首页> 外文OA文献 >Theoretical Studies on eta -lactam Antibiotics. IV. Conformational Analysis of Novel eta -lactam Antibiotics and the Binding Specificities of Crosslinking Enzyme(s) and eta -lactamases

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Theoretical Studies on eta -lactam Antibiotics. IV. Conformational Analysis of Novel eta -lactam Antibiotics and the Binding Specificities of Crosslinking Enzyme(s) and eta -lactamases

机译：β-内酰胺类抗生素的理论研究。 IV。新型β-内酰胺类抗生素的构象分析以及交联酶和β-内酰胺酶的结合特异性

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Conformational-energy calculations were carried out on the new family of eta -lactam antibiotics (viz., thienamycin, PS-5, 1-oxa- and 1-thiapenems, and their close analogs); these exhibit broad-spectrum antibacterial activity and stability towards eta -lactamase-producing strains. The bicyclic ring system in all the compounds studied was found to be highly rigid and to favor only one conformation. This is in contrast to findings in penicillins, where the five-membered ring assumes two puckered conformations. The relative orientations of the bicyclic ring system and the nature and configuration of the substituent at C-5 position, besides nonplanarity of the lactam peptide bond, are shown to be important for biological activity. The present study, in agreement with x-ray studies, predicts that the lactam peptide bond in 1-carbapenem is more nonplanar than in 1-thiapenem. These studies also suggest that the conformational requirement of bicyclic ring system to bind to crosslinking enzyme(s) and eta -lactamases is very similar.

机译：对新的β-内酰胺类抗生素（即，噻菌霉素，PS-5、1-氧杂-和1-硫代培南，及其紧密类似物）进行构象能量计算。这些表现出广谱的抗菌活性和对产生β-内酰胺酶的菌株的稳定性。发现所有研究的化合物中的双环系统都是高度刚性的，并且仅支持一种构象。这与青霉素的发现相反，青霉素的五元环具有两个折叠的构象。除了内酰胺肽键的非平面性，双环系统的相对取向以及在C-5位的取代基的性质和构型对生物活性也很重要。本研究与X射线研究一致，预测1-carbapenem中的内酰胺肽键比1-thiapenem中更不平坦。这些研究还表明，双环系统结合交联酶和β-内酰胺酶的构象要求非常相似。

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Vasudevan TK; Rao VSR;
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年度 1981
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1. Prevalence of the genes encoding extended-spectrum beta-lactamases, in Escherichia coli resistant to beta-lactam and non-beta-lactam antibiotics. [J] . Matar GM, Al Khodor S, El Zaatari M, Annals of tropical medicine and parasitology . 2005,第4期

机译：编码广谱β-内酰胺酶的基因在大肠杆菌中对β-内酰胺和非β-内酰胺抗生素具有抗性。
2. Resistance of Klebsiella pneumoniae strains producing and not producing ESBL(extended-spectrum beta-lactamase) type enzymes to selected non-beta-lactam antibiotics. [J] . Maria Szymankiewicz, Marcin Wróblewski, Grazyna Janicka, Medical science monitor : . 2002,第9期

机译：产生和不产生ESBL（超广谱β-内酰胺酶）型酶的肺炎克雷伯菌菌株对所选非β-内酰胺类抗生素的抗性。
3. Crystal structure and activity studies of the Mycobacterium tuberculosis beta-lactamase reveal its critical role in resistance to beta-lactam antibiotics. [J] . Wang F, Cassidy C, Sacchettini JC Antimicrobial agents and chemotherapy. . 2006,第8期

机译：结核分枝杆菌β-内酰胺酶的晶体结构和活性研究揭示了其在抵抗β-内酰胺抗生素中的关键作用。
4. A FLUORESCEIN-LABELED BETA-LACTAMASE MUTANT FOR HIGH-THROUGHPUT SCREENING OF BACTERIAL BETA-LACTAMASES AGAINST BETA-LACTAM ANTIBIOTICS [C] . . 2005

机译：荧光素标记的β-内酰胺酶突变体，用于抗β-内酰胺的细菌β-内酰胺酶的高通量筛选
5. Novel beta-lactam antibiotics: Study of their mode of action against beta-lactam recognizing enzymes. [D] . Du, Ying. 1994

机译：新型β-内酰胺类抗生素：研究其对抗β-内酰胺识别酶的作用方式。
6. Chromosomal beta-lactamase of Klebsiella oxytoca a new class A enzyme that hydrolyzes broad-spectrum beta-lactam antibiotics. [O] . Y Arakawa, M Ohta, N Kido, 1989

机译：产酸克雷伯菌的染色体β-内酰胺酶一种新的A类酶可水解广谱β-内酰胺抗生素。
7. Theoretical Studies on eta -lactam Antibiotics. IV. Conformational Analysis of Novel eta -lactam Antibiotics and the Binding Specificities of Crosslinking Enzyme(s) and eta -lactamases [O] . Vasudevan TK, Rao VSR 1981

机译：β-内酰胺类抗生素的理论研究。 IV。新型β-内酰胺类抗生素的构象分析以及交联酶和β-内酰胺酶的结合特异性

Theoretical Studies on eta -lactam Antibiotics. IV. Conformational Analysis of Novel eta -lactam Antibiotics and the Binding Specificities of Crosslinking Enzyme(s) and eta -lactamases

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