Kuroda, Shoichi; Kobashi, Yohei; Kawamura, Madoka; Kawabe, Kenichi; Shiozawa, Fumiyasu; Hamada, Makoto; Shimizu, Yuki; Okumura-Kitajima, Lisa; Koretsune, Hiroko; Kimura, Kayo; Yamamoto, Koji; Kakinuma, Hiroyuki published an article in Chemical & Pharmaceutical Bulletin. The title of the article was 《Synthesis and structure-activity relationship of C-phenyl D-glucitol (TP0454614) derivatives as selective sodium-dependent glucose cotransporter 1 (SGLT1) inhibitors》.Reference of Piperidine-4-carboxamide The author mentioned the following in the article:
Sodium-glucose cotransporter 1 (SGLT1) is the primary transporter for glucose absorption from the gastrointestinal tract. While C-Ph d-glucitol derivative SGL5213 has been reported to be a potent intestinal SGLT1 inhibitor for use in the treatment of type 2 diabetes, no SGLT1 selectivity was found in vitro (IC50 29 nM for hSGLT1 and 20 nM for hSGLT2). In this study we found a new method of synthesizing key intermediates 12 by a one-pot three-component condensation reaction and discovered C-Ph d-glucitol 41j (TP0454614), which has >40-fold SGLT1 selectivity in vitro (IC50 26 nM for hSGLT1 and 1101 nM for hSGLT2). The results of our study have provided new insights into the structure-activity relationships (SARs) of the SGLT1 selectivity of C-glucitol derivatives The results came from multiple reactions, including the reaction of Piperidine-4-carboxamide(cas: 39546-32-2Reference of Piperidine-4-carboxamide)
Piperidine-4-carboxamide(cas: 39546-32-2) belongs to anime. Amine, any member of a family of nitrogen-containing organic compounds that is derived, either in principle or in practice, from ammonia (NH3). Naturally occurring amines include the alkaloids, which are present in certain plants; the catecholamine neurotransmitters (i.e., dopamine, epinephrine, and norepinephrine); and a local chemical mediator, histamine, that occurs in most animal tissues.Reference of Piperidine-4-carboxamide
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem