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In this study, 17 new unreported pyrrolidine derivatives 5a-5p, 6awere synthesized in a fully synthetic manner using the FDA-approved drug captopril as the basic structure, and the antimicrobial activity was tested in vitro against clinically isolated Klebsiella pneumoniae carrying the New Delhi metal beta lactamase (NDM-1) gene and Gram-negative E. coli carrying the Klebsiella pneumoniae carbacyticase-2 (KPC-2) gene. The results showed that 5jcould reduce the minimum inhibitory concentration (MIC) of meropenem (MEM) against clinically isolated Klebsiella pneumoniae containing NDM-1 to 32 μg·mL-1, which was better than that of the positive drug captopril; 5l, 5m, and 5oreduce the MIC of MEM against KPC-2-containing Gram-negative E. coli to 2 μg·mL-1, which was better than that of the positive drug captopril; the virtual molecular docking results of some pyrrolidine derivatives suggested the possible binding mode of pyrrolidine derivatives to NDM-1 and KPC-2.
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| 科 Family | 属数 Number of genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) | 属 Genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) |
|---|---|---|---|---|---|---|
| 鹅膏菌科Amanitaceae | 2 | 11 | 5.26 | 鹅膏菌属 Amanita | 10 | 4.78 |
| 小菇科 Mycenaceae | 2 | 12 | 5.74 | 丝盖伞属 Inocybe | 5 | 2.39 |
| 多孔菌科 Polyporaceae | 8 | 14 | 6.70 | 蜡蘑属 Laccaria | 5 | 2.39 |
| 红菇科 Russulaceae | 3 | 23 | 11.00 | 小皮伞属 Marasmius | 6 | 2.87 |
| 小菇属 Mycena | 11 | 5.26 | ||||
| 光柄菇属 Pluteus | 5 | 2.39 | ||||
| 红菇属 Russula | 17 | 8.13 | ||||
| 栓菌属 Trametes | 5 | 2.39 |
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