Synthetic Chemotherapeutic Agents. II. Synthesis of 2-Substituted Thiazolo [5, 4-f] quinoline Derivatives. (2)
1976 年 24 巻 1 号 p. 136-146
詳細
1976 年 24 巻 1 号 p. 136-146
In order to search for new antimicrobial agents, a number of 2-substituted 6-ethyl-6, 9-dihydro-9-oxothiazolo [5, 4-f] quinoline-8-carboxylic acids were prepared. Nucleophilic reactions of the 2-methylsulfonyl derivative (6 or 13) gave the 2-alkoxy (12), 2-cyano (14), 2-amino (15 and 19) and other derivatives. By using the 2-cyano compound (3 or 14), various derivatives were also prepared, e.g., the 2-amidine (24h), 2-imido-ether (27), 2-carbamoyl (26 and 30) and other derivatives. Formation of the 9-ethoxy compound (33) by ethylation of the 8-decarboxylated compound (34) was also described. These compounds obtained were tested for their antimicrobial activities in vitro. The 2-cyano (14), 2-carbamoyl (26), 2-diethylaminoethylcarbamoyl (30f) and some other derivatives showed the stronger activities than nalidixic acid. The most active compound, 30f, exhibited the activities against Escherichia coli resistant to nalidixic acid, but had no activity against Ps. aeruginosa.
