Caffeoyl naphthalenesulfonamide derivatives as HIV integrase inhibitors
摘要:
HIV-1 integrase (IN) is an essential enzyme for retroviral replication and a rational target for the design of anti-AIDS drugs. In the present study, we have designed, synthesized and tested a series of caffeoyl naphthalenesulfonamide derivatives as HIV integrase inhibitors. Among these compounds, we found that HIV integrase inhibitory activities of compounds III-3 and III-4 were more potent than L-chicoric acid (IC50 = 11.8 mug/mL) and others were comparable to L-chicoric acid. Furthermore, the structure-activity relationships of these compounds were studied. The information gathered from this paper will be useful in the development and design of HIV-1 integrase inhibitors in the future. (C) 2003 Elsevier Ltd. All rights reserved.
Synthesis, application and investigation of structure–thermal stability relationships of thermally stable water-soluble azo naphthalene dyes for LCD red color filters
作者:Young Do Kim、Jung Hyun Cho、Chong Rae Park、Jae-Hong Choi、Chun Yoon、Jae Pil Kim
DOI:10.1016/j.dyepig.2010.07.008
日期:2011.4
isomeric water-soluble azo naphthalene dyes were synthesized, and their thermal properties were examined by thermogravimetric analysis and differential scanning calorimetry. Dye-based color filters were also fabricated using the synthesized dyes. Transmittance (98.9%) at 650 nm and a wide color gamut (62.8%) were achieved using one of the color filters. All the prepared dyes had a degradation temperature
A process for producing an aromatic amine comprises heating an aromatic sulfonate and a metal amide in liquid ammonia in a closed reactor at a temperature of at least 40.degree. C to produce a metal arylamide and reacting the resultant metal arylamide with water or lower aliphatic alcohol to produce an aromatic amine.
Development of Potent and Selective Inhibitors of <i>ecto</i>-5′-Nucleotidase Based on an Anthraquinone Scaffold
作者:Younis Baqi、Sang-Yong Lee、Jamshed Iqbal、Peter Ripphausen、Anne Lehr、Anja B. Scheiff、Herbert Zimmermann、Jürgen Bajorath、Christa E. Müller
DOI:10.1021/jm901851t
日期:2010.3.11
ecto-5'-Nucleotidase (eN, CD73) plays it major role in controlling extracellular adenosine levels. eN inhibitors have potential its novel drugs, for example, for the treatment of cancer. In the present study, we synthesized and investigated a series of 55 anthraquinone derivatives as potential inhibitors of eN, I I of which are novel compounds and another I I of which had previously been described but have now been synthesized by all improved method. We identified several potent inhibitors of rat eN. The most potent compounds were 1-amino-4-[4-fluoro-2-carboxyphenylamino]-9, 10-dioxo-9, 10-dihydroanthracene-2-sulfonate (45, PSB-0952, K-i = 260 nM) and 1-amino-4-[2-anthracenylamino]-9, 10-dioxo-9, 10-dihydroanthracene-2-sulfonate (52, PSB-0963, 150 nM), with 52 being the most potent eN inhibitor described to date. Selected compounds were further characterized and found to exhibit a competitive mechanism of inhibition. Investigations of ecto-nucleoside triphosphate diphosphohydrolases (NTPDases) and the P2Y receptor subtypes P2Y(2), P2Y(4), P2Y(6), and P2Y(12) showed that compound 45 exhibited the highest degree of selectivity (> 150-fold).
Rieche,A.; Seeboth,H., Justus Liebigs Annalen der Chemie, 1960, vol. 638, p. 101 - 110
作者:Rieche,A.、Seeboth,H.
DOI:——
日期:——
KUTKEVICHUS S. I.; BORIK A. G.; FILICHEVA T. B.; MATVEEVA M. K.; CHUDAKOV+, LIETTSR AUKSTUJU MOKUKLU MOKSVLO DARVAI. CHEMIJA IR CHEM. TESNNOL., VYSSH+
作者:KUTKEVICHUS S. I.、 BORIK A. G.、 FILICHEVA T. B.、 MATVEEVA M. K.、 CHUDAKOV+