Abstract:
:Nine novel acyl thioureas were synthesized. Their identities and purities were confirmed by LC-MS spectra; each structure was elucidated by elemental analysis, IR, 1 Н and 13 C NMR spectra. Applying an in vitro screening of their antifungal potential, three substances (3, 5, and 6) could be selected as showing high activity against 11 fungi and 3 Phytophthora strains of phytopathogenic significance. Analysis of gene toxicity with the Salmonella reverse mutagenicity test, as an assessment of drug likeness, lipophilicity, and calculations of frontier molecular orbitals assign a low toxicity profile to these compounds. Molecular docking studies point to 14α-demethylase (CYP51) and N-myristoyltransferase (NMT) as possible fungal targets for growth inhibition. The findings are discussed with respect to structure-activity relationship (SAR).
journal_name
Arch Pharm (Weinheim)journal_title
Archiv der Pharmazieauthors
Antypenko L,Meyer F,Kholodniak O,Sadykova Z,Jirásková T,Troianova A,Buhaiova V,Cao S,Kovalenko S,Garbe LA,Steffens KGdoi
10.1002/ardp.201800275subject
Has Abstractpub_date
2019-02-01 00:00:00pages
e1800275issue
2eissn
0365-6233issn
1521-4184journal_volume
352pub_type
杂志文章abstract::Three series of imidazolidinium ligands (NHC precursors) substituted with 4-vinylbenzyl, 2-methyl-1,4-benzodioxane, and N-propylphthalimide were synthesized. N-Heterocyclic carbene (NHC) precursors were prepared from N-alkylimidazoline and alkyl halides. The novel NHC precursors were characterized by 1 H NMR, 13 C NMR...
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journal_title:Archiv der Pharmazie
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