Design, synthesis and insulin-sensitising effects of novel PTP1B inhibitors
摘要:
Fifteen novel sulfathiazole-related compounds were designed as PTP1B inhibitors based on a previously reported allosteric inhibitor (1) of PTP1B. These compounds were synthesized and evaluated against human recombinant PTP1B. Six compounds (3, 4, 8 and 14-16) exhibited significant inhibitory activity against PTP1B. The most active compound (16) showed IC50 value of 3.2 mu M and kinetic analysis indicated that it is a non-competitive inhibitor of PTP1B. Furthermore, compound 16 demonstrated excellent selectivity to PTP1B over other PTPs. It also displayed in vivo insulin sensitizing effect in the insulin resistant mice. (C) 2013 Elsevier Ltd. All rights reserved.
[EN] THERMOPLASTIC POLYMER COMPOSITION<br/>[FR] COMPOSITION DE POLYMÈRE THERMOPLASTIQUE
申请人:MILLIKEN & CO
公开号:WO2015042561A1
公开(公告)日:2015-03-26
The invention provides a thermoplastic polymer composition comprising a polyolefin polymer and a nucleating agent. The nucleating agent comprises a compound conforming to the structure of Formula (I). The invention also provides a series of compounds encompassed by the structure of Formula (I).
The invention provides a compound conforming to the structure of Formula (CXX)
The invention also provides a thermoplastic polymer composition comprising a polyolefin polymer and a compound conforming to the structure of Formula (CXX) as a nucleating agent.