68252-72-2Relevant academic research and scientific papers
Tri-substituted triazoles as potent non-nucleoside inhibitors of the HIV-1 reverse transcriptase
De La Rosa, Martha,Kim, Hong Woo,Gunic, Esmir,Jenket, Cheryl,Boyle, Uyen,Koh, Yung-hyo,Korboukh, Ilia,Allan, Matthew,Zhang, Weijian,Chen, Huanming,Xu, Wen,Nilar, Shahul,Yao, Nanhua,Hamatake, Robert,Lang, Stanley A.,Hong, Zhi,Zhang, Zhijun,Girardet, Jean-Luc
, p. 4444 - 4449 (2007/10/03)
A new series of 1,2,4-triazoles was synthesized and tested against several NNRTI-resistant HIV-1 isolates. Several of these compounds exhibited potent antiviral activities against efavirenz- and nevirapine-resistant viruses, containing K103N and/or Y181C mutations or Y188L mutation. Triazoles were first synthesized from commercially available substituted phenylthiosemicarbazides, then from isothiocyanates, and later by condensing the desired substituted anilines with thiosemicarbazones.
HIV REVERSE TRANSCRIPTASE INHIBITORS
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Page/Page column 40, (2010/10/20)
Compounds of Formula (I) are HIV reverse transcriptase inhibitors, wherein T is O or S; U is O, S, N(R4), or a direct bond linking V to the C(=T) moiety; V is optionally substituted C1-6 alkylene; W is C(O)N(R5) or a direct bond linking V to R3; and R1, R2, R3, R4 and R5 are defined herein. The compounds of Formula (I) and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
HIV REVERSE TRANSCRIPTASE INHIBITORS
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Page/Page column 39-40, (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.
Carbonic anhydrase inhibitors. Inhibition of tumor-associated isozyme IX by halogenosulfanilamide and halogenophenylaminobenzolamide derivatives
Ilies, Marc A.,Vullo, Daniela,Pastorek, Jaromir,Scozzafava, Andrea,Ilies, Monica,Caproiu, Miron T.,Pastorekova, Silvia,Supuran, Claudiu T.
, p. 2187 - 2196 (2007/10/03)
Two series of halogenated sulfonamides have been prepared. The first consists of mono/ dihalogenated sulfanilamides, whereas the second one consists of the mono/dihalogenated aminobenzolamides, incorporating equal or different halogens (F, Cl, Br, and I). These sulfonamides have been synthesized from the corresponding anilines by acetylation (protection of the amino group), chlorosulfonylation, followed either by amidation, or reaction with 5-amino1,3,4-thiadiazole-2-sulfonamide (and eventually deacetylation). All these compounds, together with the six clinically used sulfonamide inhibitors (acetazolamide, methazolamide, ethoxzolamide, dichlorophenamide, dorzolamide, and brinzolamide) were investigated as inhibitors of the transmembrane, tumor-associated isozyme carbonic anhydrase (CA) IX. Inhibition data against the classical, physiologically relevant isozymes I, II, and IV were also obtained. CA IX shows an inhibition profile which is generally completely different from those of isozymes I, II, and IV, with potent inhibitors (inhibition constants in the range of 12-40 nM) among both simple aromatic (such as 3-fluoro-5-chloro-4-aminobenzenesulfonamide) as well as heterocyclic compounds (such as acetazolamide, methazolamide, 5-amino-1,3,4-thiadiazole-2-sulfonamide, aminobenzolamide, and dihalogenated aminobenzolamides). This first detailed CA IX inhibition study revealed many interesting leads, suggesting the possibility to design even more potent and eventually CA IX-selective inhibitors, with putative applications as antitumor agents.
