Design, synthesis, and antimicrobial activity of some novel homodrimane sesquiterpenoids with diazine skeleton

被引：26

作者：

Kuchkova, Kaleria ^{[1
]}

Aricu, Aculina ^{[1
]}

Secara, Elena ^{[1
]}

Barba, Alic ^{[1
]}

Vlad, Pavel ^{[1
]}

Ungur, Nicon ^{[1
]}

Tuchilus, Cristina ^{[2
]}

Shova, Sergiu ^{[3
]}

Zbancioc, Gheorghita ^{[4
]}

Mangalagiu, Ionel I. ^{[4
,5
]}

机构：

[1] Moldavian Acad Sci, Inst Chem, Acad 3, MD-2028 Kishinev, Moldova

[2] Grigore T Popa Univ Med & Pharm Iasi, Iasi 700115, Romania

[3] P Poni Inst Macromol Chem, Iasi 700487, Romania

[4] Alexandru Ioan Cuza Univ, Dept Organ Chem, Iasi 700506, Romania

[5] Alexandru Ioan Cuza Univ, Dept Organ Chem, Iasi 700506, Romania

来源：

MEDICINAL CHEMISTRY RESEARCH | 2014年 / 23卷 / 03期

关键词：

Sesquiterpenoids; Homodrimane; Diazine; Antimicrobial; Design and synthesis; CONTAINING DRIMANE SESQUITERPENOIDS; TITHONIA-DIVERSIFOLIA; PHARMACOLOGICAL EVALUATION; ANTIINFLAMMATORY ACTIVITY; ANTIFUNGAL ACTIVITY; DERIVATIVES; PYRAZINE; INHIBITORS; ACID;

D O I：

10.1007/s00044-013-0720-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Herein we report a feasible study concerning the design, synthesis, and in vitro antimicrobial activity of some novel homodrimane sesquiterpenoids with diazine skeleton. The reaction pathway is efficient and straight, involving the direct N-acylation of diazine with homodrimane sesquiterpenoids bearing acyl chlorides or organic acids functionality. A reliable explication and a feasible reaction mechanism for the obtained compounds are presented. The in vitro antimicrobial activity of the homodrimane sesquiterpenoids with and without diazine skeleton has been evaluated. All the tested compounds have an excellent antibacterial activity against Gram-positive strains S. aureus and B. cereus. SAR correlations concerning antimicrobial activity are reported.

引用

页码：1559 / 1568

页数：10

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