16478-52-7Relevant articles and documents
Pyridine - 2 - amide compound and its preparation method, its pharmaceutical composition and use thereof
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Paragraph 0092; 0097; 0098, (2018/04/01)
The invention relates to a pyridine-2-amide compound shown as a general formula I as well as a preparation method, a pharmaceutical composition and use thereof. The compound as an integrase inhibitor is used for preparing medicines for treating diseases mediated by various vetrovirus integrases including HIV-1 (Human Immunodeficiency Virus-1) integrase.
Inhibitors of type I MetAPs containing pyridine-2-carboxylic acid thiazol-2-ylamide. Part 1: SAR studies on the determination of the key scaffold
Luo, Qun-Li,Li, Jing-Ya,Liu, Zhi-Ying,Chen, Ling-Ling,Li, Jia,Ye, Qi-Zhuang,Nan, Fa-Jun
, p. 635 - 638 (2007/10/03)
Systematic SAR studies on the HTS hit pyridine-2-carboxylic acid thiazol-2-ylamide (PACT) analogues revealed that the scaffold of PCAT is indispensable for the inhibition of type I MetAP. For effective inhibition of the enzyme, the most suitable position to modify is the 3-position of the pyridine ring of PCAT, and the best substituents are those containing O or N atoms connected directly with the pyridine ring. These findings provide useful information for the design and discovery of more potent inhibitors of type I MetAPs.