Zobrazeno 1 - 10
of 12
pro vyhledávání: '"Michelle B. Ayer"'
Autor:
Dan A. Ostlind, Marlene D. Drag, Matthew J. Wyvratt, Pierre deMontigny, David W. Fink, Steven L. Colletti, Wesley L. Shoop, Michelle B. Ayer, Chunshi Li, Steve Salva, Michelle Zakson, Lynn M. Warmke, Peter T. Meinke, Thomas L. Shih, Dong Ok, Michael H. Fisher, B.F. Michael, Dennis M. Schmatz, Julie Lim
Publikováno v:
Journal of Medicinal Chemistry. 52:3505-3515
Nodulisporic acid A (1) is a structurally complex fungal metabolite that exhibits systemic efficacy against fleas via modulation of an invertebrate specific glutamate-gated ion channel. In order to identify a nodulisporamide suitable for monthly oral
Autor:
Peter T. Meinke, Dennis M. Schmatz, L.M. Gregory, Steven L. Colletti, Prasun K. Chakravarty, Steve Salva, Matthew J. Wyvratt, Wesley L. Shoop, Michelle B. Ayer, Chunshi Li, Thomas L. Shih, Michelle Zakson-Aiken, Dong Ok, Michael H. Fisher
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 12:1751-1754
A series of new, diene-modified nodulisporic acid analogues ( 2 ) bearing diverse functionality at the 3″- and 4″-sites was efficiently prepared from the 3″-aldehyde 3 . Biological evaluation of these synthetic nodulisporic acid analogues for s
Autor:
Michelle B. Ayer, Chunshi Li, Anne Gurnett, Michael H. Fisher, Steven L. Colletti, Dennis M. Schmatz, Matthew J. Wyvratt, Paula M. Dulski, Peter T. Meinke, Julie Lim, Tami Crumley, Stefan Galuska, John J. Allocco, Sandra J. Darkin-Rattray, Christine Lange Cannova, Robert W. Myers
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 11:107-111
Apicidin, a natural product recently isolated at Merck, inhibits both mammalian and protozoan histone deacetylases (HDACs). The conversion of apicidin, a nanomolar inhibitor of HDACs, into a series of side-chain analogues that display picomolar enzym
Autor:
Robert W. Myers, Matthew J. Wyvratt, Peter T. Meinke, Steven L. Colletti, Sandra J. Darkin-Rattray, Michael H. Fisher, Dennis M. Schmatz, Michelle B. Ayer
Publikováno v:
Tetrahedron Letters. 41:7831-7835
An efficient degradation of apicidin's ketone-containing side chain to two common intermediates (the C7-aldehyde and the C8-methyl ester) is described. From these intermediates, a series of potent mechanism-based histone deacetylase inhibitors was pr
Autor:
Dennis M. Schmatz, Steven L. Colletti, Julie Lim, Peter T. Meinke, Lynn M. Warmke, Wesley L. Shoop, Steve Salva, Thomas L. Shih, Matthew J. Wyvratt, Michelle B. Ayer, Chunshi Li, Michelle Zakson-Aiken, Dong Ok, Michael H. Fisher
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 10:2371-2374
Medicinal chemistry efforts were initiated to identify the key constituents of the nodulisporic acid A (1) pharmacophore that are integral to its potent insecticidal activity. New semisynthetic derivatives delineated 1 into 'permissive' and 'nonpermi
Autor:
James P. Springer, Bernard K. Choi, S J Siciliano, Michelle B. Ayer, Robert E. Schwartz, Jesús Martín
Publikováno v:
Combinatorial chemistryhigh throughput screening. 8(6)
An approach to rapidly process and interpret high-throughput liquid chromatography mass spectrometry data is presented. This approach applies an in-house developed computer application to process LC-MS report files containing spectral and chromatogra
Autor:
Prasun K. Chakravarty, Steven L. Colletti, Howard C. H. Kuo, Christine Snedden, Michelle B. Ayer, L.M. Gregory, Michael H. Fisher, Wesley L. Shoop, Matthew J. Wyvratt, Michelle Zakson-Aiken, Peter T. Meinke, Thomas L. Shih, Dennis M. Schmatz, Sriram Tyagarajan
Publikováno v:
Bioorganicmedicinal chemistry letters. 13(1)
Efficient routes to access the 2", 3", 4", and 6" registers of the nodulisporic acid (NsA) side chain are disclosed. A mild one-carbon, Ph(2)CdoublebondNCH(2)CtriplebondN mediated homologation of NsA's 3"-aldehyde permitted access to the 4"-register.
Autor:
Dennis C. Dean, Michael A. Wallace, Marjorie A. Egan, Vivien A. Warren, Michelle B. Ayer, Doris F. Cully, Peter T. Meinke, David C. Hunt, McHardy M. Smith, Steven W. Ludmerer, Brande S. Williams, Maria L. Garcia, Yingcong Zheng, Ashok Chaudhary
Publikováno v:
Biochemistry. 41(20)
35S-labeled derivatives of the insecticides nodulisporic acid and ivermectin were synthesized and demonstrated to bind with high affinity to a population of receptors in Drosophila head membranes that were previously shown to be associated with a glu
Autor:
Michelle B. Ayer, Chunshi Li, Sandra J. Darkin-Rattray, Paula M. Dulski, Christine Lange Cannova, Dennis M. Schmatz, Matthew J. Wyvratt, Julie Lim, Michael H. Fisher, Anne Gurnett, Tami Crumley, Stefan Galuska, John J. Allocco, Peter T. Meinke, Robert W. Myers, Steven L. Colletti
Publikováno v:
Bioorganicmedicinal chemistry letters. 11(2)
Recently isolated at Merck, apicidin inhibits both mammalian and protozoan histone deacetylases (HDACs). The conversion of apicidin, a nonselective nanomolar inhibitor of HDACs, into a series of picomolar indole-modified and parasite-selective trypto
Autor:
Steven L. Colletti, Michael H. Fisher, Peter T. Meinke, Matthew J. Wyvratt, Dennis M. Schmatz, Michelle B. Ayer, Sandra J. Darkin-Rattray, Robert W. Myers
Publikováno v:
ChemInform. 31
An efficient degradation of apicidin's ketone-containing side chain to two common intermediates (the C7-aldehyde and the C8-methyl ester) is described. From these intermediates, a series of potent mechanism-based histone deacetylase inhibitors was pr