Zobrazeno 1 - 10
of 51
pro vyhledávání: '"Neli Melman"'
Autor:
Yong-Chul, Kim, Yishai, Karton, Xiao-Duo, Ji, Neli, Melman, Joel, Linden, Kenneth A, Jacobson
Publikováno v:
Drug development research. 47(4)
The structure-activity relationships (SAR) of 8-phenyl-1,3-dipropylxanthine derivatives in binding to recombinant human A
Publikováno v:
Biochemical Pharmacology. 65:1675-1684
The activation of the human A(3) adenosine receptor (AR) by a wide range of N(6)-substituted adenosine derivatives was studied in intact CHO cells stably expressing this receptor. Selectivity of binding at rat and human ARs was also determined. Among
Autor:
Seung Jin Lee, Moo Hong Lim, Joong Hyup Kim, Neli Melman, Moon Woo Chun, Hea Ok Kim, Kenneth A. Jacobson, Lak Shin Jeong, Zhan Guo Gao, Hyung Ryong Moon
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:817-820
Several 3′-fluoro analogues, 1a , 1b , and 1c of selective and potent adenosine A 3 receptor agonist, Cl-IB-MECA were synthesized from d -xylose via highly regioselective opening of lyxo -epoxides, 8a and 8b with fluoride anion. Compared to the hig
Autor:
Seong Gon Kim, Adriaan P. IJzerman, Neli Melman, Andreas A. Erdmann, Christa E. Müller, Kenneth A. Jacobson, Zhan-Guo Gao
Publikováno v:
Biochem Pharmacol
The diuretic drug amiloride and its analogues were found previously to be allosteric modulators of antagonist binding to A(2A) adenosine receptors. In this study, the possibility of the allosteric modulation by amiloride analogues of antagonist bindi
Autor:
Joel Linden, Neli Melman, Kenneth A. Jacobson, Hak Sung Kim, Soon-Ai Kim, Christa E. Müller, Melissa A. Marshall
Publikováno v:
Journal of Medicinal Chemistry. 45:2131-2138
In the search for improved selective antagonist ligands of the A(2B) adenosine receptor, which have the potential as antiasthmatic or antidiabetic drugs, we have synthesized and screened a variety of alkylxanthine derivatives substituted at the 1-, 3
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 10:31-34
Pharmacophore queries from previously known potent selective A3 antagonists were generated by Chem-X. These queries were used to search a pharmacophore database of diverse compounds (CNS-SetTM). In vitro assays of 186 ‘hits’ yielded over 30 activ
Publikováno v:
Drug Development Research. 48:171-177
[Table: see text] A3 adenosine receptor antagonists have potential as anti-inflammatory, anti-asthmatic, and anti-ischemic agents. We previously reported the preparation of chemical libraries of 1,4-dihydropyridine (DHP) and pyridine derivatives and
Autor:
Rongyuan Xie, Neli Melman, Kenneth A. Jacobson, An-Hu Li, Xiao-duo Ji, Mark E. Olah, Gary L. Stiles
Publikováno v:
Journal of Medicinal Chemistry. 42:4232-4238
A(3) adenosine receptor antagonists are sought for their potential antiinflammatory, antiasthmatic, and antiischemic properties. We have found that 3,5-diacyl-1,2,4-trialkyl-6-phenylpyridinium derivatives constitute a novel class of selective A(3) ad
Publikováno v:
Drug Development Research. 47:178-188
The structure–activity relationships (SAR) of 8-phenyl-1,3-dipropylxanthine derivatives in binding to recombinant human A2B adenosine receptors were explored, in order to identify selective antagonists. Based on the finding of receptor selectivity
Autor:
Ji-Long Jiang, Jon C. Clardy, Louis Chang, Emil B. Lobkovsky, Kenneth A. Jacobson, Xiao-duo Ji, An-Hu Li, Stefano Moro, Soo-Yeon Jang, Neli Melman
Publikováno v:
Journal of Medicinal Chemistry. 42:3055-3065
Racemic 6-phenyl-4-phenylethynyl-1,4-dihydropyridine derivatives have been shown to be highly selective A(3) adenosine receptor antagonists (Jiang et al. J. Med. Chem. 1997, 40, 2596-2608). Methods for resolving the optical isomers at the C4 position