دورية أكاديمية
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Synthetic modifications of abietane diterpene acids to potent antimicrobial agents.

التفاصيل البيبلوغرافية
العنوان: Synthetic modifications of abietane diterpene acids to potent antimicrobial agents.
المؤلفون: Smirnova IE; Ufa Institute of Chemistry of the Ufa Federal Research Centre of the Russian Academy of Sciences, Ufa, Russian Federation., Tret'yakova EV; Ufa Institute of Chemistry of the Ufa Federal Research Centre of the Russian Academy of Sciences, Ufa, Russian Federation., Baev DS; N.N. Vorozhtsov Novosibirsk Institute of Organic Chemistry of Siberian Branch of Russian Academy of Sciences, Novosibirsk, Russian Federation., Kazakova OB; Ufa Institute of Chemistry of the Ufa Federal Research Centre of the Russian Academy of Sciences, Ufa, Russian Federation.
المصدر: Natural product research [Nat Prod Res] 2023 Jan; Vol. 37 (2), pp. 313-321. Date of Electronic Publication: 2021 Aug 27.
نوع المنشور: Journal Article
اللغة: English
بيانات الدورية: Publisher: Taylor & Francis Health Sciences Country of Publication: England NLM ID: 101167924 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1478-6427 (Electronic) Linking ISSN: 14786419 NLM ISO Abbreviation: Nat Prod Res Subsets: MEDLINE
أسماء مطبوعة: Original Publication: Milton Park, UK : Taylor & Francis Health Sciences, c2003-
مواضيع طبية MeSH: Methicillin-Resistant Staphylococcus aureus* , Anti-Infective Agents*/pharmacology , Cryptococcus neoformans* , Mycobacterium tuberculosis*, Humans ; Abietanes/pharmacology ; HEK293 Cells ; Antifungal Agents/pharmacology ; Microbial Sensitivity Tests ; Anti-Bacterial Agents/pharmacology
مستخلص: 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 H 37 Rv 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 H 37 Rv with MIC of 1.25 µg/mL. The docking studies suggest possible interactions of the leading compounds with the molecular targets.
فهرسة مساهمة: Keywords: Dihydroquinopimaric acid; M. tuberculosis H37Rv; antifungal activity; antimicrobial activity; antitubercular activity; docking studies; maleopimaric acid
المشرفين على المادة: 0 (Abietanes)
0 (Anti-Infective Agents)
0 (Antifungal Agents)
0 (Anti-Bacterial Agents)
تواريخ الأحداث: Date Created: 20210827 Date Completed: 20230109 Latest Revision: 20230111
رمز التحديث: 20231215
DOI: 10.1080/14786419.2021.1969566
PMID: 34448419
قاعدة البيانات: MEDLINE
الوصف
تدمد:1478-6427
DOI:10.1080/14786419.2021.1969566