Zobrazeno 1 - 10
of 50
pro vyhledávání: '"George Y. Lesher"'
Autor:
Mary J. Connell, Baldev Singh, Paul J. Silver, Ross G. Bentley, Patrick O. Pennock, Bacon Edward R, Donald C. Bode, Linda T. Hamel, Edward D. Pagani, George Y. Lesher, Shaughnessy Robinson
Publikováno v:
Journal of Medicinal Chemistry. 38:2546-2550
The transformation of 3-bromo-1,6-naphthyridin-2(1H)-ones 8 to thiazolo[4,5-b][1,6]naphthyridin-2(1H)-ones 12 resulted in a 2-9-fold increase in cAMP phosphodiesterase (PDE) III inhibitory potency. Unlike the secondary binding sites on the cAMP PDE I
Autor:
David M. Sedlock, George Y. Lesher, Manohar Saindane, Sol J. Daum, Philip M. Carabateas, James B. Rake, Dorff Peter H, Michael Reuman, Robert B. Perni, S. A. Coughlin, Patrick O. Pennock, Mark P. Wentland, Baldev Singh, Monte D. Gruett
Publikováno v:
Journal of Medicinal Chemistry. 38:2531-2540
The palladium-catalyzed coupling of 3- and 4-(trialkylstannyl)pyridines with 7-bromo or 7-chloro 1-substituted 1,4-dihydro-4-oxo-3-quinolinecarboxylates has provided access to the corresponding 1-substituted 1,4-dihydro-4-oxo-7-pyridinyl-3-quinolinec
Autor:
Paul J. Silver, Buchholz Ra, Ronald L. Dundore, B Singh, George Y. Lesher, Edward R. Bacon, Edward D. Pagani, Donald C. Bode
Publikováno v:
Journal of Cardiovascular Pharmacology. 25:14-21
We describe the biochemical and pharmacologic effects of two novel fused pyridinones derived from milrinone: WIN 58993 and WIN 62005. Both WIN 58993 and WIN 62005 competitively inhibit cyclic GMP-inhibitable low Km cyclic AMP phosphodiesterase (PDE I
Autor:
Gee-Hong Kuo, George Y. Lesher, Edward R. Bacon, Michael Reuman, Michael Eissenstat, Kumar, John A. Dority, R. K. Fritz, Baldev Singh, Shaughnessy Robinson
Publikováno v:
Journal of Medicinal Chemistry. 37:248-254
The transformation of milrinone to 1,3-dihydro-5-methyl-6-(4-pyridinyl)-2H-imidazo[4,5-b]pyridin-2-one (13a), 5-methyl-6-(4-pyridinyl)thiazolo[4,5-b]pyridin-2(3H)-one (51), and 7-methyl-6-(4-pyridinyl)-1,8-naphthyridin-2(1H)-one (22) resulted in very
Autor:
Susan A. Coughlin, Manohar T. Saindane, James B. Rake, Michael Reuman, Baldev Singh, Michael Eissenstat, Mark P. Wentland, Garry M. Pilling, John D. Weaver, George Y. Lesher, Robert B. Perni
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 3:1711-1716
Several enantiomerically pure (2,6-dimethyl-4-pyridinyl)quinolones, previously shown to be potent inhibitors of bacterial DNA gyrase, exhibit topoisomerase II inhibitory activity. Among these and other analogues, topoisomerase II inhibitory potency w
Publikováno v:
Journal of Heterocyclic Chemistry. 30:37-40
Trifluoro or pentafluoroacylation of heteroaryl-enamines 2a,b gave the corresponding perfluoroacylated heteroaryl-enamines 3a-c. Heating the latter compounds with diethyl iminomalonate gave 2-amino-3-pyridinecarboxylates 4a-c. Hydrolysis to the free
Publikováno v:
ChemInform. 22
Reaction of phosphorus oxychloride with 2,6-dimethylpyridine N-oxide hydrochloride (1) gave a mixture of 2-(chloromethyl)-6-methylpyridine (2) and 4-chloro-2,6-dimethylpyridine (3). Treatment of this mixture with triethylamine converted 2 to the quat
Autor:
Baldev Singh, George Y. Lesher
Publikováno v:
ChemInform. 22
Publikováno v:
ChemInform. 22
Autor:
Baldev Singh, George Y. Lesher
Publikováno v:
ChemInform. 22
Several 8-alkyl-2-(4-pyridyl)adenine analogs 5 were prepared by reacting 4,5,6-triaminopyrimidine 4 with acid anhydrides, acids or dimethylformamide dimethyl acetal. 8-Mercapto-2-(4-pyridyl)-adenine (6), prepared by treating 4 with O-potassium O-ethy