Zobrazeno 1 - 8
of 8
pro vyhledávání: '"Francis A. Mennona"'
Autor:
Karin Conde-Knape, Yonglin Ren, Irina Hakimi, Paul Gillespie, Jefferson Wright Tilley, Sung-Sau So, Shawn David Erickson, Fiorenza Falcioni, Francis A. Mennona, Yimin Qian, Hamid Salari
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:4216-4220
Benzimidazole and indane are the two key fragments in our potent and selective MCH-1 receptor (MCHR1) antagonists. To identify novel linkers connecting the two fragments, we investigated diamino-cycloalkane-derived analogs and discovered highly poten
Autor:
Dorota Miklowski, Richard V. Trilles, Robert William Guthrie, Karen Rowan, Gerry Kaplan, Nicolas Huby, Barry A. Wolitzky, Jefferson Wright Tilley, Virginia Schwinge, Francis A. Mennona, Tai-Nan Huang, Li Chen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 10:729-733
A series of N-(N-benzylpyroglutamyl)-4-substituted-L-phenylalanine derivatives was prepared as VLA-4/VCAM antagonists. Analogues substituted by electron deficient benzoylamino groups bearing bulky ortho substituents had low-nM potency in an ELISA ass
Autor:
Joseph Grimsby, Wanping Geng, Navita L. Mallalieu, Mark T. Dvorozniak, Wendy Lea Corbett, Nancy-Ellen Haynes, Jagdish Kumar Racha, Yimin Qian, David J Moore, Kevin Richard Guertin, Nathan Robert Scott, Robert Francis Kester, Steven Joseph Berthel, Roumen Nikolaev Radinov, Francis A. Mennona, Ramakanth Sarabu, Duk Soon Choi, Paul Gillespie
Publikováno v:
ACS medicinal chemistry letters. 4(4)
To resolve the metabolite redox cycling associated with our earlier clinical compound 2, we carried out lead optimization of lead molecule 1. Compound 4 showed improved lipophilic ligand efficiency and demonstrated robust glucose lowering in diet-ind
Autor:
Rebecca Taub, Karin Conde-Knape, Lucy Orzechowski, Warren McComas, Chun Ma, Bruce L. Banner, Fiorenza Falcioni, Steven Gregory Mischke, Irina Hakimi, John P. Tengi, Hong Wang, Robert Francis Kester, Kyungjin Kim, Kshitij Chhabilbhai Thakkar, Francis A. Mennona, Bernard Michael Hennessy, Yimin Qian, Hamid Salari, Steven Joseph Berthel, Jefferson Wright Tilley, Shawn David Erickson
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(4)
This paper describes the lead optimization of a new series of potent, selective, orally bioavailable, brain-penetrant MCH-1 receptor antagonists. A major focus of the work was to achieve a selectivity profile appropriate for in vivo efficacy studies
Autor:
Mullin John Guilfoyle, Herman J. Crowley, Robert William Guthrie, L. C. Blaber, A. Faraone, B. Simko, Francis A. Mennona, R. W. Kierstead
Publikováno v:
Journal of Medicinal Chemistry. 26:1561-1569
A series of binary (aryloxy)propanolamines has been prepared and examined in vitro and in vivo for beta-adrenoreceptor blocking activity. These symmetrical compounds consist of two (S)-(phenyloxy)propanolamine pharmacophores coupled through alkylened
Autor:
Francis A. Mennona, Alfred Boris, Richard W. Kierstead, Robert William Guthrie, Mullin John Guilfoyle
Publikováno v:
Journal of Medicinal Chemistry. 16:257-262
Autor:
Robert W. Guthrie, Arnold Brossi, Francis A. Mennona, John G. Mullin, Richard W. Kierstead, E. Grunberg
Publikováno v:
Journal of medicinal chemistry. 18(7)
Several acyloxy and alkyl derivatives of ellipticine have been prepared. In addition, a modified synthesis leading to the hitherto unobtainable 8,9-dimethoxy- and 8,9-methylenedioxyellipticines is described. Some of the derivatives described herein e
Autor:
Alfred Boris, Robert William Guthrie, Francis A. Mennona, Richard W. Kierstead, Mullin John Guilfoyle
Publikováno v:
Journal of medicinal chemistry. 16(1)