Pyridine N-oxides as coformers in the development of drug cocrystals

作者: Basanta Saikia , Rajiv Khatioda , Pranita Bora , Bipul Sarma

DOI: 10.1039/C6CE01838F

关键词: Hydrogen bondChemistryFerulic acidPyridineActive ingredientSupramolecular chemistryCocrystalSynthonOrganic chemistryCrystal structure

摘要: Pyridine N-oxides were synthesized via a convenient method and exploited in the preparation of drug cocrystals. Drugs associated with aqueous solubility issues such as propofol, ferulic acid, sulfathiazole, p-aminobenzoic acid etc. used representative active ingredients to engineer pharmaceutical solids desired phase. In this study, 4,4′-bipyridine-N,N′-dioxide was picked cocrystal former. The types supramolecular heterosynthons exhibited by binary systems N-oxide·drugs analyzed. formation hydrogen bond synthons COOH–pyridine N-oxide, OH or NH–pyridine N-oxide found be robust followed trend observed Crystal Structure Database. These further correlated ameliorated properties drugs, which supported experiments, DFT studies Hirshfeld surface analysis. This has been goal development.

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