Zobrazeno 1 - 10
of 14
pro vyhledávání: '"Clara I. Villamil"'
Autor:
Cele Abad-Zapatero, Anil Vasudevan, Clara I. Villamil, Kent D. Stewart, Tetsuro Oie, Mary K. Verzal, Stevan W. Djuric
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:4502-4505
The design and synthesis of indazolinone containing kinase inhibitors are reported. Regioisomers that showed profound potency variation in previously-reported isoindolinone and aminoindazole systems were surprisingly found to have similar potencies i
Publikováno v:
Tetrahedron. 55:11787-11802
A racemic synthesis of azanoradamantane (±) -3 was accomplished via Yamamoto's MAD-catalyzed Diels-Alder protocol. Subsequently, a scalable asymmetric synthesis of azanoradamantane benzamide SC-52491 was carried out employing Helmchen's asymmetric D
Autor:
Dai-Chang Yang, G. W. Gullikson, Daniel L. Flynn, Daniel P. Becker, Clara I. Villamil, Roger Nosal, Chafiq Moummi
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 7:2149-2154
A series of meso-amino(methyl)azanoradamantane benzamides has been prepared and evaluated for 5-HT4 agonism activity in the rat tunica muscularis mucosae (TMM) assay. Compound 8i is the most potent 5-HT4 agonist in the series, with an EC50 of 217 nM.
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:3073-3075
Pyrrolizidine benzamide (+/-)-2, the bridgehead-methyl analog of SC-53116, was prepared and evaluated for 5-HT(4) agonism activity in the rat tunica muscularis (TMM) mucosae assay. Compound (+/-)-2 has an EC(50) of 449 nM in the TMM assay, as compare
Autor:
Karl J. Mathis, Madeleine H. Li, Alan M. Easton, Clara I. Villamil, Barta Thomas E, Grace E. Munie, Daniel P. Becker, Jennifer M. Williams, James R. Kiefer, Louis J. Bedell, Rico Joseph G, Susan L. Hockerman
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(10)
Seeking compounds preferentially potent and selective for MMP-13, we reported in the preceding Letter on a series of hydroxamic acids with a flexible benzamide tail groups.(1a) Here, we replace the amide moiety with non-hydrolyzable heterocycles in a
Autor:
Chris P. Carron, Madeleine H. Li, Daniel P. Becker, T. Sunyer, John N. Freskos, Louis J. Bedell, Boehm Terri L, Chris L. Funckes-Shippy, Decrescenzo Gary A, Clara I. Villamil, Joseph J. McDonald, Grace E. Munie, Jeffery N. Carroll, Pramod P. Mehta, Jun Yao, Brian R. Bond, Craig Swearingen, Jennifer M. Williams, Barta Thomas E, Marcia I. Heron, Dean Welsch, Karl J. Mathis, Carol Pearcy Howard, James R. Kiefer, Susan L. Hockerman, Alan M. Easton, Ying Yu
Publikováno v:
Journal of medicinal chemistry. 53(18)
α-Sulfone-α-piperidine and α-tetrahydropyranyl hydroxamates were explored that are potent inhibitors of MMP's-2, -9, and -13 that spare MMP-1, with oral efficacy in inhibiting tumor growth in mice and left-ventricular hypertrophy in rats and in th
Autor:
Dai-Chang Yang, Roger Nosal, Daniel L. Flynn, Clara I. Villamil, Chafiq Moummi, G. W. Gullikson, Daniel P. Becker
Publikováno v:
ChemInform. 29
A series of meso-amino(methyl)azanoradamantane benzamides has been prepared and evaluated for 5-HT4 agonism activity in the rat tunica muscularis mucosae (TMM) assay. Compound 8i is the most potent 5-HT4 agonist in the series, with an EC50 of 217 nM.
Autor:
Daniel L. Flynn, Chafiq Moummi, Dai-Chang Yang, Daniel P. Becker, G. W. Gullikson, Clara I. Villamil
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 2:1251-1256
A new series of cholecystokinin (CCK) antagonists are described which utilizes a new 1,3,4-trisubstituted pyrrolidinone as a scaffold for appending specific amino acid R group mimics (Figure 1). Compound 1A and 1E (SC-50998) exhibit potent nanomolar
Autor:
Daniel L. Flynn, Gary W. Gullikson, Roger Nosal, Dai C. Yang, Daniel Lamar Zabrowski, Daniel P. Becker, Chafiq Moummi, Clara I. Villamil
Publikováno v:
Journal of Medicinal Chemistry. 35:1486-1489
Autor:
Roger Nosal, Alan E. Moormann, Richard F. Loeffler, Daniel L. Flynn, Gary W. Gullikson, Clara I. Villamil, Daniel P. Becker, Chafiq Moummi, Dai-C Yang
Publikováno v:
Journal of medicinal chemistry. 49(3)
A series of pyrrolizidine esters, amides, and ureas was prepared and tested for 5-HT(4) and 5-HT(3) receptor binding, 5-HT(4) receptor agonism in the rat tunica muscularis mucosae (TMM) assay, and for 5-HT(3) receptor-mediated functional antagonism i