15849-57-7Relevant academic research and scientific papers
Synthesis and Inhibitory Effect of Some Indole-Pyrimidine Based Hybrid Heterocycles on α-Glucosidase and α-Amylase as Potential Hypoglycemic Agents
Badria, Farid A.,Atef, Saleh,Al-Majid, Abdullah Mohammed,Ali,Elshaier, Yaseen A. M. M.,Ghabbour, Hazem A.,Islam, Mohammad Shahidul,Barakat, Assem
, p. 1288 - 1297 (2019)
The Michael addition reaction of barbituric acid with chalcones incorporating the indole scaffold was achieved by using a highly efficient bimetallic Iron–palladium catalyst in the presence of acetylacetone (acac). This catalytic approach produced the desired products in a simple operation and low catalyst loading with acceptable yield of the new hybrids. All tested compounds were subjected for biological activity on α-glucosidase and α-amylase. The results revealed that all synthesized compounds exhibited very good activity against both enzymes when compared to positive control (acarbose). Moreover, compound 5o showed the best activity whereas its IC50 (μM) are 13.02+0.01 and 21.71+0.82 for α-glucosidase and α-amylase respectively. Both compounds 5o and 5l exhibited high similarity in binding mode and pose with amylase protein (4UAC). The obtained data may be used for developing potential hypoglycemic agents.
Synthesis of chalcones via domino dehydrochlorination/Pd(OAc)2-catalyzed Heck reaction
Guo, Tenglong,Jiang, Quanbin,Yu, Likun,Yu, Zhengkun
, p. 78 - 85 (2015/09/28)
A new method has been developed for the cross-coupling of aryl halides with β-chloroalkyl aryl ketones and their ester and amide analogs through a domino dehydrochlorination/Pd(OAc)2- catalyzed Heck reaction sequence. The enone intermediates generated in situ reduced the occurrence of side reactions and therefore enhanced the efficiency of the reaction. This reaction exhibited good tolerance to various functional groups on both substrates and provides rapid access to a wide range of chalcone derivatives.
Nitrones and Oxaziridines. XLII Synthesis of Indol-3-yl Substituted 1-Pyrroline 1-Oxides
Black, David St.C.,Deb-Das, Renu B.,Kumar, Naresh
, p. 611 - 621 (2007/10/02)
The 1-pyrroline 1-oxides (13), (14), (16) and (18) with indol-3-yl substituents attached to the 2- or 4-positions have been synthesized by reductive cyclization of the related γ-nitro ketones.The corresponding 1-pyrrolines (15), (17) and (19) have also be
