacology; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis / Q000494:pharmacology; D007212:Indolizines / Q000138:chemical synthesis / Q000494:pharmacology; D008862:Microsomes, Liver; D011720:Pyrazoles / Q000138:chemical synthesis / Q000494:pharmacology; D011725:Pyridines / Q000138:chemical synthesis / Q000494:pharmacology; D051381:Rats; D018100:Receptors, Histamine H3; D013329:Structure-Activity Relationship
D006576:Heterocyclic Compounds, 4 or More Rings; D006633:Histamine Antagonists; D007211:Indoles; D007212:Indolizines; D011720:Pyrazoles; D011725:Pyridines; D018100:Receptors, Histamine H3; C118531:pyrazolopyridine