Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 3: SAR studies on the benzylpyrazole segment.
暂无分享,去创建一个
Karen Holmes | Kathy Lyons | Joseph Kessler | Anthony Carella | D. Hazuda | Michael D. Miller | W. Schleif | E. Emini | J. Lineberger | J. Demartino | K. Chapman | Michael D Miller | Sander G Mills | Martin S Springer | Julie A DeMartino | Janet Lineberger | L. Malkowitz | D. Shen | Dong-Ming Shen | A. Carella | Kevin T Chapman | Lorraine Malkowitz | M. Shu | J. Loebach | Kerry A Parker | S. Mills | M. Springer | S. Gould | S. Siciliano | J. D. Salvo | K. Lyons | J. Pivnichny | G. Kwei | G. Carver | K. Holmes | R. Danzeisen | J. Kessler | Min Shu | Jennifer L Loebach | Sandra L Gould | Salvatore J Siciliano | Jerry Di Salvo | James V Pivnichny | Gloria Y Kwei | Gwen Carver | William A Schleif | Renee Danzeisen | Daria Hazuda | Emilio A Emini | M. Miller | Michael D. Miller | J. DeMartino
[1] D. Hazuda,et al. Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 2: Discovery of potent, selective, and orally bioavailable compounds. , 2004, Bioorganic & medicinal chemistry letters.
[2] Karen Holmes,et al. Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 1: Discovery and SAR study of 4-pyrazolylpiperidine side chains. , 2004, Bioorganic & medicinal chemistry letters.
[3] Terry Kenakin,et al. Recent progress in discovery of small-molecule CCR5 chemokine receptor ligands as HIV-1 inhibitors. , 2003, Bioorganic & medicinal chemistry.
[4] B. Fermini,et al. The impact of drug-induced QT interval prolongation on drug discovery and development , 2003, Nature Reviews Drug Discovery.
[5] Karen Holmes,et al. 1,3,4 Trisubstituted pyrrolidine CCR5 receptor antagonists bearing 4-aminoheterocycle substituted piperidine side chains. , 2003, Bioorganic & medicinal chemistry letters.
[6] D. Hazuda,et al. 1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 4: synthesis of N-1 acidic functionality affording analogues with enhanced antiviral activity against HIV. , 2002, Bioorganic & medicinal chemistry letters.
[7] D. Hazuda,et al. CCR5 antagonists: bicyclic isoxazolidines as conformationally constrained N-1-substituted pyrrolidines. , 2002, Bioorganic & medicinal chemistry letters.
[8] D. Hazuda,et al. Combinatorial synthesis of CCR5 antagonists. , 2001, Bioorganic & medicinal chemistry letters.
[9] D. Hazuda,et al. Discovery of human CCR5 antagonists containing hydantoins for the treatment of HIV-1 infection. , 2001, Bioorganic & medicinal chemistry letters.
[10] D. Hazuda,et al. 1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 2: lead optimization affording selective, orally bioavailable compounds with potent anti-HIV activity. , 2001, Bioorganic & medicinal chemistry letters.
[11] E A Emini,et al. Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 4: synthesis and structure-activity relationships for 1-[N-(methyl)-N-(phenylsulfonyl)amino]-2-(phenyl)-4-(4-(N-(alkyl)-N-(benzyloxycarbonyl)amino)piperidin-1-yl)butanes. , 2001, Bioorganic & medicinal chemistry letters.
[12] B. Neustadt,et al. Piperazine-based CCR5 antagonists as HIV-1 inhibitors. II. Discovery of 1-[(2,4-dimethyl-3-pyridinyl)carbonyl]-4- methyl-4-[3(S)-methyl-4-[1(S)-[4-(trifluoromethyl)phenyl]ethyl]-1-piperazinyl]- piperidine N1-oxide (Sch-350634), an orally bioavailable, potent CCR5 antagonist. , 2001, Journal of medicinal chemistry.
[13] M. Maccoss,et al. 1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 1: discovery of the pyrrolidine scaffold and determination of its stereochemical requirements. , 2001, Bioorganic & medicinal chemistry letters.
[14] J A Grobler,et al. Inhibitors of strand transfer that prevent integration and inhibit HIV-1 replication in cells. , 2000, Science.
[15] Cavero,et al. QT interval prolongation by non-cardiovascular drugs: issues and solutions for novel drug development. , 1999, Pharmaceutical science & technology today.
[16] O. Nishimura,et al. A small-molecule, nonpeptide CCR5 antagonist with highly potent and selective anti-HIV-1 activity. , 1999, Proceedings of the National Academy of Sciences of the United States of America.
[17] S. Buchwald,et al. A Catalytic Method for the Conversion of Silanes to Stannanes , 1994 .
[18] Michael S. Saag,et al. A Short-Term Clinical Evaluation of L-697,661, a Non-Nucleoside Inhibitor of HIV-1 Reverse Transcriptase , 1993 .
[19] K. Teng,et al. Palladium-catalyzed reactions of acyl chlorides with (1-alkynyl)tributylstannanes. A convenient synthesis for 1-alkynyl ketones , 1982 .
[20] D. Hazuda,et al. 1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists: modifications of the arylpropylpiperidine side chains. , 2003, Bioorganic & medicinal chemistry letters.
[21] Hao Wang,et al. Functional and pharmacological properties of canine ERG potassium channels. , 2003, American journal of physiology. Heart and circulatory physiology.
[22] E. Corey,et al. A synthetic method for formyl→ethynyl conversion (RCHO→RCCH or RCCR′) , 1972 .