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Prediction of drug absorption using multivariate statistics.
Literature data on compounds both well- and poorly-absorbed in humans were used to build a statistical pattern recognition model of passive intestinal absorption. Robust outlier detection wasExpand
Transglutaminase inhibition by 2-[(2-oxopropyl)thio]imidazolium derivatives: mechanism of factor XIIIa inactivation.
The physiologic role of several transglutaminases could be more precisely defined with the development of specific inhibitors for these enzymes. In addition, specific plasma transglutaminase (fXIIIa)Expand
Allosteric inhibitors of inducible nitric oxide synthase dimerization discovered via combinatorial chemistry.
Potent and selective inhibitors of inducible nitric oxide synthase (iNOS) (EC ) were identified in an encoded combinatorial chemical library that blocked human iNOS dimerization, and thereby NOExpand
Discovery of 2-hydroxy-N,N-dimethyl-3-{2-[[(R)-1-(5- methylfuran-2-yl)propyl]amino]-3,4-dioxocyclobut-1-enylamino}benzamide (SCH 527123): a potent, orally bioavailable CXCR2/CXCR1 receptor antagonist.
Structure-activity studies on lead cyclobutenedione 3 led to the discovery of 4 (SCH 527123), a potent, orally bioavailable CXCR2/CXCR1 receptor antagonist with excellent cell-based activity.Expand
Blockade of peripheral α2‐adrenoceptors by L‐659,066 enhances glucose tolerance and insulin release in mice
The purpose of this study was to compare the effects of a peripherally selective (L‐659,066) vs. a centrally and peripherally active (L‐657,743; MK‐912) α2‐adrenergic antagonist on murine plasmaExpand
Thienothiopyran-2-sulfonamides: novel topically active carbonic anhydrase inhibitors for the treatment of glaucoma.
The bulk of aqueous humor entering the eye is produced through an active secretory process by the nonpigmented epithelial cells of the ciliary process. Carbonic anhydrase is present in these cells,Expand
Type Ic, a novel glycogenosis. Underlying mechanism.
The availability of a fresh, unfrozen liver biopsy specimen permitted the characterization of a unique type of glycogen storage disease. The subject, an 11-year-old female, showed the classicExpand
Positions of His‐64 and a bound water in human carbonic anhydrase II upon binding three structurally related inhibitors
The 3‐dimensional structure of human carbonic anhydrase II (HCAII; EC complexed with 3 structurally related inhibitors, la, lb, and lc, has been determined by X‐ray crystallographic methods.Expand
Topically active carbonic anhydrase inhibitors. 2. Benzo[b]thiophenesulfonamide derivatives with ocular hypotensive activity.
Derivatives of benzo[b]thiophene-2-sulfonamide were prepared to investigate their potential utility as topically active inhibitors of ocular carbonic anhydrase. Such an agent would be useful in theExpand