1029441-03-9Relevant academic research and scientific papers
Design, synthesis and in vitro activities on anti-platelet aggregation of 4-methoxybenzene-1,3-isophthalamides
Liu, Xiu Jie,Shi, Xin Xin,Zhong, Yong Liang,Liu, Ning,Liu, Kai
, p. 6591 - 6595,5 (2012/12/12)
On the purpose of searching for the structure-activity relationship (SAR) and obtaining novel anti-platelet drugs, 41 4-methoxybenzene-1,3-isophthalamides have been described the synthesis process and in vitro activities on anti-platelet aggregation. The target compounds have been classified into four series: series 1 (ortho-substituted phenyl: 1a-1j), series 2 (meta-substituted phenyl: 2a-2k), series 3 (para-substituted phenyl: 3a-3l) and series 4 (aromatic of no substituted group and aromatic heterocyclic substituted groups: 4a-4h). The chemical structures of the target compounds were confirmed by MS, IR, 1H NMR, and their in vitro activities on anti-platelet aggregation were tested and assessed by using Born test. The result showed that thirteen compounds 1c, 1d, 1i, 1j, 2g, 3a, 3c, 3d, 3f, 3h, 3l, 4b and 4c have superior anti-platelet aggregation activities than the reference drug Picotamide.
Synthesis and in vitro activities on anti-platelet aggregation of N,N′-di(2-substituted-phenyl)-4-methoxy isophthalamides and benzene-1,3-disulfonamides
Liu, Xiu Jie,He, Xin,Shi, Cheng Ling,Meng, Jie,Shao, Ying Lu,Si, Hong Qiang,Hu, Tao
, p. 1139 - 1142 (2012/01/06)
On the propose of searching for the SAR and obtaining novel antiplatelet aggregating drugs, we have described the synthesis procedure and the activities in vitro on antiplatelet aggregation of two series of derivatives, which contain both 18 N,N′-di(2-substitutedphenyl)-4-methoxyisophthalamides (2a-2r) of the 2 series and nine N,N′-di(2-substitutedphenyl)-4-methoxybenzene-1,3- disulfonamides (3a-3i) of the 3 series. The results showed that three compounds 2e, 2i and 3g emerged as significant activities of antiplatelet aggregation, superior to two reference drugs picotamide and aspirin, and eight compounds 2j, 2k, 2l, 2o, 2p, 2q, 2r and 3i merely superior to picotamide. The preliminary SAR shows that it is favorable for the 2 series to increase the activities via the steric hindrance substituents attached to the two side chain benzene rings at 2-positions. And the arylamides of the 2 series have better the activity values than the arylsulfonamides of the 3 series respective except for 3b and 3g. On the contrary, electrostatic factors would not contribute evidently to the activities of the two series. The structures of 15 compounds newly synthesized have been established by MS and 1H NMR and been first reported in this paper.
