期刊
CRYSTAL GROWTH & DESIGN
卷 13, 期 5, 页码 2208-2219出版社
AMER CHEMICAL SOC
DOI: 10.1021/cg400322t
关键词
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资金
- UGC
- Council of Scientific and Industrial Research (Pharmaceutical Cocrystals project) [(01/2410)/10/EMR-II]
- University Grants Commission (UGC-PURSE grant)
- Department of Science and Technology [SR/S2/JCB-06/2009]
Temozolomide (TMZ) is an antitumor prodrug of broad spectrum antineoplastic activity. TMZ is stable in efforts to design stable in acidic medium (pH < 4) but starts to decompose at alkaline pH (>7). In continuation of our crystals of TMZ with partners such as organic acids (pK(a) 2-5) and a salt dihydrate with hydrochloric acid, we report herein TMZ cocrystals with amide coformers, e.g., isonicotinamide, nicotinamide, pyrazinamide, p-hydroxybenzamide, saccharin, and caffeine. TMZ exhibits polymorphs in the p-hydroxybenzamide cocrystal (synthon polymorphism). The occurrence of the stable conformation A of temozolomide and metastable conformation B (energy difference 1.44 kcal mol(-1)) in amide cocrystals is compared with the overall statistics in temozolomide cocrystal structures and polymorphs. The novel cocrystals were characterized by spectroscopic, X-ray diffraction, and thermal methods.
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