870819-89-9Relevant academic research and scientific papers
Tetrazole thioacetanilides: Potent non-nucleoside inhibitors of WT HIV reverse transcriptase and its K103N mutant
Muraglia, Ester,Kinzel, Olaf D.,Laufer, Ralph,Miller, Michael D.,Moyer, Gregory,Munshi, Vandna,Orvieto, Federica,Palumbi, Maria Cecilia,Pescatore, Giovanna,Rowley, Michael,Williams, Peter D.,Summa, Vincenzo
, p. 2748 - 2752 (2007/10/03)
A series of aryltetrazolylacetanilides was synthesized and evaluated as HIV-1 non-nucleoside reverse transcriptase inhibitors on wild-type virus and on the clinically relevant K103N mutant strain. Extensive SAR investigation led to potent compounds, with nanomolar activity on K103N, and orally bioavailable in rats.
HIV REVERSE TRANSCRIPTASE INHIBITORS
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Page/Page column 40-41, (2010/02/14)
Tetrazolyl derivatives of Formula I: are HIV reverse transcriptase inhibitors, wherein U is O, S(O)n where n is an integer equal to zero, 1 or 2, or N(R4); V is optionally substituted C1-8 alkylene; W is C(O)N(R2) or a direct bond linking V to R3; and R1, R2, R3 and R4 are defined herein. The derivatives of Formula I are useful in the inhibition of HIV reverse transcriptase, the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The derivatives are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The derivatives and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
