Zobrazeno 1 - 10
of 15
pro vyhledávání: '"Kristie A. Faust"'
Autor:
Stephen E. de Laszlo, Raymond S. Chang, Tsing-Bau Chen, Kristie A. Faust, William J. Greenlee, Salah D. Kivlighn, Victor J. Lotti, Stacey S. O'Malley, Terry W. Schorn, Peter K. Siegl, Jennifer Tran, Gloria J. Zingaro
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 5:1359-1364
Modification of the 6-N-alkyl-N-acyl groups of L-159,689, 6 6-(N-benzoyl-N-pentyl)-amino-2-propyl-3-[(2′-(tetrazol-5-yl)biphen-4-yl)methyl]quinazolin-4-(3H)one led to the identification of the 6-(N-benzoyl-N-(3-pyridylmethyl)) analog (L-162,537). L
Autor:
Peter K. S. Siegl, Salah D. Kivlighn, Gloria J. Zingaro, Tsing-Bau Chen, Kristie A. Faust, Victor J. Lotti, William J. Greenlee, Arthur A. Patchett, Thomas F. Walsh, Kenneth J. Fitch, Raymond S.L. Chang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 5:1151-1154
Directed synthesis and pharmacological evaluation in a recently described class of α-phenoxyphenylacetic acid bearing angiotensin II (AII) receptor antagonists has afforded further potent AT 1 -selective AII antagonists. Substitution in the central
Autor:
Salah D. Kivlighn, Kenneth J. Fitch, W.J. Greenlee, T. F. Walsh, Peter K. S. Siegl, R. S. L. Chang, Kristie A. Faust, Arthur A. Patchett, Tsing-Bau Chen, Victor J. Lotti, Gloria J. Zingaro
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 5:155-158
A series of nonpeptidic AT1 selective angiotensin II (AII) antagonists containing a phenoxyphenylacetic acid element as a biphenyl tetrazole replacement have been identified. This series yielded compound 20 which exhibited binding affinities of AT1 =
Autor:
William J. Greenlee, Terry S. Schorn, Kristie A. Faust, Peter K. S. Siegl, Salah D. Kivlighn, Tsing-Bau Chen, Stephen E. de Laszlo, Gloria J. Zingaro, Victor J. Lotti, Tomasz W. Glinka, Raymond S.L. Chang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 4:2337-2342
The quinazoline sulfonylcarbamate L-163,579 (9) is a potent, balanced antagonist of the binding of angiotensin II (Ang II) to human AT 1 and AT 2 receptors. This antagonist produces a long-lasting blockade of Ang II-induced pressor response in both r
Autor:
Tsing-B. Chen, Kristie A. Faust, Elizabeth M. Naylor, Bradley V. Clineschmidt, Prasun K. Chakravarty, Victor J. Lotti, Robert J. Bendesky, Stacey A. O'Malley, Paul J. Kling, Raymond S.L. Chang, Arthur A. Patchett, William J. Greenlee
Publikováno v:
Drug Development Research. 32:161-171
MK-996 (N-((4′-((5,7-Dimethyl-2-ethyl-3H-imidazo[4,5-b]pyridin-3-yl)methyl) (1,1′-biphenyl)-2-yl) sulfonylbenzamide) interacted in a competitive manner with rabbit aortic angiotensin II (All) receptors as determined by Scatchard analysis of speci
Autor:
William J. Greenlee, Salah D. Kivlighn, Victor J. Lotti, Terry S. Schorn, Peter K. S. Siegl, Stephen E. de Laszlo, Raymond S.L. Chang, Gloria J. Zingaro, Tomasz W. Glinka, Tsing-Bau Chen, Kristie A. Faust
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 4:81-86
The structure activity relationships of a series of 2-alkyl-6-(acylamino)-3-[((2′-acylaminosulfonyl)biphenyl-4-yl)methyl]quinazolin-4-(3H)-ones were studied in order to identify balanced angiotensin II antagonists capable of potent binding to both
Autor:
L.W. Schaffer, Victor J. Lotti, Prasun K. Chakravarty, Wallace T. Ashton, Arthur A. Patchett, Tsing-Bau Chen, K. L. Flanagan, Salah D. Kivlighn, Elizabeth M. Naylor, W.J. Greenlee, Robert J. Bendesky, Linda L. Chang, Peter K. S. Siegl, R. S. L. Chang, Terry W. Schorn, Kristie A. Faust, Gloria J. Zingaro, Paul J. Kling
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 4:115-120
A series of trisubstituted triazolinones with a [2′-(N-acylsulfamoy)biphenyl-4-yl]methyl side chain at N4 has been prepared. The inhibition of AII pressor responses by these potent AT1-selective AII antagonists indicated some of them to be superior
Autor:
Gloria J. Zingaro, William J. Greenlee, Tsing-Bau Chen, Kristie A. Faust, Pancras C. Wong, Ruth R. Wexler, Victor J. Lotti, Peter K. S. Siegl, Raymond S.L. Chang, Prasun K. Chakravarty, Elizabeth M. Naylor, Salah D. Kivlighn, Colleen A. Costello, Arthur A. Patchett, David J. Carini
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 4:69-74
Acyl sulfonamides and acyl sulfamides were synthesized and their in vitro and in vivo biological properties evaluated. AT1 binding affinities for these potent AII antagonists were similar to their tetrazole analogs. An enhancement in AT2 potencies wa
Autor:
Victor J. Lotti, Wallace T. Ashton, Flanagan Kl, R. S. L. Chang, William J. Greenlee, M. Maccoss, Tsing-Bau Chen, Robert A. Strelitz, Linda L. Chang, Kristie A. Faust
Publikováno v:
Journal of Medicinal Chemistry. 36:2558-2568
A series of 2,4-dihydro-2,4,5-trisubstituted-3H-1,2,4-triazol-3-ones was prepared via several synthetic routes and evaluated as AII receptor antagonists in vitro and in vivo. The preferred compounds contained a [2'-(5-tetrazolyl)biphenyl-4-yl]methyl
Autor:
William J. Greenlee, Tsing-Bau Chen, Kristie A. Faust, Stephen E. de Laszlo, Carol S. Quagliato, Victor J. Lotti, Raymond S.L. Chang, Song X. Huang, Eric E. Allen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 3:1293-1298
We present the design, syntheses, and in vitro biological data of a series of substituted quinazolinone containing, AT1 selective, Angiotensin II (AII) receptor antagonists. Substituents at the 6-position of the quinazolin-4(3H)-ones 3 have pronounce