Zobrazeno 1 - 10
of 26
pro vyhledávání: '"Melissa S. Egbertson"'
Publikováno v:
Current Topics in Medicinal Chemistry. 7:1251-1272
Replication of the human immunodeficiency virus (HIV) is dependent upon the enzyme HIV integrase (IN), one of three essential enzymes encoded in the viral genome. HIV-1 IN catalyzes the insertion of the proviral DNA into the host genome (strand trans
Autor:
Thomayant Prueksaritanont, Jerome H. Hochman, Samuel L. Graham, Yuhsin Kuo, Joan D. Ellis, Maria S. Michener, Melissa S. Egbertson, Cuyue Tang, Nicole T. Pudvah, Jacquelynn J. Cook
Publikováno v:
Biochemical Pharmacology. 78:642-647
Brain penetration of drugs which are subject to P-glycoprotein (Pgp)-mediated efflux is attenuated, as manifested by the fact that the cerebrospinal fluid concentration ( C CSF ), a good surrogate of the unbound brain concentration ( C ub ), is lower
Publikováno v:
Synthetic Communications. 37:1887-1897
Practical syntheses of 4‐fluoro‐2‐(methylthio)benzylamine 1 and the corresponding 2‐methylsulfonyl analog 2 are reported. The methylthio moiety was introduced regioselectively by two methods. In the first method, metallation of 4‐fluoro‐2
Autor:
Gail Murphy, Joseph J. Lynch, Lawrence I. Deckelbaum, Frederick L. Sax and, George D. Hartman, Man-Wai Lo, Melissa S. Egbertson, Robert J. Gould, Eliav Barr, Wasyl Halczenko, Jacquelynn J. Cook, Bohumil Bednar, Mark E. Duggan
Publikováno v:
Cardiovascular Drug Reviews. 17:199-224
Autor:
Melissa S. Egbertson, Marc V. Witmer, Linghang Zhuang, James P. Guare, William A. Schleif, Abigail Wolfe, Payne Linda S, Peter J. Felock, Stuart R. Michelson, Daria J. Hazuda, Steven D. Young, John S. Wai, Joseph J. Lynch, Kara A. Stillmock, Joseph P. Vacca, Lori J. Gabryelski, Yvonne M. Leonard, Mark Embrey, Thorsten E. Fisher, Gregory Moyer
Publikováno v:
Journal of Medicinal Chemistry. 46:453-456
Naphthyridine 7 inhibits the strand transfer of the integration process catalyzed by integrase with an IC50 of 10 nM and inhibits 95% of the spread of HIV-1 infection in cell culture at 0.39 microM. It does not exhibit cytotoxicity in cell culture at
Autor:
Keith W. Rickert, Ming-Tain Lai, Daniel Riley, Melissa S. Egbertson, Mike T. Rudd, Kausik K. Nanda, Barbara Hanney, Shawn J. Stachel, Stephanie A. Kane, Jay A. Grobler, Ahren Iver Green, John M. Sanders, Christopher Daley, Paul Zuck, Vandna Munshi, Edward J. Brnardic, Kristen G. Jones, Darrell A. Henze, Alicja Krasowska-Zoladek, Hua-Poo Su, Mark T. Bilodeau, Yiwei Li, Dennis Murphy, Michael D. Leitl, Peter J. Manley
Publikováno v:
Journal of medicinal chemistry. 57(13)
We have identified several series of small molecule inhibitors of TrkA with unique binding modes. The starting leads were chosen to maximize the structural and binding mode diversity derived from a high throughput screen of our internal compound coll
Autor:
Bohumil Bednar, Patricia A. McQueney, Michael E. Cunningham, Rodney A. Bednar, B. C. Askew, George D. Hartman, Melissa S. Egbertson, Robert J. Gould
Publikováno v:
Cytometry. 28:58-65
Antagonists of platelet glycoprotein IIb/IIIa (GPIIb/IIIa) represent a new therapeutic approach in inhibiting platelet aggregation, thus providing a powerful form of antithrombotic therapy. The measurement of binding of arginine-glycine-aspartic acid
Autor:
R. J. Lynch, Rodney A. Bednar, Bohumil Bednar, Jacquelynn J. Cook, L.M. Vassallo, Marie A. Holahan, Stanley L. Gaul, Melissa S. Egbertson, Laura A. Libby, G. R. Sitko, Robert J. Gould, J.J. Lynch, George D. Hartman, Maria T. Stranieri
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 6:2519-2524
Potency enhancing features of two series of fibrinogen receptor antagonists were combined to give analogs with improved potency and oral activity. Antagonists containing either alkyl or aryl sulfonamides and a central isoindolinone structural constra
Autor:
Melissa S. Egbertson, Jeffrey A. Vivian, Vanita Puri, Jason M. Uslaner, Christopher E. Cannon, Donnie Eddins
Publikováno v:
Neuropharmacology. 64
The cognitive deficits associated with schizophrenia are recognized as a core component of the disorder, yet there remain no available therapeutics to treat these symptoms of the disease. As a result, there is a need for establishing predictive precl
Autor:
Robert J. Gould, Marie A. Holahan, J.J. Lynch, R. J. Lynch, Maria T. Stranieri, Melissa S. Egbertson, A.M. Naylor, George D. Hartman, Jacquelynn J. Cook, L.M. Vassallo
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 4:1835-1840
Analysis of platelet aggregation inhibition results and rotational isomer preferences has provided an understanding of inhibitory potency for m-phthalic acid analogs 7–7. Constraint of the N-terminal amide led to compound 9, which is potent, select