Zobrazeno 1 - 10
of 13
pro vyhledávání: '"Robert J. Bendesky"'
Autor:
Robert L. Hudkins, Joanne R. Mathiasen, Reddeppa reddy Dandu, Lisa D. Aimone, Rita Raddatz, Val R. Marcy, Greg A. Hostetler, John A. Gruner, Caitlyn Benfield, Robert J. Bendesky
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:6362-6365
A series of pyridazinone-phenethylamine derivatives with moderate to low nanomolar affinity for rat and human H(3)R are described. These analogs exhibited excellent selectivity and metabolic stability, with acceptable rat pharmacokinetic properties.
Autor:
Kurt A. Josef, Allison L. Zulli, Lisa D. Aimone, Derek Dunn, Rita Raddatz, Jacquelyn A. Lyons, Ming Tao, Joanne R. Mathiasen, Reddeppa reddy Dandu, Thomas R. Bailey, Val R. Marcy, Babu G. Sundar, John A. Gruner, Edward R. Bacon, Robert L. Hudkins, Robert J. Bendesky, Yin-Guo Lin
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:5493-5497
H3R structure–activity relationships on a novel class of pyridazin-3-one H3R antagonists/inverse agonists are disclosed. Modifications of the pyridazinone core, central phenyl ring and linker led to the identification of molecules with excellent ta
Autor:
Robert J. Bendesky, Wai C. Wong, Theodore P. Broten, Fengqi Zhang, Dake Tian, Carlos Forray, James Fang, Sriram Tyagarajan, Dhanapalan Nagarathnam, and Kamlesh P. Vyas, Shou Wu Miao, George Chiu, Mohammad R. Marzabadi, T. G. Murali Dhar, Charles Gluchowski, Kathryn Schneck, Paul J. Kling, Raymond S.L. Chang, Bharat Lagu, Jack Zhang, Wanying Sun, Stacey O'Malley, Tsing B. Chen, Richard W. Ransom, Terry W. Schorn, Charles M. Harrell, John M. Wetzel
Publikováno v:
Journal of Medicinal Chemistry. 42:4764-4777
Dihydropyrimidinones such as compound 12 exhibited high binding affinity and subtype selectivity for the cloned human alpha(1a) receptor. Systematic modifications of 12 led to identification of highly potent and subtype-selective compounds such as (+
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:
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:
Robert L, Hudkins, Lisa D, Aimone, Thomas R, Bailey, Robert J, Bendesky, Reddeppa Reddy, Dandu, Derek, Dunn, John A, Gruner, Kurt A, Josef, Yin-Guo, Lin, Jacquelyn, Lyons, Val R, Marcy, Joanne R, Mathiasen, Babu G, Sundar, Ming, Tao, Allison L, Zulli, Rita, Raddatz, Edward R, Bacon
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(18)
H(3)R structure-activity relationships on a novel class of pyridazin-3-one H(3)R antagonists/inverse agonists are disclosed. Modifications of the pyridazinone core, central phenyl ring and linker led to the identification of molecules with excellent
Autor:
Mangeng Cheng, Lisa D. Aimone, Sheila J. Miknyoczki, Robert J. Bendesky, Thelma S. Angeles, Jie Qian, Robert L. Hudkins, Bruce D. Dorsey, Jean Husten, Bruce Ruggeri, Thomas Conners, Seetha Murthy, Hong Chang, Amy J. Landis, Jennifer Grobelny, Mark A. Ator
Publikováno v:
Molecular Cancer Therapeutics. 12:C275-C275
The oncogenic receptor tyrosine kinases AXL and c-Met are over-expressed and constitutively activated in a variety of human cancers. Activation of these receptors contributes to multiple steps in tumor progression by promoting cancer cell migration a
Autor:
Bharat Lagu, Mohammad R. Marzabadi, Wanying Sun, John D. Gilbert, Douglas J. Pettibone, Sriram Tyagarajan, Robert J. Bendesky, T. G. Murali Dhar, Michael A. Patane, Theodore P. Broten, Dhanapalan Nagarathnam, Mark G. Bock, S. S. O'malley, and Roger M. Freidinger, Fengqi Zhang, George Chiu, Shou Wu Miao, Tsing Bao Chen, Jack Zhang, Kanyin Zhang, Kamlesh P. Vyas, Terry W. Schorn, Dake Tian, John M. Wetzel, Quanrong Shen, Kathryn Schneck, Charles M. Harrell, Charles Gluchowski, Wai C. Wong, Richard W. Ransom, Carlos Forray, Raymond S.L. Chang
Publikováno v:
Journal of medicinal chemistry. 42(23)
We have previously described compound 1a as a high-affinity subtype selective alpha(1a) antagonist. In vitro and in vivo evaluation of compound 1a showed its major metabolite to be a mu-opioid agonist, 4-methoxycarbonyl-4-phenylpiperidine (3). Severa
Autor:
William J. Greenlee, Salah D. Kivlighn, Deborah Ondeyka, Peter K. S. Siegl, Victor J. Lotti, Raymond S.L. Chang, Stacey O'Malley, Paul J. Kling, Tsing-Bau Chen, Robert J. Bendesky, Nathan B. Mantlo
Publikováno v:
European journal of pharmacology. 294(2-3)
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]pyridine) inhibited specific 125I-[Sar1, Ile8]angiotensin II binding to angiotensin AT1 receptor (Ki = 0.
Autor:
Gregory E. Martin, Robert J. Bendesky
Publikováno v:
Neuroscience Letters. 27:37-40
Data are reported to support the hypothesis that kojic amine is a GABA agonist in an in vivo model of GABAergic activity. The unilateral intranigral microinjection of kojic amine elicited dose-related turning contraversive from the injection site. Th