Design, synthesis of novel N, N'-bis-(halogenophenyl)-4- methoxybenzene-1, 3-disulfonamides and evaluation of their anti-platelet aggregation activity.
- Author:
Gui-Ang LI
;
Xiao WANG
;
Xia MENG
;
Yong-Bin LIN
;
Xu LI
;
Xiu-Jie LIU
- Publication Type:Journal Article
- MeSH:
Adenosine Diphosphate;
Drug Design;
Phthalic Acids;
Platelet Aggregation;
Platelet Aggregation Inhibitors;
chemical synthesis;
chemistry;
Structure-Activity Relationship;
Sulfonamides;
chemical synthesis;
chemistry
- From:
Acta Pharmaceutica Sinica
2015;50(2):185-190
- CountryChina
- Language:Chinese
-
Abstract:
Combining the structural features of picotamide and linotroban, a series of N,N'-bis-(halogenophenyl)-4-methoxybenzene-1, 3-disulfonamides were designed and synthesized on the basic principles of drug design. The structures of target compounds were confirmed by IR, 1H NMR and HR-MS, and the in vitro antiplatelet aggregation activity was evaluated by Born turbidimetric method with adenosine diphosphate (ADP) as the platelet aggregation inducers. The assay results showed that twelve compounds (4b, 4f, 4l, 5b, 5d-5g, 5j, 5k, 5m and 5n) were found to have superior anti-platelet aggregation activities than the positive drug picotamide. The preliminary structure-activity relationship (SAR) has been explored.
