Yoshida, Tomohiro; Akahoshi, Fumihiko; Sakashita, Hiroshi; Sonda, Shuji; Takeuchi, Masahiro; Tanaka, Yoshihito; Nabeno, Mika; Kishida, Hiroyuki; Miyaguchi, Ikuko; Hayashi, Yoshiharu published the artcile< Fused bicyclic heteroarylpiperazine-substituted L-prolylthiazolidines as highly potent DPP-4 inhibitors lacking the electrophilic nitrile group>, Synthetic Route of 401567-00-8, the main research area is antidiabetic DPP4 inhibitor heteroarylpiperazine prolylthiazolidine preparation structure activity.
Hypoglycemic agents with a mechanism of dipeptidyl peptidase IV (DPP-4) inhibition are suitable for once daily oral dosing. It is difficult to strike a balance between inhibitory activity and duration of action in plasma for inhibitors bearing an electrophilic nitrile group. We explored fused bicyclic heteroarylpiperazine substituted at the γ-position of the proline structure in the investigation of L-prolylthiazolidines lacking the electrophilic nitrile. Among them, 2-trifluoroquinolyl compound 8g is the most potent, long-lasting DPP-4 inhibitor (IC50 = 0.37 nmol/L) with high selectivity against other related peptidases. X-ray crystal structure determination of 8g indicates that CH-π interactions generated between the quinolyl ring and the guanidinyl group of Arg358 enhances the DPP-4 inhibitory activity and selectivity.
Bioorganic & Medicinal Chemistry published new progress about Antidiabetic agents. 401567-00-8 belongs to class imidazoles-derivatives, and the molecular formula is C8H4ClN3, Synthetic Route of 401567-00-8.
Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem