Synthesis and biological evaluation of new aryl substituted Schiff’s bases

V. Parcha, J. Kaur
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引用次数: 1

Abstract

Objective : Chemical substances employed to treat various infections caused by various types of microorganism are termed as antimicrobials and natural chemical compounds produced by specific types of bacteria are termed as antibiotics. Unlimited use of antibiotics in humans and animals and in areas other than the treatment and prophylaxis of disease have resulted in a serious problem of drug resistance. Various attempts have been adopted to cope with the resistance problem and enhance the activity, or broaden the spectrum of drugs . Based on structure-activity relationship synthesis of new compounds has been one of the best approaches for better results. It has been demonstrated that Schiff base of some leading molecules and antibiotics possess good potential as more effective and safe drugs. Encouraged by reports on potential of Schiff’s bases as antimicrobial agents and to cope up with the current requirements of developing newer, safer and broad spectrum agents attempts were made to synthesize new Schiff’s bases. Methods : Our earlier in which structure activity relationship studies revealed that substitution by nitro and amino gp in Schiff’s base moiety resulted in the enhancement of activity. So further attempts were made to extend the series with incorporation of nitro and amino moiety by condensing o,m dinitro substituted acid hydrazide with various nitro/amino substituted benzaldehydes for increasing their antimicrobial potential. Results : Synthesized compounds were characterized on the basis of spectral studies (like UV, IR, and NMR). All the synthesized derivatives were screened further for their antibacterial effect. All the synthesized derivatives were screened further for their antibacterial effect. Conclusions : Highest activity was observed in the derivative with nitro substitution in both the aryl rings.
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新的芳基取代席夫碱的合成及生物学评价
目的:用于治疗由各种微生物引起的各种感染的化学物质称为抗菌剂,由特定类型的细菌产生的天然化合物称为抗生素。在人类和动物身上以及在治疗和预防疾病以外的领域无限制地使用抗生素,造成了严重的耐药性问题。已经采取了各种尝试来应对耐药性问题,提高药物的活性,或拓宽药物的范围。基于构效关系合成新化合物已成为获得较好效果的最佳途径之一。研究表明,一些先导分子和抗生素的希夫碱具有成为更有效、更安全的药物的良好潜力。受到希夫碱作为抗菌剂潜力的报道的鼓舞,以及为了适应开发更新、更安全、广谱抗菌剂的当前要求,人们尝试合成新的希夫碱。方法:我们早期的结构活性关系研究表明,在希夫碱基上取代硝基和氨基gp可以提高活性。因此,进一步尝试通过与各种硝基/氨基取代的苯甲醛缩合o,m二硝基取代的酸肼,以增加其抗菌潜力,以加入硝基和氨基部分来扩展该系列。结果:合成的化合物在光谱研究(如紫外、红外和核磁共振)的基础上进行了表征。对所有合成的衍生物进行了进一步的抗菌效果筛选。对所有合成的衍生物进行了进一步的抗菌效果筛选。结论:两个芳基环上都有硝基取代的衍生物活性最高。
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