ペニシリン塩類の合成及び抗菌作用

抄録

4-Nitrosalicylic acid was acetylated and derived to its acid chloride, and this was condensed with 2-diethylaminoethanethiol to give 2-diethylaminoethyl 2-acetoxy-4-nitrobenzothiolate hydrochloride. Its reduction and deacetylation afforded the objective 2-diethylaminoethyl 2-hydroxy-4-aminobenzothiolate (IX). Condensation of 4-nitrosalicyloyl chloride and 2-diethylaminoethanethiol, and reduction of the nitro compound so produced also gave (IX), with better yield and by a simpler procedure than the former process. Antitubercular action of the hydrochloride of (IX) and its salts of penicillin G and V was examined in comparison with the oxyprocaine-penicillin G salt (I) of Grimme and others. It was found that the antitubercular activity of the penicillin G salt (II) and V salt (III) of (IX) was better than that of (I), and that penicillin V salt was less soluble in water.