In their quest to develop specific ligands for drug target proteins, Professor Satoshi Shuto and coll. have used a stereochemical diversity-oriented conformational restriction strategy to synthesize potent histamine H3 and/or H4 receptor ligands. Some of these cyclopropane-based analogs of histamine with a chiral cis- or trans-2,3-methanobutane backbone show remarkable antagonistic activity towards H3 and H4.
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Cyclopropane-based stereochemical diversity-oriented conformational restriction strategy: Histamine H3 and/or H4 receptor ligands with the 2,3-methanobutane backbone
Mizuki Watanabe, Takaaki Kobayashi, Takatsugu Hirokawa, Akira Yoshida, Yoshihiko Ito, Shizuo Yamada, Naoki Orimoto, Yasundo Yamasaki, Mitsuhiro Arisawa and Satoshi Shuto
Org. Biomol. Chem., 2012, Advance Article
DOI: 10.1039/C1OB06496G, Paper
