新型1,3,4-恶二唑异烟碱酰肼衍生物的合成、抑菌研究及ADME评价

Mazen Mohammed Jwaid, Karima Fadhil Ali, Mayada Hadi Abd-alwahab
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引用次数: 5

摘要

合成了含1,3,4-恶二唑药效团的新型异烟肼衍生物。利用红外光谱和核磁共振光谱对化合物的化学结构进行了表征和确认。采用琼脂孔扩散技术对所制备的化合物进行了抑菌实验,结果表明所制备的化合物对革兰氏阴性菌和革兰氏阴性菌均具有良好的抑菌活性。此外,使用瑞士ADME进行ADME评估,以预测合成的化合物是否可以口服,生物利用度,拓扑极性表面积和药物相似性。结果表明,所有化合物均可经口吸收,符合利平斯基规则。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Synthesis, Antibacterial study and ADME Evaluation of Novel Isonicotinoyl Hydrazide Derivative Containing 1,3,4-Oxadiazole Moiety
Novel derivative of isoniazid containing 1,3,4-oxadiazole pharmacophore has been synthesized. The chemical structure of the compound was characterized and confirmed by using FT-IR and 1H-NMR spectroscopy.   The desired compound was tested against gram-positive and gram-negative bacteria using agar well-diffusion technique for their ability as antibacterial agent and showed good antibacterial activity against gram-negative bacteria and gram-positive bacteria. In addition, ADME evaluations were performed using Swiss ADME to predict if the synthesized compound can be given orally, the bioavailability, topological polar surface area, and drug-likeness. The result showed that all tested compounds absorbed orally and fulfilled the Lipinski rule.
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