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首页> 外文期刊>Current medicinal chemistry. Anti-infective agents >Bioisosters of beta-Lactams as Anti-Infectives
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Bioisosters of beta-Lactams as Anti-Infectives

机译：β-内酰胺的生物甾醇作为抗感染药

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Control of microbial growth, through inhibition of proteases including serine, cysteine and metalloproteases, has been a focus of both man and nature. Although beta-lactams have proven to be most successful in control of pathogens, their utility has become significantly limited as a result of development of antibiotic resistance, especially the production of extended spectrum (3-lactamases. Preparations of biologically active gamma- or delta-lactam mimics of penicillin, have led to the discovery of several types of bioisosters of (3-lactams, These mimics can not only exhibit antimicrobial activity, but similar to their beta-lactam parentage, they can also act as inhibitors of (3-lactamases. Both synthetic and naturally occurring gamma-lactams and beta-lactones also inhibit mammalian and viral enzymes, In addition to the beta-lactam analogs, several other classes of inhibitors, whose inhibitory mechanism is based on acylation of proteases have been developed.These include the heterocyclic inhibitors, such as isocoumarins, benzoxazinones, epoxides, sulfonamides, and pyrazolidinones. While acylation is the mechanism of choice for both these and (3-lactam inhibitors, alternative mechanisms for enzyme inhibition are described including alkylation and chelation, as in the case of metalloproteases. Novel approaches, including mimicking nature though the use of homoserine lactones is a new direction, which may aid in reduction of bacterial loads and inhibition of colonization. The focus of this review is to compare the various structure-function relationships of these non-beta-lactam mimics.
机译：通过抑制包括丝氨酸，半胱氨酸和金属蛋白酶在内的蛋白酶来控制微生物的生长已成为人类和自然界关注的焦点。尽管已证明β-内酰胺在控制病原体方面最为成功，但由于产生了抗生素抗性，尤其是产生了广谱光谱（3-内酰胺酶。具有生物活性的γ-或δ-青霉素的内酰胺模拟物已导致发现了多种类型的（3-内酰胺类）生物等效物。这些模拟物不仅具有抗菌活性，而且类似于其β-内酰胺类亲本，它们还可以作为（3-内酰胺酶的抑制剂合成的和天然存在的γ-内酰胺和β-内酯也都抑制哺乳动物和病毒酶，除了β-内酰胺类似物外，还开发了其他几种抑制剂，其抑制机理是基于蛋白酶的酰化作用，其中包括杂环抑制剂，例如异香豆素，苯并恶嗪酮，环氧化物，磺酰胺和吡唑烷酮。这些和（3-内酰胺抑制剂）描述了用于酶抑制的替代机制，包括烷基化和螯合，如在金属蛋白酶的情况下。通过使用高丝氨酸内酯来模仿自然等新方法是一个新的方向，它可能有助于减少细菌载量并抑制定植。这篇综述的重点是比较这些非β-内酰胺模拟物的各种结构-功能关系。

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