38153-27-4Relevant academic research and scientific papers
A New Series of Salicylic Acid Derivatives as Non-saccharide α-Glucosidase Inhibitors and Antioxidants
Chen, Jiangang,Lu, Wenfang,Chen, Hao,Bian, Xiaoli,Yang, Guangde
, p. 231 - 246 (2019/02/19)
In this study, a series of salicylic acid derivatives were designed and synthesized as novel non-saccharide α-glucosidase inhibitors. Biological evaluation indicated that when compared to acarbose, compounds T9, T10, and T32 exhibited a higher potency of α-glucosidase inhibitory activity with IC50 values of 0.15±0.01, 0.086±0.01 and 0.32±0.02mM, respectively. Evaluation of the inhibition kinetics indicated that T9, T10, T32, and acarbose interacted with α-glucosidase in a mixed non-competitive inhibitory manner. Moreover, T9, T10, and T32 statically quenched the fluorescence of α-glucosidase by formation of an inhibitor-α-glucosidase complex. The docking results showed that hydrogen bonds were generated between the test compounds and α-glucosidase. The antioxidant study revealed that compound T10 exhibited a higher antioxidant activity via scavenging 1,1-diphenyl-2-picrylhydrazyl free radical (DPPH), thereby inhibiting lipid peroxidation and the total reduction capacity. In brief, the salicylic acid derivatives identified in this study were promising candidates for development as novel non-saccharide α-glucosidase inhibitors.
Synthesis of acyl analogues of coniferyl alcohol and their antimycobacterial activity
Bhatti, Huma Aslam,Uddin, Nizam,Begum, Sabira,Siddiqui, Bina Shaheen
, p. 886 - 889 (2013/07/26)
In search of new anti-mycobacterial agents seven acyl and one benzyl derivatives of coniferyl alcohol were synthesized and evaluated along with coniferyl alcohol for antitubercular activity against Mycobacterium tuberculosis H37Rv (Mtb) in vitro. Four com
Asymmetric synthesis of the natural erythro-(1R,2S)-8-O-4′-neolignan myrislignan
Xia,Wang, Wei
, p. 93 - 96 (2011/10/01)
An efficient and practical asymmetric synthesis of erythro-(1R,2S)-8-O- 4′-neolignan myrislignan was achieved by using vanillin and pyrogallic acid as the starting materials. Two key steps are involved: preparation of an enantiopure threo alcohol of predictable stereochemistry by dihydroxylation with AD-mix-β, and inversion of the absolute configuration from the threo to the erythro isomer using a Mitsunobu reaction. The route illustrates a new methodology for the synthesis of erythro-8-O-4′-neolignan. Graphical abstract: [Figure not available: see fulltext.]
Asymmetric synthesis of erythro-8-O-4'-neolignan Machilin C
Xia, Yamu,Chang, Liang,Ding, Yining,Jiao, Bin
, p. 151 - 152 (2011/07/08)
A new methodology for the synthesis of the erythro-8-O-4'-neolignan Machilin C based on the Sharpless asymmetric dihydroxylation reaction and the Mitsunobu reaction as two key steps is described.
Asymmetric synthesis of machilin C and its analogue
Xia, Yamu,Wang, Wei
, p. 630 - 636 (2011/10/19)
Full details of the asymmetric total synthesis of erythro-8-O-4′-neolignan, machilin C, and its analogue perseal A are reported. The synthesis was involved in the Sharpless dihydroxylation reaction that occurred with excellent asymmetric induction, and the Mitsunobu reaction which occurred with inversion of the absolute configuration from the threo to the erythro isomer. The synthesis was achieved from simple vanillin in eight to twelve steps.
Asymmetric synthesis of 8-O-4′-neolignan perseal B
Xia, Ya-Mu,Wang, Wei,Guo, Ying-Lan,Li, Jun-Feng
experimental part, p. 375 - 380 (2010/11/03)
Full details of an enantioselective total synthesis of 8-O-4'-neolignan perseal B are presented for the first time. The synthesis was achieved in 8 steps from vanillin and involved the asymmetric dihydroxylation reaction using AD-mix-α to give the key intermedium (1S,2S)-1-(4-(benzyloxy)-3- methoxyphenyl)propane-1,2,3-triol, and the Mitsunobu reaction between phenylpropanoid and vanillin formed perseal B. The synthetic method of perseal B exhibits a new route for 8-O-4'-neolignan. TUBITAK.
A novel and efficient procedure for the preparation of allylic alcohols from α,β-unsaturated carboxylic esters using LiAlH4/BnCl
Wang, Xiaolong,Li, Xiaodong,Xue, Jijun,Zhao, Yuling,Zhang, Yumei
experimental part, p. 413 - 415 (2009/05/11)
A new and efficient method for the reduction of α,β-unsaturated carboxylic esters to allylic alcohols utilizing LiAlH4/BnCl is described. Various α,β-unsaturated esters, including the coumarins bearing α,β-unsaturated lactone skeleton, can be converted smoothly into their corresponding allylic alcohols in high yields under mild conditions with short reaction times.
Histamine H3-receptor ligands and their therapeutic application
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Page/Page column 17, (2010/11/24)
The present patent application concerns new compounds of formula (I) with R 1 and R 2 taken together with the nitrogen atom to which they are attached, form a saturated nitrogen-containing ring, A is a saturated C1-4 alkylene and B a C3-4 alkylene or alkenylene chain; their preparation and their use as a H3 receptor ligand for treating e.g. CNS disorders like Alzheimer's disease.
Highly Efficient and Convenient Deprotection of Methoxymethyl Ethers and Esters Using Bismuth Triflate in an Aqueous Medium
Venkat Reddy,Jagadeeshwar Rao,Sampath Kumar,Madhusudana Rao
, p. 1038 - 1039 (2007/10/03)
A simple and efficient method has been developed for the hydrolysis of methoxymethyl (MOM) ethers and esters to the corresponding alcohols and acids employing a catalytic amount of bismuth triflate in an aqueous medium. The conversions occur at ambient temperature and the yields of the deprotected alcohols are very good. The reaction was highly selective in the presence of other protecting groups such as TBDMS, TBDPS, benzyl, and allyl ethers.
A new approach for synthesis of erythro 8-0-4′ neolignans
Chen, XiaoChuan,Gu, WenXin,Jing, XiaoBi,Pan, XinFu
, p. 557 - 564 (2007/10/03)
Erythro- 1-(4-hydroxy-3-methoxyphenyl)-2- (4-formyl-2-methoxy-phenoxy)-propane-1,3-diol, a 8-0-4′ norneolignan, has been stereoselectively synthesized in eight steps from ferulic acid. In this new route to prepare erythro 8-0-4′ neolignans the cis addition of mCPBA to a double bond with high regioselectivity was a key step, and its mechanism is discussed.
