Methimazole-Related Substances: Structural Characterization and In Silico Toxicity Assessment

The continuous tightening of pharmaceutical regulations forces drug manufacturers to unambiguously characterize the substances related to the active pharmaceutical ingredients (API). Here, we report the synthesis, complete spectroscopic, chromatographic, thermal and computational characterization, as well as in silico prediction of bacterial mutagenicity for two previously reported but never fully characterized impurities of methimazole. Additionally, their structures were analyzed by single-crystal X-ray diffraction. 1-Methyl-(2-methylthio)-1H-imidazole also known as methimazole impurity C, was obtained mainly in the form of the iodide salt (C5H9IN2S) crystallizing in monoclinic space group P21/c. The disulfide (2,2′-disulphanylbis(1-methyl-1H-imidazole)), C8H10N4S2) was obtained in yellow form crystallizing in the monoclinic C2/c space group.

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Publication Details

Journal
Crystals
Published
2024-12-12
DOI
https://doi.org/10.3390/cryst14121073
Primary Topic
Analytical Chemistry and Chromatography
Type
article
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article

Methimazole-Related Substances: Structural Characterization and In Silico Toxicity Assessment

Ana Čikoš, Leo Štefan, Robert Vianello, Lara Saftić Martinović et al.
Crystals
Analytical Chemistry and Chromatography
article

Methimazole-Related Substances: Structural Characterization and In Silico Toxicity Assessment

Ana Čikoš, Leo Štefan, Robert Vianello, Lara Saftić Martinović, Ivica Đilović
article en

Abstract

The continuous tightening of pharmaceutical regulations forces drug manufacturers to unambiguously characterize the substances related to the active pharmaceutical ingredients (API). Here, we report the synthesis, complete spectroscopic, chromatographic, thermal and computational characterization, as well as in silico prediction of bacterial mutagenicity for two previously reported but never fully characterized impurities of methimazole. Additionally, their structures were analyzed by single-crystal X-ray diffraction. 1-Methyl-(2-methylthio)-1H-imidazole also known as methimazole impurity C, was obtained mainly in the form of the iodide salt (C5H9IN2S) crystallizing in monoclinic space group P21/c. The disulfide (2,2′-disulphanylbis(1-methyl-1H-imidazole)), C8H10N4S2) was obtained in yellow form crystallizing in the monoclinic C2/c space group.

CrystalsVol. 14(12)
University of Rijeka (HR), University of Zagreb (HR), Ruđer Bošković Institute (HR)
Clean water and sanitation
Openalex Percentile: Top 82%
Analytical Chemistry and Chromatography
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Methimazole-Related Substances: Structural Characterization and In Silico Toxicity Assessment — Ana Čikoš, Leo Štefan, et al. · Crystals (2024) | TGRS Research Map | TGRS