共查询到20条相似文献,搜索用时 46 毫秒
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J Balzarini M J Pérez-Pérez A San-Félix M J Camarasa I C Bathurst P J Barr E De Clercq 《The Journal of biological chemistry》1992,267(17):11831-11838
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Breslin HJ Kukla MJ Kromis T Cullis H De Knaep F Pauwels R Andries K De Clercq E Janssen MA Janssen PA 《Bioorganic & medicinal chemistry》1999,7(11):2427-2436
4,5,6,7-Tetrahydro-5-methylimidazo[4,5,1-jk][1,4]benzodiazepin-2(1 H)-ones (TIBO), 1, have been shown to significantly inhibit HIV-1 replication, as reported in detail in our prior publications. Since our earlier reports, we have modified the TIBO structures 1 by removing the 5-membered ring of 1, generating 1,3,4,5-tetrahydro-2H-1,4-benzodiazepin-2-ones (TBO), 4, a bicyclic series of compounds. Although compounds 4 possess modest activity when compared to TIBO analogues 1, they clearly demonstrated significant anti-HIV-1 activity. 相似文献
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Hiromichi Tanaka Masanori Baba Emiko Takahashi Kouichiro Matsumoto Atsushi Kittaka Richard T. Walker 《Nucleosides, nucleotides & nucleic acids》2013,32(1-3):155-162
Abstract Regioisomeric analogues of the anti-HIV-1 lead 1-[(2-hydroxy-ethoxy)methyl]-6-(phenylthio)thymine (1: HEPT) have been synthesized. These compounds, having an ethoxymethyl side chain at C-5 and an ethyl group at the N-1 position of the uracil ring, also possess activity against HIV-1. 相似文献
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Hiromichi Tanaka Tadashi Miyasaka Kouichi Sekiya Hideaki Takashima Masaru Ubasawa Issei Nitta 《Nucleosides, nucleotides & nucleic acids》2013,32(2-4):447-456
Abstract Analogues of a recently developed specific anti-HIV-1 agent HEPT, 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine, having different types of acyclic moieties were synthesized based on lithiation chemistry. Anti-HIV-1 activity of these analogues is also described. 相似文献
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Masanori Baba Hlromichi Tanaka Tadashi Miyasaka Satoshi Yuasa Masaru Ubasawa Richard T. Walker 《Nucleosides, nucleotides & nucleic acids》2013,32(3-5):575-583
Abstract The 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) derivatives have been found to be potent and specific inhibitors of human immunodeficiency virus type 1 (HIV-1) replication in vitro. Among the compounds, MKC-442 (6-benzyl-1-ethoxymethyl-5-isopropyluracil) has recently been chosen as a candidate for clinical efficacy and safety studies in patients with the acquired immune deficiency syndrome (AIDS). 相似文献
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Inhibition of HIV-1 ribonuclease H by a novel diketo acid, 4-[5-(benzoylamino)thien-2-yl]-2,4-dioxobutanoic acid 总被引:7,自引:0,他引:7
Shaw-Reid CA Munshi V Graham P Wolfe A Witmer M Danzeisen R Olsen DB Carroll SS Embrey M Wai JS Miller MD Cole JL Hazuda DJ 《The Journal of biological chemistry》2003,278(5):2777-2780