Discovery of a Series of 6,7-Dimethoxy-4-pyrrolidylquinazoline PDE10A Inhibitors
A papaverine based pharmacophore model for PDE10A inhibition was generated via SBDD and used to design a library of 4-amino-6,7-dimethoxyquinazolines. From this library emerged an aryl ether pyrrolidyl 6,7-dimethoxyquinazoline series that became the focal point for additional modeling, X-ray, and sy...
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| Published in | Journal of medicinal chemistry Vol. 50; no. 2; pp. 182 - 185 |
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| Main Authors | , , , , , , , , , , , , , |
| Format | Journal Article |
| Language | English |
| Published |
WASHINGTON
American Chemical Society
25.01.2007
Amer Chemical Soc |
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| Online Access | Get full text |
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| Abstract | A papaverine based pharmacophore model for PDE10A inhibition was generated via SBDD and used to design a library of 4-amino-6,7-dimethoxyquinazolines. From this library emerged an aryl ether pyrrolidyl 6,7-dimethoxyquinazoline series that became the focal point for additional modeling, X-ray, and synthetic efforts toward increasing PDE10A inhibitory potency and selectivity versus PDE3A/B. These efforts culminated in the discovery of 29, a potent and selective brain penetrable inhibitor of PDE10A. |
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| AbstractList | A papaverine based pharmacophore model for PDE10A inhibition was generated via SBDD and used to design a library of 4-amino-6,7-dimethoxyquinazolines. From this library emerged an aryl ether pyrrolidyl 6,7-dimethoxyquinazoline series that became the focal point for additional modeling, X-ray, and synthetic efforts toward increasing PDE10A inhibitory potency and selectivity versus PDE3A/B. These efforts culminated in the discovery of 29, a potent and selective brain penetrable inhibitor of PDE10A. |
| Author | Liras, Spiros Pandit, Jayvardhan Fox, Carol B. Chappie, Thomas A. Yang, Feng V. Humphrey, John M. Allen, Martin P. Menniti, Frank S. Lebel, Lorraine A. Schmidt, Christopher J. Marr, Eric S. Williams, Robert D. Tu, Meihua Estep, Kimberly G. |
| Author_xml | – sequence: 1 givenname: Thomas A. surname: Chappie fullname: Chappie, Thomas A. – sequence: 2 givenname: John M. surname: Humphrey fullname: Humphrey, John M. – sequence: 3 givenname: Martin P. surname: Allen fullname: Allen, Martin P. – sequence: 4 givenname: Kimberly G. surname: Estep fullname: Estep, Kimberly G. – sequence: 5 givenname: Carol B. surname: Fox fullname: Fox, Carol B. – sequence: 6 givenname: Lorraine A. surname: Lebel fullname: Lebel, Lorraine A. – sequence: 7 givenname: Spiros surname: Liras fullname: Liras, Spiros – sequence: 8 givenname: Eric S. surname: Marr fullname: Marr, Eric S. – sequence: 9 givenname: Frank S. surname: Menniti fullname: Menniti, Frank S. – sequence: 10 givenname: Jayvardhan surname: Pandit fullname: Pandit, Jayvardhan – sequence: 11 givenname: Christopher J. surname: Schmidt fullname: Schmidt, Christopher J. – sequence: 12 givenname: Meihua surname: Tu fullname: Tu, Meihua – sequence: 13 givenname: Robert D. surname: Williams fullname: Williams, Robert D. – sequence: 14 givenname: Feng V. surname: Yang fullname: Yang, Feng V. |
| BackLink | https://www.ncbi.nlm.nih.gov/pubmed/17228859$$D View this record in MEDLINE/PubMed |
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| Snippet | A papaverine based pharmacophore model for PDE10A inhibition was generated via SBDD and used to design a library of 4-amino-6,7-dimethoxyquinazolines. From... |
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| SubjectTerms | Animals Chemistry, Medicinal Corpus Striatum - metabolism Crystallography, X-Ray Cyclic GMP - metabolism Life Sciences & Biomedicine Mice Models, Molecular Pharmacology & Pharmacy Phosphodiesterase Inhibitors - chemical synthesis Phosphodiesterase Inhibitors - chemistry Phosphodiesterase Inhibitors - pharmacology Phosphoric Diester Hydrolases - chemistry Phosphoric Diester Hydrolases - metabolism Pyrrolidines - chemical synthesis Pyrrolidines - chemistry Pyrrolidines - pharmacology Quinazolines - chemical synthesis Quinazolines - chemistry Quinazolines - pharmacology Science & Technology Structure-Activity Relationship |
| Title | Discovery of a Series of 6,7-Dimethoxy-4-pyrrolidylquinazoline PDE10A Inhibitors |
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