Abstract

Synthesized N-(7-R)-2-oxa-8-azabicyclo[4.2.0]octan-8-yl)isonicotinamide derivatives (4a-n) and N-(2,4-dioxo-3-oxa-6-azabicyclo[3.2.0]heptan-6-yl)isonicotinamide derivatives (5a-m) were screened for biologically activity. Both azetidine derivatives (4a-n) and (5a-m) were screened for antibacterial activity by ‘Disk Diffusion method’ using Escherichia coli (ATCC 25922), Pseudomonas aeruginosa (ATCC 27853) and Staphylococcus aureus (ATCC 25923) and antifungal activity using candida sp. Similar series of azetidine derivatives (4a-n) and (5a-m) were screened for in vitro antituberculosis activity by ‘Clairo Combi method’ using Mycobacterium tuberculosis and in vitro anti-inflammatory activity was evaluated using ‘HRBC membrane stabilization method’. Experimented azetidine derivatives excellent biological activities, (N-(7-R)-2-oxa-6-azabicyclo [3.2.0] heptan-6-yl) isonicotinamide derivatives (4a-n) against S. aureus bacteria and N-(2,4-dioxo-3-oxa-6-azabicyclo[3.2.0] heptan-6-yl) isonicotinamide derivatives (5a-m) against M. tuberculosis (T.B.). Both series of azetidine derivatives (4a-n) and (5a-m) show potent anti-inflammatory activity. All synthesized azetidine derivatives (4a-n) and (5a-m) were characterized by IR, ¹H NMR, 13C NMR and elemental analysis.

摘要

合成 N-(7 - R )-2-oxa-8-azabicyclo[4.2.0]octan-8-yl)isoicotinamide 衍生物 ( 4a-n ) 和 N-(2,4-dioxo-3-oxa-6-对氮杂双环[3.2.0]庚烷-6-基）异烟酰胺衍生物（5a-m）的生物活性进行了筛选。使用大肠杆菌 ( ATCC 25922)、铜绿假单胞菌 ( ATCC 27853) 和金黄色葡萄球菌 ( ATCC 25923)通过“磁盘扩散法”筛选氮杂环丁烷衍生物 ( 4a-n ) 和 ( 5a-m ) 的抗菌活性，并使用念珠菌属 在体外筛选了类似系列的氮杂环丁烷衍生物 (4a-n) 和 (5a-m)使用结核分枝杆菌的“Clairo Combi 方法”的抗结核活性和使用“HRBC 膜稳定方法”评估体外抗炎活性。实验的氮杂环丁烷衍生物具有优异的生物活性，(N-(7-R)-2-oxa-6-azabicyclo [3.2.0] heptan-6-yl) 异烟酰胺衍生物 ( 4a-n ) 对金黄色葡萄球菌和 N-( 2,4-dioxo-3-oxa-6-azabicyclo[3.2.0] heptan-6-yl) isonicotinamide 衍生物 ( 5a-m )抗结核分枝杆菌(TB)。氮杂环丁烷衍生物系列 ( 4a-n ) 和 ( 5a-m ) 均显示出有效的抗炎活性。所有合成的氮杂环丁烷衍生物 ( 4a-n) 和 ( 5a-m ) 通过 IR、¹ H NMR、 13C NMR 和元素分析表征。