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Microwave-assisted synthesis and in vitro antibacterial activity of novel steroidal thiosemicarbazone derivatives.

Abstract：

:Herein, we reported the synthesis of 16 novel steroidal thiosemicarbazone derivatives via the condensation of steroidal ketones and substituted thiosemicarbazides under solvent-free conditions using microwave irradiation. The yields obtained are in the range of 84-96% using microwave method and 46-62% using conventional method. All the synthesized compounds (7a-p) have been characterized by (1)H NMR, ESI-MS, IR and elemental analyses. All the series compounds (7a-p) were evaluated for their antibacterial activity against and the results were compared with the standard drug Amoxicillin. Some of the compounds from the series like 7c, 7o and 7p were equipotent with Amoxicillin against Pseudomonas aeruginosa. Also compound 7h was better than Amoxicillin against Staphylococcus aureus and Bacillus subtilis.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Zhao Z,Shi Z,Liu M,Liu X

doi

10.1016/j.bmcl.2012.09.083

subject

Has Abstract

pub_date

2012-12-15 00:00:00

pages

7730-4

issue

24

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(12)01238-3

journal_volume

22

pub_type

杂志文章

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