Zobrazeno 1 - 10
of 53
pro vyhledávání: '"J. Zingaro"'
Autor:
Haifeng Tang, Zack Zhiqiang Guo, Lee-Yuh Pai, Adam B. Weinglass, Xin Gu, Shuzhi Dong, Alexander Pasternak, Yang Yu, Kathleen A. Sullivan, Mengwei Hu, Kelsey VanGelder, Gloria J. Zingaro, Sophie Roy, Jessica Liu, Qinghong Fu, Birgit T. Priest, Michael Margulis, Brande Thomas-Fowlkes, Pierre Morissette, Robin E. Haimbach, Zhicai Wu, Juliann Ehrhart, Karen Owens, Caryn Hampton, Zhi-Cai Shi, Jessica Frie, Ron Ferguson, Shiyao Xu, Vincent Tong
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 27:2559-2566
SAR in the previously described spirocyclic ROMK inhibitor series was further evolved from lead 4 by modification of the spirocyclic core and identification of novel right-side pharmacophores. In this process, it was discovered that the spiropyrrolid
Autor:
A. Galijatovic-Idrizbegovic, S. O'Sullivan, H. Schuck, K.A. Bustard, Alysia A. Chaves, Richard Briscoe, M.A. Yordy, C.M. Hoe, D.B. Christian, Gloria J. Zingaro
Publikováno v:
Journal of Pharmacological and Toxicological Methods. 56:103-114
Introduction Preclinical evaluation of delayed ventricular repolarization manifests electrocardiographically as QT interval prolongation and is routinely used as an indicator of potential risk for pro-arrhythmia (potential to cause Torsades de Pointe
Autor:
J. Zingaro, R. Chris Clarke, J.C. Golombeck, Andre Berghmans, Tracy Wait, Hong Zhang, Narsingh B. Singh
Publikováno v:
Journal of Crystal Growth. 250:107-112
Single crystals of aluminum nitride were grown by physical vapor transport (PVT) method. Evaluation of transport conditions was carried out during bulk growth of aluminum nitride in a vertical, cylindrical geometry. Experiments were carried out for t
The anesthetized guinea pig: an effective early cardiovascular derisking and lead optimization model
Autor:
Jeffrey Travis, Chao-Min Hoe, Joseph J. Salata, Gloria J. Zingaro, Matthew M. Zrada, Pamela Gerenser, Armando Lagrutta, John Imredy, Elena Trepakova, Alysia A. Chaves, Greg Friedrichs, Masahiro Nishida, Kimberly M. Hoagland, Pierre Morissette
Publikováno v:
Journal of pharmacological and toxicological methods. 68(1)
Introduction In recent years, the anesthetized guinea pig has been used increasingly to evaluate the cardiovascular effects of drug-candidate molecules during lead optimization prior to conducting longer, more resource intensive safety pharmacology a
Autor:
Theodore P. Broten, William J. Greenlee, Robert A. Gabel, Nathan B. Mantlo, Peter K. S. Siegl, Debra Ondeyka, Salah D. Kivlighn, Raymond S.L. Chang, Gloria J. Zingaro, Raymond E. Gibson
Publikováno v:
European Journal of Pharmacology. 294:439-450
L-163,017 (6-[benzoylamino]-7-methyl-2-propyl-3-[(2′-(N-(3-methyl-1-butoxy)carbonylaminosulfonyl)[1,1′]-biphenyl-4-yl]-methyl]-3H-imidazo-[4,5-b] is a potent, orally active, nonpeptide angiotensin II receptor antagonist. Conscious rats and dogs w
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:
Robert A. Gabel, Theodore P. Broten, Gloria J. Zingaro, Linda W. Schaffer, Peter K. S. Siegl, Arthur A. Patchett, Terry W. Schorn, William J. Greenlee, Prasun K. Chakravarty, Elizabeth M. Naylor, Salah D. Kivlighn
Publikováno v:
American Journal of Hypertension. 8:58-66
MK-996, N-(4'-(5,7-dimethyl-2-ethyl-3H-imidazo[4,5-b]pyridin-3-yl- methyl)1,1'-biphenyl-2-yl)-sulfonylbenzamide, is a potent, orally active, highly selective, nonpeptide angiotensin II (AII) receptor antagonist. MK-996 prevents the pressor response t
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