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Design , synthesis and activity of new anti II diabetes PTP-1B inhibitors

Author: LuDianYun
Tutor: HuChun；XiaoZhiYan
School: Shenyang Pharmaceutical University
Course: Medicinal Chemistry
Keywords: Medicinal Chemistry Drug Design Protein tyrosine phosphatase 1B Synthesis Anti-diabetic drug
CLC: R914
Type: Master's thesis
Year: 2006
Downloads: 44
Quote: 0
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Abstract


Protein tyrosine phosphatase 1B (PTP-1B) is a negative regulator of insulin and leptin signaling pathway . Mouse PTP-1B knockout and antisense oligonucleotide therapy experiments showed that PTP-1B is a potential target for the treatment of diabetes and obesity . Therefore , the use of small molecules to inhibit PTP-1B enzyme may become a new way to treat insulin resistance , type II diabetes and obesity . In order to find new PTP-1B inhibitor treatment of type Ⅱ diabetes , mainly for the following work : analysis summarizes the known crystal structure of PTP-1B inhibitors with the enzyme complex interaction way and inhibitor molecules summarized the pharmacophore model , according to the pharmacophore model and drug-like requirements , combined with synthetic feasibility , design for the catalytic activity of PTP-1B regional and allosteric sites following nine categories of target compounds in two different binding modes : the use of different the synthetic route of synthesis of target compounds have not been reported , 30 structures were recognized by ~ 1HNMR and MS . In addition , in the process of synthesis of target compounds synthesized some of the key intermediate 58 , of which 31 compounds have not been reported . Some target compounds synthesized recombinant PTP-1B activity inhibition experiments , the results show that : the area designed for the catalytic activity of PTP-1B compounds inhibit the activity is not ideal , and did not get the expected results . Allosteric inhibitor compound LDY - 4- 7 - 4 -23 and LDY - 5 -19 inhibitory activity in LDY better structural transformation of such compounds for the pilot , it is desirable to obtain a high inhibitory activity of PTP- 1B inhibitors .

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