40615-11-0Relevant articles and documents
Design and synthesis of DPP-IV inhibitors lacking the electrophilic nitrile group
Kondo, Takashi,Nekado, Takahiro,Sugimoto, Isamu,Ochi, Kenya,Takai, Shigeyuki,Kinoshita, Atsushi,Hatayama, Akira,Yamamoto, Susumu,Kishikawa, Katsuya,Nakai, Hisao,Toda, Masaaki
, p. 1613 - 1631 (2008/09/20)
A series of (4β-substituted)-l-prolylpyrrolidine analogs lacking the electrophilic nitrile function were synthesized and their dipeptidyl peptidase IV (DPP-IV) inhibitory activity and duration of ex vivo activity were evaluated. Structural optimization of a N-(3-phenyl-1,2,4-thiadiazol-5-yl)piperazine analog 8, which was found by high-speed analog synthesis, was carried out to improve the potency and duration of action. A representative compound 26 was evaluated to assess its effect on the plasma glucose level after the oGTT (oral glucose tolerance test) in normal rats. Structure-activity relationships (SAR) are also presented.
[4-(HETEROARYL) PIPERAZIN-1-YL]-(2,5-SUBSTITUTED -PHENYL)METHANONE DERIVATIVES AS GLYCINE TRANSPORTER 1 (GLYT-1) INHIBITORS FOR THE TREATMENT OF NEUROLOGICAL AND NEUROPSYCHIATRIC DISORDERS
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Page/Page column 34, (2008/06/13)
The present invention relates to compounds of the general formula (I) wherein R1 is-OR1’,-SR1’ or is a heterocycloalkyl group; R1’ is lower alkyl, lower alkyl substituted by halogen or is -(CH2)n
