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Salts of Antifolate Pyrimethamine with Isomeric Aminobenzoic Acids: Exploring Packing Interactions and
Karolina Cichocka1, Magdalena Zimnicka2, Karolina Kędra3
1Faculty of Mathematics and Natural Sciences, Cardinal Stefan Wyszyński University, 01-938 Warsaw, Poland.
This study explores new solid forms of pyrimethamine (PYR) by co-crystallizing it with aminobenzoic acids. Researchers identified novel solvated salts and characterized their properties, offering insights into drug formulation and molecular interactions.
Area of Science:
- Materials Science
- Pharmaceutical Chemistry
- Crystallography
Background:
- Pyrimethamine (PYR) is an established antiprotozoal drug.
- The 2,4-diaminopyrimidine scaffold is key to PYR's functionality.
- Developing novel solid forms can enhance drug properties.
Purpose of the Study:
- To synthesize and characterize new solid forms of pyrimethamine.
- To investigate co-crystallization of PYR with isomeric aminobenzoic acids.
- To understand molecular interactions in solution and solid states.
Main Methods:
- Solution crystallization was employed to form new PYR salts.
- Characterization included SC-XRD, FTIR, PXRD, TG, and DSC.
- ESI-MS was used to study solution-phase aggregation.
Main Results:
- Three new solvated salts of PYR were successfully formed.
- Detailed physicochemical properties of the new salts were elucidated.
- ESI-MS revealed various non-covalent aggregates in solution.
Conclusions:
- Novel pyrimethamine solvated salts were synthesized.
- The study provides insights into PYR-aminobenzoic acid interactions.
- Understanding aggregation aids in designing new drug formulations.
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