N-thiolated beta-lactams: a new family of anti-Bacillus agents.

Turos E; Long TE; Heldreth B; Leslie JM; Reddy GS; Wang Y; Coates C; Konaklieva M; Dickey S; Lim DV; Alonso E; Gonzalez J

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N-thiolated beta-lactams: a new family of anti-Bacillus agents.

机译：N-硫醇化β-内酰胺类：抗芽孢杆菌新药家族。

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This report describes the evaluation of N-thiolated beta-lactam antibiotics as potential anti-Bacillus agents. N-Thiolated beta-lactams are a new family of antibacterials that previously have been found to selectively inhibit the growth of Staphylococcus bacteria over many other genera of microbes. From the data presented herein, these lactams similarly inhibit a variety of Bacillus species, including Bacillus anthracis. The preliminary structure-activity studies suggest that there is a need to balance the lipophilic character of the C3/C4 groups in order to obtain optimal anti-Bacillus activity. Elongation or extensive branching of the organothio substituent diminishes antibacterial effects, with the sec-butylthio derivative providing the strongest activity.

机译：该报告描述了对N-硫醇化β-内酰胺类抗生素作为潜在抗芽孢杆菌药物的评估。 N-硫代β-内酰胺类是一个新的抗菌家族，以前发现它比许多其他微生物有选择地抑制葡萄球菌的生长。根据本文提供的数据，这些内酰胺类似地抑制多种芽孢杆菌属物种，包括炭疽芽孢杆菌。初步的结构活性研究表明，需要平衡C3 / C4基团的亲脂性以获得最佳的抗芽孢杆菌活性。有机硫取代基的伸长或广泛分支减弱了抗菌作用，其中仲丁硫基衍生物提供了最强的活性。

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来源
《Bioorganic and Medicinal Chemistry Letters》 |2006年第8期|共7页
作者
Turos E; Long TE; Heldreth B; Leslie JM; Reddy GS; Wang Y; Coates C; Konaklieva M; Dickey S; Lim DV; Alonso E; Gonzalez J;
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正文语种 eng
中图分类药学;生物化学;
关键词
Anti-Bacterial Agents; Bacillus; beta-Lactams; 芽孢杆菌属;

机译：Anti-Bacterial Agents;Bacillus;beta-Lactams;芽孢杆菌属;

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专利

1. N-thiolated beta-lactams: a new family of anti-Bacillus agents. [J] . Turos E, Long TE, Heldreth B, Bioorganic and Medicinal Chemistry Letters . 2006,第8期

机译：N-硫醇化β-内酰胺类：抗芽孢杆菌新药家族。
2. Induction of tumor cell apoptosis by a novel class of N-thiolated beta-lactam antibiotics with structural modifications at N1 and C3 of the lactam ring. [J] . Frezza M, Garay J, Chen D, International journal of molecular medicine . 2008,第6期

机译：新型内酰胺环N1和C3结构修饰的新型N-硫代β-内酰胺类抗生素诱导的肿瘤细胞凋亡。
3. N-Thiolated beta-lactam antibacterials: effects of the N-organothio substituent on anti-MRSA activity. [J] . Heldreth B, Long TE, Jang S, Bioorganic and medicinal chemistry . 2006,第11期

机译：N-硫代β-内酰胺类抗菌剂：N-有机硫取代基对抗MRSA活性的影响。
4. Identifying Beta-Lactam Resistance with Neural Networks [C] . Cory Kromer-Edwards, Jace Neubaum, Suely Oliveira, IEEE International Conference on Bioinformatics and Biomedicine . 2019

机译：用神经网络识别β-内酰胺抗性
5. Synthesis and Anti-MRSA Activity of Hydrophilic C3-Acylated N-Thiolated Beta-Lactams and N-Acyl Ciprofloxacin-N-Thiolated Beta-Lactam Hybrids. [D] . Bhattacharya, Biplob. 2012

机译：亲水性C3-酰化N-硫代β-内酰胺和N-酰基环丙沙星-N-硫代β-内酰胺杂化物的合成及抗MRSA活性。
6. Susceptibilities of beta-lactamase-positive and -negative strains of Campylobacter coli to beta-lactam agents. [O] . N Lachance, C Gaudreau, F Lamothe, 1993

机译：弯曲杆菌的β-内酰胺酶阳性和阴性菌株对β-内酰胺类药物的敏感性。
7. Susceptibilities of beta-lactamase-positive and -negative strains of Campylobacter coli to beta-lactam agents. [O] . Lachance, N, Gaudreau, C, Lamothe, F, 1993

机译：弯曲杆菌的β-内酰胺酶阳性和阴性菌株对β-内酰胺类药物的敏感性。
8. Examination of Potential Anti-Tumor Activity of N-Thiolated b-Lactam Antibiotics in Nude Mice Bearing Human Breast Tumors [R] . Dou, Q. P. 2006

机译：人乳腺肿瘤裸鼠体内N-硫醇化b-内酰胺类抗生素的潜在抗肿瘤活性检测

N-thiolated beta-lactams: a new family of anti-Bacillus agents.

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