2bhj: Difference between revisions

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==Overview==

Inducible nitric oxide synthase (iNOS) has been implicated in various, central and peripheral pathophysiological diseases. Our high throughput, screening initially identified a weak inhibitor of iNOS, thiocoumarin 13., From this lead, a number of potent derivatives were prepared that, demonstrate favorable potency, selectivity and kinetics. Compound 30 has, an IC50 of 60 nM for mouse iNOS and 185-fold and 9-fold selectivity for, bovine eNOS and rat nNOS, respectively. In cellular assays for iNOS, this, compound has micromolar potency. Furthermore, two compounds (16 and 30), demonstrate a reasonable pharmacokinetic profile in rodents. The, synthesis, SAR, and biological activity of this novel class of compounds, is described.

Inducible nitric oxide synthase (iNOS) has been implicated in various central and peripheral pathophysiological diseases. Our high throughput screening initially identified a weak inhibitor of iNOS, thiocoumarin 13. From this lead, a number of potent derivatives were prepared that demonstrate favorable potency, selectivity and kinetics. Compound 30 has an IC50 of 60 nM for mouse iNOS and 185-fold and 9-fold selectivity for bovine eNOS and rat nNOS, respectively. In cellular assays for iNOS, this compound has micromolar potency. Furthermore, two compounds (16 and 30) demonstrate a reasonable pharmacokinetic profile in rodents. The synthesis, SAR, and biological activity of this novel class of compounds is described.

==About this Structure==

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[[Category: Nitric-oxide synthase]]

[[Category: Single protein]]

[[Category: Guilloteau, J.P.]]

[[Category: Guilloteau, J P.]]

[[Category: Mathieu, M.]]

[[Category: FC1]]

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[[Category: zinc]]

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on ~~Sun~~ Feb ~~3 10~~:24:11 2008''

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 16:37:51 2008''

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@@ Line 4: / Line 4: @@
 ==Overview==
-Inducible nitric oxide synthase (iNOS) has been implicated in various, central and peripheral pathophysiological diseases. Our high throughput, screening initially identified a weak inhibitor of iNOS, thiocoumarin 13., From this lead, a number of potent derivatives were prepared that, demonstrate favorable potency, selectivity and kinetics. Compound 30 has, an IC50 of 60 nM for mouse iNOS and 185-fold and 9-fold selectivity for, bovine eNOS and rat nNOS, respectively. In cellular assays for iNOS, this, compound has micromolar potency. Furthermore, two compounds (16 and 30), demonstrate a reasonable pharmacokinetic profile in rodents. The, synthesis, SAR, and biological activity of this novel class of compounds, is described.
+Inducible nitric oxide synthase (iNOS) has been implicated in various central and peripheral pathophysiological diseases. Our high throughput screening initially identified a weak inhibitor of iNOS, thiocoumarin 13. From this lead, a number of potent derivatives were prepared that demonstrate favorable potency, selectivity and kinetics. Compound 30 has an IC50 of 60 nM for mouse iNOS and 185-fold and 9-fold selectivity for bovine eNOS and rat nNOS, respectively. In cellular assays for iNOS, this compound has micromolar potency. Furthermore, two compounds (16 and 30) demonstrate a reasonable pharmacokinetic profile in rodents. The synthesis, SAR, and biological activity of this novel class of compounds is described.
 ==About this Structure==
@@ Line 14: / Line 14: @@
 [[Category: Nitric-oxide synthase]]
 [[Category: Single protein]]
-[[Category: Guilloteau, J.P.]]
+[[Category: Guilloteau, J P.]]
 [[Category: Mathieu, M.]]
 [[Category: FC1]]
@@ Line 30: / Line 30: @@
 [[Category: zinc]]
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Feb  3 10:24:11 2008''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 16:37:51 2008''