Zobrazeno 1 - 10
of 108
pro vyhledávání: '"Victor J. Lotti"'
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:
Ralph A. Rivero, Peter K. S. Siegl, K. L. Flanagan, Salah D. Kivlighn, Wallace T. Ashton, Gloria J. Zingaro, Tsing-Bau Chen, Victor J. Lotti, R. S. L. Chang, S. S. O'malley, W.J. Greenlee, Linda L. Chang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 4:2787-2792
A series of subnanomolar (IC50 triazolinone-based AT1/AT2-balanced AII antagonists has been identified. The 70-240-fold gain in AT2 activity relative to prototype compounds was achieved by the introduction of a 5-acylamino group on the N2-aryl moiety
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:
Gloria J. Zingaro, Salah D. Kivlighn, Peter K.S. Siegel, Raymond S.L. Chang, Victor J. Lotti, Robert A. Strelitz, Arthur A. Patchett, William J. Greenlee, Terry W. Schorn, Prasun K. Chakravarty, Tsing-Bau Chen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 4:75-80
A new series of quinazolinone-based AT 1 selective antagonists, bearing acylsulfonamides (-SO 2 NHCOR) as the tetrazole bioisosteres, was evaluated. While AT 1 potencies remained similar to the tetrazole analogs, the AT 2 receptor affinities were sig
Autor:
William J. Greenlee, Peter K. S. Siegl, Victor J. Lotti, Kenneth J. Fitch, Salah D. Kivlighn, Malcolm MacCoss, Thomas F. Walsh, Arthur A. Patchett, Raymond S.L. Chang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 4:219-222
The synthesis of a new class of angiotensin II receptor antagonists bearing a substituted imidazo[1,2-b]pyridazine moiety, and the evaluation of these compounds as isosteric replacements for potent imidazo[4,5-b]pyridine based antagonists is presente
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