苯并二氧杂环戊烯部分的某些咪唑-缩氨基脲轭合物的合成与光谱鉴定：新型抗真菌剂。
Synthesis and Spectroscopic Identification of Certain Imidazole-Semicarbazone Conjugates Bearing Benzodioxole Moieties: New Antifungal Agents.
机构信息
Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia.
Department of Medicinal Chemistry, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt.
出版信息
Molecules. 2019 Jan 7;24(1):200. doi: 10.3390/molecules24010200.
During the last three decades the extent of life-threatening fungal infections has increased remarkably worldwide. Synthesis and structure elucidation of certain imidazole-semicarbazone conjugates ⁻ are reported. Single crystal X-ray analysis of compound unequivocally confirmed its assigned chemical structure and the ()-configuration of its imine double bond. Compound crystallized in the triclinic system, P-1, a = 6.3561 (3) Å, b = 12.5095 (8) Å, c = 14.5411 (9) Å, α = 67.073 (4)°, β = 79.989 (4)°, γ =84.370 (4)°, V = 1048.05 (11) ų, Z = 2. In addition, DIZ and MIC assays were used to examine the in vitro antifungal activity of the title conjugates ⁻ against four fungal strains. Compound , bearing a 4-ethoxyphenyl fragment, showed the best MIC value (0.304 µmol/mL) against both and species, while compounds (MIC = 0.311 µmol/mL), , and (MIC = 0.287 µmol/mL) exhibited the best anti- activity.
在过去的三十年中，全球范围内危及生命的真菌感染的程度显著增加。本文报道了某些咪唑-半卡巴腙缀合物的合成和结构阐明。化合物 的单晶 X 射线分析明确证实了其指定的化学结构和其亚胺双键的 ()-构型。化合物 结晶为三斜晶系，P-1，a = 6.3561 (3) Å，b = 12.5095 (8) Å，c = 14.5411 (9) Å，α = 67.073 (4)°，β = 79.989 (4)°，γ = 84.370 (4)°，V = 1048.05 (11) ų，Z = 2。此外，DIZ 和 MIC 测定用于检查标题缀合物 ⁻ 对四种真菌菌株的体外抗真菌活性。具有 4-乙氧基苯基片段的化合物 对 和 两种物种表现出最佳的 MIC 值（0.304 µmol/mL），而化合物 （MIC = 0.311 µmol/mL）、 、 和 （MIC = 0.287 µmol/mL）则表现出最佳的 抗真菌活性。
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