Azole derivatives as histamine H3 receptor antagonists, part 2: C-C and C-S coupled heterocycles.
With a small series of compounds we demonstrated the variability in the core region of the human histamine H(3) receptor (hH(3)R) antagonist structural blueprint by introducing polar azole groups (oxazole, oxadiazole, thiazole and triazole). Additional variations achieved by coupling different residues to the heterocyclic core structure led to further optimisation of in vitro receptor binding of the novel azole derivatives.
Walter
M
M
Johann Wolfgang Goethe University, Institute of Pharmaceutical Chemistry, Biozentrum, ZAFES/LiFF/CMP/ICNF, Max-von-Laue-Str. 9, 60438 Frankfurt, Germany.
Isensee
K
K
Kottke
T
T
Ligneau
X
X
Camelin
J-C
JC
Schwartz
J-C
JC
Stark
H
H
D001393:Azoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D002244:Carbon / Q000737:chemistry*; D002460:Cell Line; D006571:Heterocyclic Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D054828:Histamine H3 Antagonists / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D011485:Protein Binding; D018100:Receptors, Histamine H3 / Q000737:chemistry* / Q000378:metabolism; D013329:Structure-Activity Relationship; D013455:Sulfur / Q000737:chemistry*
D001393:Azoles; D006571:Heterocyclic Compounds; D054828:Histamine H3 Antagonists; D018100:Receptors, Histamine H3; D013455:Sulfur; D002244:Carbon