130200-58-7Relevant articles and documents
Design, Conformation, and Crystallography of 2-Naphthyl Phenyl Ethers as Potent Anti-HIV Agents
Lee, Won-Gil,Chan, Albert H.,Spasov, Krasimir A.,Anderson, Karen S.,Jorgensen, William L.
supporting information, p. 1156 - 1160 (2016/12/16)
Catechol diethers that incorporate a 7-cyano-2-naphthyl substituent are reported as non-nucleoside inhibitors of HIV-1 reverse transcriptase (NNRTIs). Many of the compounds have 1-10 nM potencies toward wild-type HIV-1. An interesting conformational effect allows two unique conformers for the naphthyl group in complexes with HIV-RT. X-ray crystal structures for 4a and 4f illustrate the alternatives.
Dicationic DNA-targeted antiprotozoal agents: Naphthalene replacement of benzimidazole
Chackal-Catoen, Sarah,Miao, Yi,Wilson, W. David,Wenzler, Tanja,Brun, Reto,Boykin, David W.
, p. 7434 - 7445 (2007/10/03)
A series of naphthalene analogues of highly active benzimidazole diamidines were synthesized using sequential Stille and Suzuki coupling reactions for preparation of the bis-nitrile intermediates. All of the diamidines showed strong DNA affinities as judged by high ΔTm values with poly(dA-dT). The dicationic compounds were quite active in vitro versus Trypanosoma brucei rhodesiense (T. b. r.) exhibiting IC50 values ranging from 4 to 98 nM. These compounds were also active versus Plasmodium falciparum (P. f.) giving IC50 values ranging from 4 to 33 nM. Two of the compounds showed good activity in vivo in the STIB900 model for acute African trypanosomiasis; one gave 3/4 cures and the other gave 4/4 cures on ip dosage of 20 mg/kg for 4 days. The amidoxime prodrugs of the naphthalene analogues were essentially ineffective.
Pharmaceutical compounds
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, (2008/06/13)
This invention relates to compounds of formula (I) where R1 to R12, —W—V—, —X—Y—, m and n have the values defined in claim 1, their preparation and use as pharmaceuticals.
