Zobrazeno 1 - 8
of 8
pro vyhledávání: '"Jeff Tillett"'
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:2191-2194
Piperidine, pyrrolidine, and azetidine sulfonamides were examined as linkers in designing novel human beta(3) adrenergic receptor (beta(3)-AR) agonists. The azetidine derivative 37, and piperidine derivatives 7, 8, and 13 were found to be potent beta
Autor:
Rebecca Cowling, Michele A. Sharr, Jerauld S. Skotnicki, Zhang Bao Xu, Venkatesan Aranapakam, Vincent Sandanayaka, G. Jin, Arie Zask, Mila Du, John W. Ellingboe, Joseph Mcdevitt, Jannie Lea Baker, Jeff Tillett, Loran M. Killar, Jamie Marie Davis, Thomas Walter, Weiguang Zhao, Amy Sung, George Theodore Grosu, John F. DiJoseph, Levin Jeremy Ian
Publikováno v:
Journal of Medicinal Chemistry. 46:2376-2396
The matrix metalloproteinases (MMPs) are a family of zinc-containing endopeptidases that play a key role in both physiological and pathological tissue degradation. In our preceding paper, we have reported on a series of novel and orally active N-hydr
Autor:
Jeff Tillett, Ruth Mulvey, Alexander Oliphant, Elwood Largis, John W. Ellingboe, Fuk-Wah Sum, Baihua Hu, Stella Han
Publikováno v:
Journal of Medicinal Chemistry. 44:1456-1466
In search of potent and selective human beta(3) agonists as potential drugs for the treatment of human obesity and type II diabetes, a series of (4-piperidin-1-yl)phenyl amides was prepared and evaluated for their biological activity on the human bet
Autor:
Elwood Largis, Michael S. Malamas, Baihua Hu, Ruth Mulvey, John W. Ellingboe, Stella Han, Jeff Tillett
Publikováno v:
ChemInform. 32
As part of our investigation into the development of potent and selective human β 3 agonists, a series of thiazolidinedione analogues was prepared and evaluated for their biological activity on the human β 3 -adrenergic receptor. The oxadiazolidine
Autor:
James K. Hennan, Richard K. Harrison, Belew Mekonnen, Larocque James Paul, Jeff Tillett, Manoj Samuel, Jeff W. Paslay, Veronica Soloveva, Kun Liu
Publikováno v:
Journal of biomolecular screening. 15(2)
Voltage-gated K(+) channels are potential drug targets for an increasing number of disease indications. Searching for compounds that modulate K(+) channel activities by high-throughput screening (HTS) is becoming a standard approach in the drug disco
Autor:
John W. Ellingboe, Kitae Lim, Stella Han, Jeffrey C. Pelletier, Jeff Tillett, Thiruvikraman Singanallore, Chuansheng Niu, Alexander Oliphant, Michael S. Malamas, Victoria Wong, Elwood Largis, Ruth Mulvey, Fuk-Wah Sum, Baihua Hu
Publikováno v:
Bioorganicmedicinal chemistry. 9(8)
A series of novel (4-piperidin-1-yl)-phenyl sulfonamides was prepared and evaluated for their biological activity on the human beta(3)-adrenergic receptor (AR). Replacement of the 3,4-dihydroxyl group of the catechol moiety with 4-hydroxyl-3-methyl s
Autor:
John W. Ellingboe, Ruth Mulvey, Stella Han, Elwood Largis, Michael S. Malamas, Baihua Hu, Jeff Tillett
Publikováno v:
Bioorganicmedicinal chemistry letters. 11(8)
As part of our investigation into the development of potent and selective human β 3 agonists, a series of thiazolidinedione analogues was prepared and evaluated for their biological activity on the human β 3 -adrenergic receptor. The oxadiazolidine
Autor:
Fuk-Wah Sum, Ruth Mulvey, Victoria D. Wong, Stella Han, Alexander Oliphant, Baihua Hu, Iwan Gunawan, Michael S. Malamas, John W. Ellingboe, Elwood Largis, Zenan Li, Jeff Tillett
Publikováno v:
Bioorganicmedicinal chemistry letters. 11(6)
Methylsulfonamide substituted 2,4-thiazolidinedione 22c is a potent (EC50=0.01 microM, IA=1.19) and selective (more than 110-fold over beta1 and beta2 agonist activity) beta3 agonist. This compound has also been proven to be active and selective in a