Synthetic modifications of abietane diterpene acids to potent antimicrobial agents.
Nat Prod Res
; 37(2): 313-321, 2023 Jan.
Article
em En
| MEDLINE
| ID: mdl-34448419
ABSTRACT
Among abietane type semisynthetic diterpenoids, a series of quinopimaric and maleopimaric acid derivatives modified at the carboxyl and carbonyl groups, and in ring E were synthesised to obtain new compounds with antimicrobial potency against Mycobacterium tuberculosis H37Rv and key ESKAPE pathogens. It was found that compound 8 exhibited low toxicity to human embryonic kidney cell line HEK-293 (> 32 µg/mL) and showed significant bacteriostatic activity against methicillin-resistant Staphylococcus aureus (MRSA) (MIC ≤ 0.25 µg/mL) and excellent antifungal activity against Cryptococcus neoformans var. grubii (MICs ≤0.25 µg/mL) being ≈4 and ≈30 fold more active than vancomycin and fluconazole. It also showed moderate activity against fungus Candida albicans (MIC ≤ 0.25 µg/mL). Compound 9 inhibited M. tuberculosis H37Rv with MIC of 1.25 µg/mL. The docking studies suggest possible interactions of the leading compounds with the molecular targets.
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Texto completo:
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Base de dados:
MEDLINE
Assunto principal:
Cryptococcus neoformans
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Staphylococcus aureus Resistente à Meticilina
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Anti-Infecciosos
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Mycobacterium tuberculosis
Limite:
Humans
Idioma:
En
Ano de publicação:
2023
Tipo de documento:
Article