Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 2: Discovery of potent, selective, and orally bioavailable compounds

Inhibitors of Strand Transfer That Prevent Integration and Inhibit HIV-1 Replication in Cells

Daria J. Hazuda, Peter J. Felock, Marc Witmer et al. · Science · 2000 · 1.1K citations

Life Sciences, Medicinal Chemistry, Molecular Biology +16

A small-molecule, nonpeptide CCR5 antagonist with highly potent and selective anti-HIV-1 activity

Masanori Baba, Osamu Nishimura, Naoyuki Kanzaki et al. · Proceedings of the National Academy of Sciences · 1999 · 755 citations

Medicine, Immunology, Pharmacology +17

A Short-Term Clinical Evaluation of L-697,661, a Non-Nucleoside Inhibitor of HIV-1 Reverse Transcriptase

Michael S. Saag, Emilio A. Emini, Oscar L. Laskin et al. · New England Journal of Medicine · 1993 · 147 citations · Full text

Life Sciences, Molecular Biology, Pharmacotherapy +16

Piperazine-Based CCR5 Antagonists as HIV-1 Inhibitors. II. Discovery of 1-[(2,4-Dimethyl-3-pyridinyl)carbonyl]-4- methyl-4-[3(<i>S</i>)-methyl-4-[1(<i>S</i>)-[4-(trifluoro- methyl)phenyl]ethyl]-1-piperazinyl]- piperidine <i>N</i>1-Oxide (Sch-350634), an Orally Bioavailable, Potent CCR5 Antagonist

Jayaram R. Tagat, Ruo W. Steensma, Stuart W. McCombie et al. · Journal of Medicinal Chemistry · 2001 · 113 citations · Full text

Pharmacy, Medicinal Chemistry, Pharmacology +17

Tandem Radical Decarboxylation−Oxidation of Amino Acids:  A Mild and Efficient Method for the Generation of <i>N</i>-Acyliminium Ions and Their Nucleophilic Trapping

Alicia Boto, Rosendo Hernández, Ernesto Suárez · The Journal of Organic Chemistry · 2000 · 111 citations

Natural Sciences, Chemistry, Bioorganic Chemistry +14