2ovy: Difference between revisions

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==Overview==

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.

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.

==About this Structure==

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[[Category: Rattus norvegicus]]

[[Category: Single protein]]

[[Category: Marr, E.S.]]

[[Category: Marr, E S.]]

[[Category: Pandit, J.]]

[[Category: MG]]

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[[Category: phosphodiesterase 10a; zn-binding site]]

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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 18:23:06 2008''

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@@ Line 4: / Line 4: @@
 ==Overview==
-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.
+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.
 ==About this Structure==
@@ Line 14: / Line 14: @@
 [[Category: Rattus norvegicus]]
 [[Category: Single protein]]
-[[Category: Marr, E.S.]]
+[[Category: Marr, E S.]]
 [[Category: Pandit, J.]]
 [[Category: MG]]
@@ Line 22: / Line 22: @@
 [[Category: phosphodiesterase 10a; zn-binding site]]
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jan 29 21:16:51 2008''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 18:23:06 2008''