Metabohc stabihty

Consequently, S-1360, a triazole analogue of DKA, was the first integrase strand transfer inhibitor (INSTI) to enter clinical trials, but the development was stopped during phase Eli (Billich 2003). Subsequently, a novel series of potent INSTIs, which replaced the 1,3-diketo acid moiety by an isosteric 8-hydroxy-1,6-naphthyridine core, showed improved metabohc stabihty (Zhuang et al. 2003). The compound L-870,810 moved into clinical trials, where it provided proof of concept in antiretroviral therapy-experienced and antiretroviral therapy-naive... 

A series of selective D2 dopamine receptor agonists were discovered and optimized to obtain benzothiazepine amide 161, a lead compound that possessed good in vitro physical properties, metaboHc stabihty, and in vivo pharmacokinetics (14JME3450). A number of 8-alkoxy-4,5-dihydrobenzo[l)] [l,2,4]triazolo[4,3-(/][l,4]thiazepine derivatives were synthesized, with compound 162 showing potent anticonvulsant activity (14JEIM272). 

Xu, R., Manuel, M., Cramlett, J., et al. (2010) A high throughput metabohc stabihty screening workflow with automated assessment of data quahty in pharmaceutical industry. Journal of Chromatography. A, 1217,1616-1625. 

Shou, W.Z., Magis, L., Li, A.C., et al. (2005) A novel approach to perform metabohte screening during the quantitative LC-MS/MS analyses of in vitro metabohc stabihty samples using a hybrid triple-quadrupole linear... 

Kubiak, T.M. et al.. Position 2 and position 2/Alal5-substituted analogs of bovine growth hormone-releasing factor (bGRF) with enhanced metabohc stabihty and improved in vivo... 

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