引用本文:
Xiu Jie Liu, Xin He, Cheng Ling Shi, Jie Meng, Ying Lu Shao, Hong Qiang Si, Tao Hu. Synthesis and in vitro activities on anti-platelet aggregation of N,N'-di(2-substituted-phenyl)-4-methoxyisophthalamides and benzene-1,3-disulfonamides[J]. Chinese Chemical Letters,
2011, 22(10): 1139-1142.
doi:
10.1016/j.cclet.2011.05.032
Citation: Xiu Jie Liu, Xin He, Cheng Ling Shi, Jie Meng, Ying Lu Shao, Hong Qiang Si, Tao Hu. Synthesis and in vitro activities on anti-platelet aggregation of N,N'-di(2-substituted-phenyl)-4-methoxyisophthalamides and benzene-1,3-disulfonamides[J]. Chinese Chemical Letters, 2011, 22(10): 1139-1142. doi: 10.1016/j.cclet.2011.05.032
Citation: Xiu Jie Liu, Xin He, Cheng Ling Shi, Jie Meng, Ying Lu Shao, Hong Qiang Si, Tao Hu. Synthesis and in vitro activities on anti-platelet aggregation of N,N'-di(2-substituted-phenyl)-4-methoxyisophthalamides and benzene-1,3-disulfonamides[J]. Chinese Chemical Letters, 2011, 22(10): 1139-1142. doi: 10.1016/j.cclet.2011.05.032
Synthesis and in vitro activities on anti-platelet aggregation of N,N'-di(2-substituted-phenyl)-4-methoxyisophthalamides and benzene-1,3-disulfonamides
摘要:
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.
English
Synthesis and in vitro activities on anti-platelet aggregation of N,N'-di(2-substituted-phenyl)-4-methoxyisophthalamides and benzene-1,3-disulfonamides
Abstract:
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.
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Key words:
- Synthesis
- / Anti-platelet aggregating
- / Isophthalamides
- / Benzene-1
- / 3-Disulfonamides
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