Zobrazeno 1 - 10
of 31
pro vyhledávání: '"Joseph P. Burkhart"'
Publikováno v:
Bioorganic & Medicinal Chemistry. 4:1411-1420
Steroids bearing a heteroaromatic substituent at C-17 were designed as inhibitors of C 17(20) lyase. The thiazoles, furans, and thiophenes appended to the steroid nucleus were positioned on the α-face and the β-face of the steroid, and conjugated w
Autor:
Michael R. Angelastro, Joseph P. Burkhart, M J Janusz, Chen Tm, Edward W. Huber, Koehl, Baugh Le, S L Durham, Philippe Bey, C M Hare
Publikováno v:
Journal of Medicinal Chemistry. 37:4538-4553
Valylprolylvalyl pentafluoroethyl ketones with different N-protecting groups were evaluated in vitro and in vivo as inhibitors of human neutrophil elastase (HNE). Several of these compounds were found to be orally active in HNE-induced rat and hamste
Publikováno v:
Journal of Heterocyclic Chemistry. 31:419-423
2,5-Bis-(3,4,5-trimethoxyphenyl)-2-oxazoline (5, MDL 100,270) was desi- gned as a potential plateletactivating factor (PAF) antagonist on the basis of computer modeling comparison studies with known PAF antagonis- ts. An efficient, four-step synthesi
Publikováno v:
The Journal of Steroid Biochemistry and Molecular Biology. 44:409-420
The design and syntheses of androstenedione derivatives with bridges spanning the 2,19-, 3,19-, 4,19- and 6,19-positions are described. 2,19-Bridged compounds bearing hydroxyl groups on the two-carbon bridge ( 3a and 3b ) were designed as stable carb
Publikováno v:
ChemInform. 23
Publikováno v:
ChemInform. 26
2,5-Bis-(3,4,5-trimethoxyphenyl)-2-oxazoline (5, MDL 100,270) was desi- gned as a potential plateletactivating factor (PAF) antagonist on the basis of computer modeling comparison studies with known PAF antagonis- ts. An efficient, four-step synthesi
Autor:
Dirk Friederich, Norton P. Peet, Michael R. Angelastro, Roy J. Vaz, Robert J. Resvick, Joseph P. Burkhart, Cynthia A. Gates, Philip M. Weintraub, Philippe Bey
Publikováno v:
ChemInform. 33
Publikováno v:
The Journal of Organic Chemistry. 57:5150-5154
The syntheses of 2,19-(methyleneoxy)androst-4-ene-3,17-dione (4a), a potent, time-dependent inhibitor of human placental aromatase, and its thio (4b), amino (5), and methylene (14) analogs are described. The key step in the construction of 4a, 4b, an
Publikováno v:
Journal of Medicinal Chemistry. 35:3303-3306
Publikováno v:
Tetrahedron Letters. 33:3265-3268
A concise method for the preparation of α-amino pentafluoroethyl ketone salts from amino acids is described. These intermediates are useful for the preparation of peptidyl pentafluoroethyl ketones.