Diamine derivatives containing imidazolidinylidene propanedinitrile as a new class of histamine H3 receptor antagonists. Part I.
Novel diamine derivatives containing imidazolidinylidene propanedinitrile were synthesized and evaluated for histamine H(3) receptor-binding affinities. High-affinity ligands 3d, 3k, and 3n showed potent H(3) receptor antagonism and excellent selectivity over human H(1), H(2) and H(4) receptors.
Sasho
Setsuya
S
Medicinal Chemistry Research Laboratories, Pharmaceutical Research Center, Kyowa Hakko Kogyo Co. Ltd, 1188, Shimotogari, Nagaizumi-cho, Sunto-gun, Shizuoka-ken, 411-8731, Japan. setsuya.sasho@kyowa.co.jp
Seishi
Takashi
T
Kawamura
Mariko
M
Hirose
Ryo
R
Toki
Shinichiro
S
Shimada
Jun-ich
JI
D000818:Animals; D019556:COS Cells; D002522:Chlorocebus aethiops; D003959:Diamines / Q000138:chemical synthesis / Q000494:pharmacology*; D054828:Histamine H3 Antagonists / Q000138:chemical synthesis / Q000494:pharmacology*; D006801:Humans; D048289:Imidazolidines / Q000737:chemistry / Q000494:pharmacology*; D008024:Ligands; D008956:Models, Chemical; D009570:Nitriles / Q000737:chemistry / Q000494:pharmacology*; D011969:Receptors, Histamine H1 / Q000187:drug effects* / Q000378:metabolism; D011970:Receptors, Histamine H2 / Q000187:drug effects* / Q000378:metabolism; D018100:Receptors, Histamine H3 / Q000187:drug effects* / Q000378:metabolism; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D003959:Diamines; D054828:Histamine H3 Antagonists; D048289:Imidazolidines; D008024:Ligands; D009570:Nitriles; D011969:Receptors, Histamine H1; D011970:Receptors, Histamine H2; D018100:Receptors, Histamine H3