Optimization of Pharmacokinetics through Manipulation of Physicochemical Properties in a Series of HCV Inhibitors
A novel series of HCV replication inhibitors based on a pyrido[3,2-d]pyrimidine core were optimized for pharmacokinetics (PK) in rats. Several associations between physicochemical properties and PK were identified and exploited to guide the design of compounds. In addition, a simple new metric that...
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| Veröffentlicht in: | ACS medicinal chemistry letters 2011-10, Vol.2 (10), p.715-719 |
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| creator | Lazerwith, Scott E Bahador, Gina Canales, Eda Cheng, Guofeng Chong, Lee Clarke, Michael O Doerffler, Edward Eisenberg, Eugene J Hayes, Jaclyn Lu, Bing Liu, Qi Matles, Mike Mertzman, Michael Mitchell, Michael L Morganelli, Philip Murray, Bernard P Robinson, Margaret Strickley, Robert G Tessler, Megan Tirunagari, Neeraj Wang, Jianhong Wang, Yujin Zhang, Jennifer R Zheng, Xubin Zhong, Weidong Watkins, William J |
| description | A novel series of HCV replication inhibitors based on a pyrido[3,2-d]pyrimidine core were optimized for pharmacokinetics (PK) in rats. Several associations between physicochemical properties and PK were identified and exploited to guide the design of compounds. In addition, a simple new metric that may aid in the prediction of bioavailability for compounds with higher polar surface area is described (3*HBD-cLogP). |
| doi_str_mv | 10.1021/ml200163b |
| format | Article |
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Chem. Lett</addtitle><description>A novel series of HCV replication inhibitors based on a pyrido[3,2-d]pyrimidine core were optimized for pharmacokinetics (PK) in rats. Several associations between physicochemical properties and PK were identified and exploited to guide the design of compounds. 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| language | eng |
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| source | EZB-FREE-00999 freely available EZB journals; PubMed Central; American Chemical Society Journals |
| subjects | Letter |
| title | Optimization of Pharmacokinetics through Manipulation of Physicochemical Properties in a Series of HCV Inhibitors |
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