153729-53-4Relevant academic research and scientific papers
Design and synthesis of novel dihydroquinoline-3-carboxylic acids as HIV-1 integrase inhibitors
Sechi, Mario,Rizzi, Giuseppe,Bacchi, Alessia,Carcelli, Mauro,Rogolino, Dominga,Pala, Nicolino,Sanchez, Tino W.,Taheri, Laleh,Dayam, Raveendra,Neamati, Nouri
experimental part, p. 2925 - 2935 (2009/09/05)
Previously, we discovered linomide analogues as novel HIV-1 integrase (IN) inhibitors. Here, to make possible structure-activity relationships, we report on the design and synthesis of a series of substituted dihydroquinoline-3-carboxylic acids. The crystal structure of the representative compound 2c has also been solved. Among the eight new analogues, 2e showed a potency in inhibiting IN strand transfer catalytic activity similar to the reference diketo acid inhibitor L-731,988 (IC50 = 0.9 μM vs. 0.54 μM, for 2e and L-731,988, respectively). Furthermore, none of the compounds showed significant cytotoxicity in two tested cancer cell lines. These compounds represent an interesting prototype of IN inhibitors, potentially involved in a metal chelating mechanism, and further optimization is warranted.
Novel routes to 4-substituted N,N-dialkylanilines, N-alkylanilines and anilines
Katritzky, Alan R.,Lang, Hengyuan,Lan, Xiangfu
, p. 7445 - 7454 (2007/10/02)
4-(Benzotriazol-1-ylmethyl)-N,N-dialkylanilines, -N-alkylanilines, -anilines and some substituted analogs obtained via lithiation are converted by lithium aluminum hydride or Grignard reagents into 4-substituted N,N-dialkylanilines, N-alkylanilines and anilines, respectively, in good yields.
