17738-99-7Relevant academic research and scientific papers
Discovery of Cytochrome P450 4F11 Activated Inhibitors of Stearoyl Coenzyme A Desaturase
Winterton, Sarah E.,Capota, Emanuela,Wang, Xiaoyu,Chen, Hong,Mallipeddi, Prema L.,Williams, Noelle S.,Posner, Bruce A.,Nijhawan, Deepak,Ready, Joseph M.
, p. 5199 - 5221 (2018/06/13)
Stearoyl-CoA desaturase (SCD) catalyzes the first step in the conversion of saturated fatty acids to unsaturated fatty acids. Unsaturated fatty acids are required for membrane integrity and for cell proliferation. For these reasons, inhibitors of SCD represent potential treatments for cancer. However, systemically active SCD inhibitors result in skin toxicity, which presents an obstacle to their development. We recently described a series of oxalic acid diamides that are converted into active SCD inhibitors within a subset of cancers by CYP4F11-mediated metabolism. Herein, we describe the optimization of the oxalic acid diamides and related N-acyl ureas and an analysis of the structure-activity relationships related to metabolic activation and SCD inhibition.
CD4 mimics as HIV entry inhibitors: Lead optimization studies of the aromatic substituents
Narumi, Tetsuo,Arai, Hiroshi,Yoshimura, Kazuhisa,Harada, Shigeyoshi,Hirota, Yuki,Ohashi, Nami,Hashimoto, Chie,Nomura, Wataru,Matsushita, Shuzo,Tamamura, Hirokazu
, p. 2518 - 2526 (2013/06/26)
Several CD4 mimics have been reported as HIV-1 entry inhibitors that can intervene in the interaction between a viral envelope glycoprotein gp120 and a cell surface protein CD4. Our previous SAR studies led to a finding of a highly potent analogue 3 with bulky hydrophobic groups on a piperidine moiety. In the present study, the aromatic ring of 3 was modified systematically in an attempt to improve its antiviral activity and CD4 mimicry which induces the conformational changes in gp120 that can render the envelope more sensitive to neutralizing antibodies. Biological assays of the synthetic compounds revealed that the introduction of a fluorine group as a meta-substituent of the aromatic ring caused an increase of anti-HIV activity and an enhancement of a CD4 mimicry, and led to a novel compound 13a that showed twice as potent anti-HIV activity compared to 3 and a substantial increase in a CD4 mimicry even at lower concentrations.
SUBSTITUTED TRIAZOLECARBOXAMIDES
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Page 29, (2008/06/13)
Substituted triazolecarboxamides A b s t r a c t The invention relates to substituted triazolecarboxamides of the formula (I) in which R1, R2, R3 and R4 are as defined in the description, to their use as crop treatment agents, in particular as herbicides,
