Design, synthesis, and pharmacological evaluation of dual histamine H2 and gastrin receptor antagonists

✍ Scribed by Yasuyuki Kawanishi; Shoichi Ishihara; Tadahiko Tsushima; Kaoru Seno; Masanori Miyagoshi; Sanji Hagishita; Michio Ishikawa; Noriko Shima; Mayumi Shimamura; Yasunobu Ishihara

• Publisher: Elsevier Science
• Year: 1996
• Tongue: English
• Weight: 436 KB
• Volume: 6
• Category: Article
• ISSN: 0960-894X
• DOI: 10.1016/s0960-894x(96)00248-x

✦ Synopsis

The joint type of hybrid molecules composed of two pharmacophore moieties taken from histamine H2 and gastrin receptor antagonists have been designed and synthesized to exhibit dual histamine H2 and gastrin receptor antagonistic activities. Here we report the importance of spacers as well as binding sites of both pharmacophores for the dual activity.