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Design, synthesis and in vitro activities on anti-platelet aggregation of 4-methoxybenzene-1,3-isophthalamides
- Source :
- Bioorganic & Medicinal Chemistry Letters. 22:6591-6595
- Publication Year :
- 2012
- Publisher :
- Elsevier BV, 2012.
-
Abstract
- 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, (1)H 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.
- Subjects :
- Blood Platelets
Magnetic Resonance Spectroscopy
Platelet Aggregation
Stereochemistry
Clinical Biochemistry
Phthalic Acids
Pharmaceutical Science
Phthalimides
Biochemistry
Inhibitory Concentration 50
Drug Delivery Systems
Drug Discovery
medicine
Animals
Picotamide
Molecular Biology
Dose-Response Relationship, Drug
Chemistry
Organic Chemistry
Reference drug
Anti platelet
In vitro
Rats
Design synthesis
Drug Design
Proton NMR
Molecular Medicine
Platelet Aggregation Inhibitors
medicine.drug
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 22
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....eab5fb7467bd0d8f25bbe2868b4cd943