Zobrazeno 1 - 10
of 26
pro vyhledávání: '"Robert A. Conradi"'
Autor:
Brian J. Stockman, Terrence A. Scahill, Philip S. Burton, Robert A. Conradi, Jay T. Goodwin, James R. Blinn, David A. Kloosterman
Publikováno v:
Biopolymers. 53:396-410
Efficient transport of intact drug (solute) across the intestinal epithelium is typically a requirement for good oral activity. In general, the membrane permeability of a solute is a complex function of its size, lipophilicity, hydrogen bond potentia
Publikováno v:
The Journal of Peptide Research. 53:355-369
The therapeutic efficacy of an orally administered drug is dictated not only by its pharmacological properties such as potency and selectivity, but also its pharmacokinetic properties such as its access to the site of activity. Thorough evaluation of
Autor:
Ford Charles W, Robert A. Conradi, Jenifer L. Adamski, Randy M. Jensen, Debra A. Allwine, Barbachyn Michael R, John A. Tucker, Gary E. Zurenko, Jennifer L. Klock, Hutchinson Douglas K, Steven J. Brickner, Phillip S. Burton, Kevin C. Grega
Publikováno v:
Journal of Medicinal Chemistry. 41:3727-3735
Oxazolidinones are a novel class of synthetic antibacterial agents active against gram-positive organisms including methicillin-resistant Staphylococcus aureus as well as selected anaerobic organisms. Important representatives of this class include t
Publikováno v:
Advanced Drug Delivery Reviews. 23:143-156
Cellular efflux pathways function to remove both endogenous and exogenous substances from the cell. In the case of a polarized cellular barrier, such as the epithelium, these pathways serve an excretory or secretory role in transporting solutes out o
Publikováno v:
QSAR & Combinatorial Science. 13:4-10
In the search for a better model of the rate limiting processes in peptide transport we studied the partitioning of solutes between heptane and ethylene glycol. Methods for determining the log partition coefficient (logPH/G) in this solvent system we
Publikováno v:
Journal of Drug Targeting. 2:167-171
The influence of the aminoterminal substituent in a homologous series of tetrapeptide analogs on transport across Caco-2 cell monolayers was studied. In a series of pyridylcarboxamide regioisomers, the 2-pyridyl isomer was significantly more permeabl
Autor:
W. J. Howe, W. T. Lowther, J. O. Hui, W. G. Tarpley, D. E. Emmert, Chetana Rao, A G Tomasselli, John H. Kinner, V. S. Bradford, D. L. Alexander, Tomi K. Sawyer, B.M. Dunna, Robert A. Conradi, D. L. Decamp, Clark W. Smith, Allen W. Harrison, Charles S. Craik, James Michael Tustin, T. J. Mcquade, Robert L. Heinrikson, Y. Z. Zhang, Philip S. Burton, Jed F. Fisher, Roger A. Poorman, Joseph B. Moon, Jackson B. Hester, D J Staples, L. Liu, P. E. Scarborough, Maggiora Linda Louise
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 3:819-824
The structure-activity relationships and pharmacophore modeling aspects of a series of HIV PR inhibitors modified at the N- and/or C-terminus of the dipeptide isostere ChaΨ[CH(OH)CH2]Val (Cha, cyclohexylalanine) are reported. The HIV PR binding affi
Autor:
W. J. Howe, W. T. Lowther, A G Tomasselli, D. E. Emmert, D J Staples, Jackson B. Hester, W. G. Tarpley, J. O. Hui, Ben M. Dunn, John H. Kinner, Robert L. Heinrikson, Y. Z. Zhang, Tomi K. Sawyer, Charles S. Craik, D. L. Decamp, James Michael Tustin, T. J. Mcquade, D. L. Alexander, Allen W. Harrison, P. E. Scarborough, Robert A. Conradi, Jed F. Fisher, Roger A. Poorman, Philip S. Burton, Maggiora Linda Louise, V. S. Bradford, Joseph B. Moon, L. Liu, Clark W. Smith, Chetana Rao
Publikováno v:
ChemInform. 26
Publikováno v:
Journal of Controlled Release. 19:87-97
The successful development of orally bioavailable peptides and peptide-like substances as therapeutic agents will require an understanding of how structure influences absorption across the intestinal mucosa. In an attempt to define such relationships
Publikováno v:
Pharmaceutical Research. :435-439
In order to study the influence of hydrogen bonding in the amide backbone of a peptide on permeability across a cell membrane, a series of tetrapeptide analogues was prepared from D-phenylalanine. The amide nitrogens in the parent oligomer were seque