6309-49-5Relevant academic research and scientific papers
Vesicle and stable monolayer formation from simple "click" chemistry adducts in water
Bhattacharya, Santanu,Biswas, Joydeep
, p. 1581 - 1591 (2011)
Click chemistry has been successfully extended into the field of molecular design of novel amphiphatic adducts. After their syntheses and characterizations, we have studied their aggregation properties in aqueous medium. Each of these adducts forms stable suspensions in water. These suspensions have been characterized by dynamic light scattering (DLS) studies and transmission electron microscopy (TEM). The presence of inner aqueous compartments in such aggregates has been demonstrated using dye (methylene blue) entrapment studies. These aggregates have been further characterized using X-ray diffraction (XRD), which indicates the existence of bilayer structures in them. Therefore, the resulting aggregates could be described as vesicles. The temperature-induced order-to-disorder transitions of the vesicular aggregates and the accompanying changes in their packing and hydration have been examined using high-sensitivity differential scanning calorimetry, fluorescence anisotropy, and generalized polarization measurements using appropriate membrane-soluble probe, 1,6-diphenylhexatriene, and Paldan, respectively. The findings of these studies are consistent with each other in terms of the apparent phase transition temperatures. Langmuir monolayer studies confirmed that these click adducts also form stable monolayers on buffered aqueous subphase at the air-water interface.
Synthesis and evaluation of novel oleanolic acid derivatives as potential antidiabetic agents
Zhang, Liying,Jia, Xiaojian,Dong, Jizhe,Chen, Dongyin,Liu, Jun,Zhang, Luyong,Wen, Xiaoan
, p. 297 - 305 (2014/03/21)
Antidiabetic agents simultaneously inhibiting hepatic glucose production and stimulating hepatic glucose consumption could apply a better control over hyperglycemia. A series of oleanolic acid derivatives with bulky substituents at C-3 position were designed and synthesized in order to search for this kind of agents. All of the compounds were evaluated biologically in vitro using glycogen phosphorylase and HepG2 cells. The results indicated that several derivatives exhibited moderate-to-good inhibitory activities against glycogen phosphorylase. Compound 8g showed the best inhibition with an IC50 value of 5.4 μm. Moreover, most of the derivatives were found to increase the glucose consumption in HepG2 cells in a dose-dependent manner. The possible binding mode of compound 8g with glycogen phosphorylase was also explored by docking study. 8g was found to have hydrogen bonding interactions with Arg193, Arg310, and Arg60 of the allosteric site.
Identification of pentacyclic triterpenes derivatives as potent inhibitors against glycogen phosphorylase based on 3D-QSAR studies
Liang, Zhongjie,Zhang, Liying,Li, Lianchun,Liu, Jun,Li, Hongling,Zhang, Luyong,Chen, Limin,Cheng, Keguang,Zheng, Mingyue,Wen, Xiaoan,Zhang, Pu,Hao, Jia,Gong, Yanchun,Zhang, Xia,Zhu, Xiaoyun,Chen, Jun,Liu, Hong,Jiang, Hualiang,Luo, Cheng,Sun, Hongbin
supporting information; experimental part, p. 2011 - 2021 (2011/06/22)
Naturally occurring pentacyclic triterpenes (PT), a novel class of inhibitors against glycogen phosphorylase (GP), hold promise for the treatment of type-2 diabetes and other diseases with disorders in glycogen metabolism. To identify novel and more potent GP inhibitors, the receptor-based comparative molecular field analysis (CoMFA) and comparative molecular similarity analysis (CoMSIA) approaches were performed to investigate the quantitative structure-activity relationships (QSAR) among 106 PT analogues. The validated models demonstrated that the elongated or bulky substitutions in C17 position and/or C2, C3 positions are favorable. Then based on the structural information extracted from these models, 56 derivatives were synthesized and biochemically tested in this study. The IC50 value of the most potent compound P50 was found to be 1.1 μM.
Expeditious preparation of triazole-linked glycolipids via microwave accelerated click chemistry and their electrochemical and biological assessments
Song, Shao-Xing,Zhang, Hai-Lin,Kim, Chol-Guk,Sheng, Li,He, Xiao-Peng,Long, Yi-Tao,Li, Jia,Chen, Guo-Rong
body text, p. 9974 - 9980 (2011/02/23)
A series of triazole-linked ester-type glycolipids were efficiently prepared via a two-step sequence involving microwave accelerated 'click' chemistry and debenzylation. All carbon chain length varied O-alkynyl fatty esters used to couple with 1-azido-tet
Multisite modification of neomycin B: Combined Mitsunobu and click chemistry approach
Quader, Sabina,Boyd, Sue E.,Jenkins, Ian D.,Houston, Todd A.
, p. 1962 - 1979 (2007/10/03)
The aminoglycoside antibiotic neomycin B has been converted into several novel building blocks that can be used for the specific modification of three of the four ring systems. Under carefully controlled conditions, the Mitsunobu reaction can be used to s
Mild esterification and transesterification of carboxylic acids catalyzed by tetracyanoethylene and dicyanoketene dimethyl acetal
Masaki, Yukio,Tanaka, Nobuyuki,Miura, Tsuyoshi
, p. 55 - 56 (2007/10/03)
A π-acid tetracyanoethylene (TCNE) and its derivative dicyanoketene dimethyl acetal (DCKDMA) were found to catalyze esterification of lauric acid with various types of alcohols. This method was successfully applied to methyl esterification of a variety of carboxylic acids including aromatic, α,β-unsaturated, α-hydroxy, and N-Cbz and N-Boc-protected α-amino acids without racemization at the range from room temperature to 60 °C. TCNE was also found to operate as a catalyst in transeslerification reaction of methyl laurate.
Alkynyl esters for controlling mites
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, (2008/06/13)
Esters of alkynyl alcohols or alkynyl acids are useful for the control of mites.
