title: 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.
authors.affiliation: College of Chemistry and Environmental Protection Engineering, Southwest University for Nationalities, Chengdu 610041, PR China. zzg63129@yahoo.com.cn
authors.forename: Zhigang
authors.initials: Z
authors.lastname: Zhao
authors.forename: Zhichuan
authors.initials: Z
authors.lastname: Shi
authors.forename: Min
authors.initials: M
authors.lastname: Liu
authors.forename: Xingli
authors.initials: X
authors.lastname: Liu
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001412:Bacillus subtilis / Q000187:drug effects*; D004305:Dose-Response Relationship, Drug; D008826:Microbial Sensitivity Tests; D008872:Microwaves; D015394:Molecular Structure; D011550:Pseudomonas aeruginosa / Q000187:drug effects*; D013211:Staphylococcus aureus / Q000187:drug effects*; D013256:Steroids / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013882:Thiosemicarbazones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000900:Anti-Bacterial Agents; D013256:Steroids; D013882:Thiosemicarbazones