Synthetic Antibacterial Agents

N. Anand, W. Remers
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引用次数: 8

Abstract

Synthetic antibacterial compounds are divided into topical and systemic agents. Topical agents are called disinfectants or antiseptics depending on how they are used. They show little selectivity between the microbes and the host. Nevertheless, they are indispensable in hospitals, public health, and the home. The development of systemic antibacterial agents had a strong dye connection. Ehrlich's development of selective staining methods led him to propose that dyes may also have selective toxicity for microbes, and to coin the term chemotherapy. Domagk's discovery of antibacterial activity for the azo dye prontosil led to the first effective chemotherapeutic agent, sulfanilamide. This compound provided an excellent lead for structural modification and ushered in the modern era of chemotherapy and drug design. The discovery that sulfonamides act through folate inhibition resulted in the development of dihydrofolate reductase inhibitors such as trimethoprim. The availability of synthetic antibacterials and antibiotics, which were discovered almost concurrently, provided major advances in control of bacterial infections; however, the rise in bacterial resistance prompted the search for newer classes of agents. This search provided fluoroquinolines and oxazolidones. There are also synthetic antibacterials with niche needs, such as nitrofurans and methenamine, which are used for urinary tract infections. Keywords: antibacterial drug; dihydrofolate reductase inhibitors; sulfanilamide; synthetic antibacterial compounds; systemic agents; topical agents
合成抗菌剂
合成抗菌化合物分为外用和全身用。局部药物根据使用方式被称为消毒剂或防腐剂。它们在微生物和宿主之间几乎没有选择性。然而,它们在医院、公共卫生和家庭中是不可或缺的。全身性抗菌剂的开发与染料有很强的联系。埃利希对选择性染色方法的发展使他提出染料也可能对微生物具有选择性毒性,并创造了化疗这个术语。Domagk发现偶氮染料prontosil的抗菌活性,导致了第一种有效的化疗药物磺胺。这种化合物为结构修饰提供了一个很好的先导,并开创了化疗和药物设计的现代时代。磺胺类药物通过抑制叶酸发挥作用的发现导致了双氢叶酸还原酶抑制剂的开发,如甲氧苄啶。几乎同时发现的合成抗菌剂和抗生素的可用性在控制细菌感染方面取得了重大进展;然而,细菌耐药性的增加促使人们寻找新的药物。本研究提供了氟喹啉类药物和恶唑酮类药物。还有一些有特殊需求的合成抗菌药,如硝基呋喃和甲基苯丙胺,用于治疗尿路感染。关键词:抗菌药物;二氢叶酸还原酶抑制剂;磺胺;合成抗菌化合物;系统性的代理;局部代理
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