Results 171 to 180 of about 9,317 (205)

A_2B Adenosine Receptor Antagonists with Picomolar Potency

Journal of Medicinal Chemistry, 2019
The A2B adenosine receptor (A2BAR) was proposed as a novel target for the (immuno)therapy of cancer since A2BAR blockade results in antiproliferative, antiangiogenic, antimetastatic, and immunostimulatory effects. In this study, we explored the structure-activity relationships of xanthin-8-yl-benzenesulfonamides mainly by introducing a variety of ...
Jie Jiang, Catharina Julia Seel, Ahmed Temirak, Vigneshwaran Namasivayam, Antonella Arridu, Jakub Schabikowski, Younis Baqi, Sonja Hinz, Jörg Hockemeyer, Christa E. Müller   +9 more
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Discovery of oxazole-based PDE4 inhibitors with picomolar potency

Bioorganic & Medicinal Chemistry Letters, 2012
Optimization of oxazole-based PDE4 inhibitors has led to the discovery of a series of quinolyl oxazoles, with 4-benzylcarboxamide and 5-α-aminoethyl groups which exhibit picomolar potency against PDE4. Selectivity profiles and in vivo biological activity are also reported.
Rongze, Kuang, Ho-Jane, Shue, Li, Xiao, David J, Blythin, Neng-Yang, Shih, Xiao, Chen, Danlin, Gu, John, Schwerdt, Ling, Lin, Pauline C, Ting, Jianhua, Cao, Robert, Aslanian, John J, Piwinski, Daniel, Prelusky, Ping, Wu, Ji, Zhang, Xiang, Zhang, Chander S, Celly, Motasim, Billah, Peng, Wang   +19 more
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Discovery of CC Chemokine Receptor-3 (CCR3) Antagonists with Picomolar Potency

Journal of Medicinal Chemistry, 2005
Starting with our previously described(20) class of CC chemokine receptor-3 (CCR3) antagonist, we improved the potency by replacing the phenyl linker of 1 with a cyclohexyl linker and by replacing the 4-benzylpiperidine with a 3-benzylpiperidine. The resulting compound, 32, is a potent and selective antagonist of CCR3.
George V, De Lucca, Ui Tae, Kim, Brian J, Vargo, John V, Duncia, Joseph B, Santella, Daniel S, Gardner, Changsheng, Zheng, Ann, Liauw, Zhang, Wang, George, Emmett, Dean A, Wacker, Patricia K, Welch, Maryanne, Covington, Nicole C, Stowell, Eric A, Wadman, Anuk M, Das, Paul, Davies, Swamy, Yeleswaram, Danielle M, Graden, Kimberly A, Solomon, Robert C, Newton, George L, Trainor, Carl P, Decicco, Soo S, Ko   +23 more
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ChemInform Abstract: Discovery of Oxazole‐Based PDE4 Inhibitors with Picomolar Potency.

ChemInform, 2012
AbstractA series of quinolyloxazoles with 4‐benzylcarboxamide and 5‐α‐aminoethyl groups, which show picomolar potency against PDE4, is discovered.
Rongze Kuang, et al. et al.
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HIV protease inhibitors with picomolar potency against PI-Resistant HIV-1 by extension of the P3 substituent

Bioorganic & Medicinal Chemistry Letters, 2003
A biaryl pyridylfuran P(3) substituent on the hydroxyethylene isostere scaffold affords HIV protease inhibitors (PI's) with picomolar (IC(50)) potency against the protease enzymes from PI-resistant HIV-1 strains. Inclusion of a gem-dimethyl substituent afforded compound 3 with 100% oral bioavailability (dogs) and more than double the t(1/2) of ...
Joseph L, Duffy, Thomas A, Rano, Nancy J, Kevin, Kevin T, Chapman, William A, Schleif, David B, Olsen, Mark, Stahlhut, Carrie A, Rutkowski, Lawrence C, Kuo, Lixia, Jin, Jiunn H, Lin, Emilio A, Emini, James R, Tata   +12 more
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HIV-1 protease inhibitors with picomolar potency against PI-resistant HIV-1 by modification of the P1′ substituent

Bioorganic & Medicinal Chemistry Letters, 2003
Transposition of the pyridyl nitrogen from the P(3) substituent to the P(1)' substituent in HIV-1 protease inhibitors (PI) affords compounds such as 3 with an improved inhibitory profile against multiple P450 isoforms. These compounds also displayed increased potency, with 3 inhibiting viral spread (CIC(95)) at
Joseph L, Duffy, Brian A, Kirk, Nancy J, Kevin, Kevin T, Chapman, William A, Schleif, David B, Olsen, Mark, Stahlhut, Carrie A, Rutkowski, Lawrence C, Kuo, Lixia, Jin, Jiunn H, Lin, Emilio A, Emini, James R, Tata   +12 more
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Inhibition of gastric acid secretion by human calcitonin gene-related peptide with picomolar potency in guinea-pig parietal cell preparations

Biochemical and Biophysical Research Communications, 1987
The effect of CGRP on [14C]-aminopyrine accumulation in isolated parietal cell preparations from guinea-pig fundic mucosa was studied. Parietal cells consisted of 60% of the preparations. [14C]-Aminopyrine accumulation was used as an index of physiological response of parietal cells to secretagogues.
Y, Umeda, T, Okada
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6-Position optimization of tricyclic 4-quinolone-based inhibitors of glycogen synthase kinase-3β: Discovery of nitrile derivatives with picomolar potency

Bioorganic & Medicinal Chemistry Letters, 2012
We previously disclosed tricylic, 6-carboxylic acid-bearing 4-quinolones as GSK-3β inhibitors. Herein we discuss the optimization of this series to yield a series of more potent 6-nitrile analogs with insignificant anti-microbial activity. Finally, kinase profiling indicated that members of this class were highly specific GSK-3 inhibitors.
Bei, Li, Oana M, Cociorva, Tyzoon, Nomanbhoy, Qiang, Li, Kai, Nakamura, Masahiro, Nomura, Kyoko, Okada, Kazuhiro, Yumoto, Marek, Liyanage, Melissa C, Zhang, Arwin, Aban, Anna Katrin, Szardenings, John W, Kozarich, Yasushi, Kohno, Kevin R, Shreder   +14 more
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HIV Protease Inhibitors with Picomolar Potency Against PI‐Resistant HIV‐1 by Extension of the P₃ Substituent.

ChemInform, 2003
AbstractFor Abstract see ChemInform Abstract in Full Text.
Joseph L. Duffy, et al. et al.
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Synthesis and monoamine transporter affinity of new 2β-carbomethoxy-3β-[4-(substituted thiophenyl)]phenyltropanes: discovery of a selective SERT antagonist with picomolar potency

Bioorganic & Medicinal Chemistry Letters, 2005
AbstractFor Abstract see ChemInform Abstract in Full Text.
Gilles, Tamagnan, David, Alagille, Xing, Fu, Nora S, Kula, Ross J, Baldessarini, Robert B, Innis, Ronald M, Baldwin   +6 more
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