67852-86-2Relevant academic research and scientific papers
Synthesis of cellulose adipate derivatives
Kar, Nilanjana,Liu, Haoyu,Edgar, Kevin J.
, p. 1106 - 1115 (2011)
Cellulose esters containing adipates and other ester groups are synthesized by the reaction of commercially available cellulose esters in solution with the benzyl monoester of adipoyl chloride. The products, cellulose adipate esters in which the distal en
Synthesis and biological evaluation of oleanolic acid derivatives as inhibitors of protein tyrosine phosphatase 1B
Qian, Shan,Li, Haijiao,Chen, Yin,Zhang, Weiyu,Yang, Shengyong,Wu, Yong
experimental part, p. 1743 - 1750 (2011/03/18)
Protein tyrosine phosphatase 1B (PTP1B) is a negative regulator in the process of insulin signaling and a promising drug target for diabetes and obesity. Derivatives of oleanolic acid were synthesized and evaluated as PTP1B inhibitors. Several derivatives exhibited moderate to good inhibitory activities against PTP1B, with 25f displaying the most promising inhibition (IC 50 = 3.12 μM). Structure-activity relationship analyses of these derivatives demonstrated that the integrity of the A ring and 12-ene moieties was important in the retention of PTP1B enzyme inhibitory activities. In addition, hydrophilic and acidic groups as well as the distance between the oleanene and acid moieties were associated with PTP1B inhibitory activities. Possible binding modes of 25f were explored by molecular docking simulations.
Synthesis and antibiofilm activity of a second-generation reverse-amide oroidin library: A structure-activity relationship study
Eric Ballard,Richards, Justin J.,Wolfe, Amanda L.,Melander, Christian
experimental part, p. 10745 - 10761 (2009/12/04)
A second-generation library of 2-aminoimidazole-based derivatives incorporating a "reversed amide" (RA) motif in comparison to the marine natural product oroidin were synthesized and subsequently assayed for antibiofilm activity against the medically relevant Gram-negative proteobacteria P. aeruginosa and A. baumannii. Most notably, an in-depth activity profile is reported for the most active subclass of derivatives that bear linear aliphatic chains off the amide bond. Additionally, further structural modifications of the core template, such as removal of the amide bond or substitution with a triazole isostere, resulted in the discovery of analogues with antibiofilm activities that varied with respect to their inhibition and dispersal properties of P. aeruginosa and A. baumannii biofilms.
Synthesis of mimics to thymidine and 5-(2''-thienyl)-2'-deoxyuridine triphosphates
Wellmar,Hornfeldt,Gronowitz,Johansson
, p. 1059 - 1076 (2007/10/03)
Dicarboxylic acid 5'-monoesters of thymidine and 5-(2-thienyl)- 2''deoxyuridine have been synthesised and evaluated as triphosphate mimics. Glutaric (25, 29), adipic (26, 30), pimelic (27, 31) and trans-1,4- cyclohexane dicarboxylic acids (28, 32) were em
