Zobrazeno 1 - 10
of 14
pro vyhledávání: '"Dennis V. Nazareno"'
Autor:
Marc A. Labroli, Geoffrey B. Varty, Dennis V. Nazareno, Stuart W. McCombie, Steensma Ruo, Julie M. Strizki, Bahige M. Baroudy, Jayaram R. Tagat, Kathleen Cox, Robert W. Watkins, Jean E. Lachowicz, Yushi Xiao
Publikováno v:
Journal of Medicinal Chemistry. 47:2405-2408
The nature and the size of the benzylic substituent are shown to be the key to controlling receptor selectivity (CCR5 vs M1, M2) and potency in the title compounds. Optimization of the lead benzylic methyl compound 3 led to the methoxymethyl analogue
Autor:
Michael G. Murray, Bernard R. Neustadt, Julie M. Strizki, Sue-Ing Lin, Nicole Vantuno, Lisa Wojcik, Jayaram R. Tagat, Kathleen Cox, and Bahige M. Baroudy, Steensma Ruo, Dennis V. Nazareno, Stuart W. McCombie, Serena Xu
Publikováno v:
Journal of Medicinal Chemistry. 44:3343-3346
Truncation of the original piperidino-2(S)-methyl piperazine lead structure 2, from a family of muscarinic antagonists, gave compound 8 which has improved selectivity for the HIV-1 co-receptor CCR5 over muscarinic receptors. Further optimization for
Autor:
Dennis V. Nazareno, Guowei Zhou, Herbert Binch, William J. Greenlee, Mary Cohen-Williams, Jayaram R. Tagat, Diane E. Grotz, Jean E. Lachowicz, James J. Kaminski, Joseph A. Kozlowski, Gordon Crosby, Stuart W. McCombie, Vicki L. Coffin, Kathleen Cox, Vilma Ruperto, Craig D. Boyle, Samuel Chackalamannil, Ruth A. Duffy, Hubert B. Josien, Yuguang Wang, John W. Clader, William Billard
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 11:2311-2314
The potential toxicological liabilities of the M(2) muscarinic antagonist 1 were addressed by replacing the methylenedioxyphenyl moiety with a p-methoxyphenyl group, resulting in M(2) selective compounds such as 3. Several halogenated naphthamide der
Autor:
Dennis V. Nazareno, Stuart W. McCombie, Bahige M. Baroudy, Jayaram R. Tagat, Steensma Ruo, Serena Xu, Sue-Ing Lin, Nicole Vantuno, Jia Liu
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 11:2143-2146
Optimization of the piperidino-piperazines 1 and 2 provided early leads 3 and 4, which showed good activity in the CCR5–RANTES binding assay and in antiviral assays. A systematic study around these structures showed that the 2(S)-methyl piperazine
Autor:
Thomas A. Bara, Hubert B. Josien, Anandan Palani, Stuart W. McCombie, Dennis V. Nazareno, Annette Bauer, Jennifer Ford, Vice Susan F, Jayaram R. Tagat, Michael W. Miller, C A Evans
Publikováno v:
The Journal of Organic Chemistry. 66:2487-2492
Autor:
Beverly E. Barton, Stuart W. McCombie, Jayaram R. Tagat, Jennifer Shortall, Dennis V. Nazareno, James V. Jackson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 5:2139-2142
A versatile synthetic route to the title class of compounds and the development of an orally absorbed analogue of the lead structure are described. The minimum structural requirements needed in the compounds related to 1 for the inhibition of interle
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 4:1101-1104
Dehydroabietic acid 5 was converted to the exocyclic olefin 7 by applying the Barton decarboxylation protocol. The latter served as key intermediate for the stereoselective synthesis of a variety of ring-A functionalized derivatives. Compounds 13 and
Autor:
Dennis V. Nazareno, Stuart W. McCombie, Bandarpalle B. Shankar, William A. Metz, Jayaram R. Tagat
Publikováno v:
ChemInform. 22
Treatment of 2-[(dimethylamino) methylene]-3-oxobutanoates 9 or 10 with LiN(SiMe 3 ) 2 in the presence of RCOCl results in C-acylation. The resulting intermediate, without isolation, may be converted to 6-R-3-Carbethoxy-4-pyrones (e.g., 12) by H 3 O
Publikováno v:
ChemInform. 25
Autor:
Sue-Ing Lin, Dennis V. Nazareno, Jia Liu, Serena Xu, Jayaram R. Tagat, Nicole Vantuno, Steensma Ruo, Bahige M. Baroudy, Stuart W. McCombie
Publikováno v:
ChemInform. 32