Hiroshi Sakashita

Discovery and preclinical profile of teneligliptin (3-[(2S,4S)-4-[4-(3-methyl-1-phenyl-1H-pyrazol-5-yl)piperazin-1-yl]pyrrolidin-2-ylcarbonyl]thiazolidine): A highly potent, selective, long-lasting and orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes

Tomohiro Yoshida, Fumihiko Akahoshi, Hiroshi Sakashita et al. · Bioorganic & Medicinal Chemistry · 2012 · 148 citations · Full text

Biochemistry, Medicine, Rational Drug Design +7

Synthesis, Structure−Activity Relationships, and Pharmacokinetic Profiles of Nonpeptidic Difluoromethylene Ketones as Novel Inhibitors of Human Chymase

Fumihiko Akahoshi, Atsuyuki Ashimori, Hiroshi Sakashita et al. · Journal of Medicinal Chemistry · 2001 · 38 citations · Full text

Medicinal Chemistry, Nonpeptidic Difluoromethylene Ketones, Pharmaceutical Science +15

Fused bicyclic heteroarylpiperazine-substituted l-prolylthiazolidines as highly potent DPP-4 inhibitors lacking the electrophilic nitrile group

Tomohiro Yoshida, Fumihiko Akahoshi, Hiroshi Sakashita et al. · Bioorganic & Medicinal Chemistry · 2012 · 36 citations · Full text

Combinatorial Chemistry, Medicinal Chemistry, Biochemistry +11

1-((S)-γ-Substituted prolyl)-(S)-2-cyanopyrrolidine as a novel series of highly potent DPP-IV inhibitors

Hiroshi Sakashita, Hiroshi Kitajima, Mitsuharu Nakamura et al. · Bioorganic & Medicinal Chemistry Letters · 2005 · 32 citations · Full text

Molecular Pharmacology, Medicinal Chemistry, Potent Dpp-iv Inhibitors +11

[(S)-γ-(Arylamino)prolyl]thiazolidine compounds as a novel series of potent and stable DPP-IV inhibitors

Hiroshi Sakashita, Fumihiko Akahoshi, Hiroshi Kitajima et al. · Bioorganic & Medicinal Chemistry · 2006 · 31 citations

Molecular Pharmacology, Medicinal Chemistry, Pharmaceutical Science +11