合成,分子对接,和抗菌评价的2- ((替代氨基) -N- ((6-替代-1,3-Benzothiazol-2yl) 乙胺
Smita Pawar1, Amol Kale1, Priya Zori1
1Department of Pharmaceutical Chemistry, Pune District Education Association's Seth Govind Raghunath Sable College of Pharmacy, Saswad, Pune, 412 301, Maharashtra, India.
Current drug discovery technologies
|June 24, 2024
概括
新合成的西醇衍生物显示出强大的抗菌活性,与标准药物相比. 这些化合物,特别是BTC-j和BTC-r,作为新型抗菌剂,有望对抗日益增长的抗药性.
科学领域:
- 药用化学 医学化学
- 有机合成 有机合成
- 抗微生物药物发现发现
背景情况:
- 抗微生物耐药性需要不断开发新的抗微生物药物.
- 新兴的病原体和多药性耐药性强调迫切需要新的治疗策略.
研究的目的:
- 为了合成新的佐衍生物.
- 评估合成的化合物对它们对各种细菌和真菌菌株的抗菌潜力.
主要方法:
- 合成2 - 替代氨基) -N - 6 - 替代-1,3 - 二乙胺衍生物 (BTC) 的合成.
- 抗微生物查,包括抑制区和最小抑制度 (MIC) 的确定.
- 针对DNA回旋酶的分子对接研究 (PDB:3G75).
主要成果:
- 化合物BTC-j和BTC-r表现出显著的抗菌活性.
- BTC-j对*S. aureus*,*B. subtilis*,*E. coli*和*P. aeruginosa*具有强烈的活性,MIC值较低.
- 几种合成的化合物显示出与标准药物相比的抗微生物疗效.
结论:
- 成功合成了新型的佐衍生物,产量很好.
- 码头得分和观察到的抗微生物活性之间存在一致的相关性.
- 与乙胺结合的索衍生物是开发新抗菌剂的有希望的化合物.
相关概念视频
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Strong bases like NaOH or KOH deprotonate the phthalimide to form the corresponding anion, which acts as a nucleophile. Further, the anion attacks an...
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Subsequently, the amine acts as a nucleophile that attacks the acylating agent to form a tetrahedral intermediate. In the...
The DCC-promoted synthesis of amides begins with the protonation of DCC by carboxylic acid. The protonation makes it a better acceptor. Next, the addition of carboxylate to the protonated carbodiimide gives a reactive acylating agent.
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