38289-20-2Relevant articles and documents
Antimalarial activity of 2,6-dibenzylidenecyclohexanone derivatives
Eagon, Scott,Hammill, Jared T.,Fitzsimmons, Kasey,Sienko, Natalie,Nguyen, Brandon,Law, Jarvis,Manjunath, Aashrita,Wilkinson, Steven P.,Thompson, Kara,Glidden, Julia Elizabeth,Rice, Amy L.,Falade, Mofolusho O.,Kimball, Joshua J.,DiBernardo, Celine,Guy, R. Kiplin
supporting information, (2021/07/06)
Malaria remains one of the deadliest infectious diseases worldwide and continues to infect hundreds of millions of individuals each year. Here we report the discovery and derivatization of a series of 2,6-dibenzylidenecyclohexanones targeting the chloroquine-sensitive 3D7 strain of Plasmodium falciparum. While the initial lead compound displayed significant toxicity in a human cell proliferation assay, we were able to identify a derivative with no detectable toxicity and sub-micromolar potency.
Synthesis and optimization of novel 4,4-disubstituted cyclohexylbenzamide derivatives as potent 11β-HSD1 inhibitors
Sun, Daqing,Wang, Zhulun,Caille, Seb,Degraffenreid, Michael,Gonzalez-Lopez De Turiso, Felix,Hungate, Randall,Jaen, Juan C.,Jiang, Ben,Julian, Lisa D.,Kelly, Ron,McMinn, Dustin L.,Kaizerman, Jacob,Rew, Yosup,Sudom, Athena,Tu, Hua,Ursu, Stefania,Walker, Nigel,Willcockson, Maren,Yan, Xuelei,Ye, Qiuping,Powers, Jay P.
body text, p. 405 - 410 (2011/02/27)
The synthesis and SAR of a series of 4,4-disubstituted cyclohexylbenzamide inhibitors of 11β-HSD1 are described. Optimization rapidly led to potent, highly selective, and orally bioavailable inhibitors demonstrating efficacy in both rat and non-human primate ex vivo pharmacodynamic models.
Spirocyclic Azaindole Derivatives
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Page/Page column 9, (2009/07/03)
The invention relates to substituted azaindole derivatives, to methods for the production thereof, to medicaments containing said compounds and to the use of substituted azaindole derivatives for producing medicaments.