화학요법제 합성연구 II

Synthetic Studies on Chemotherapeutic Agents II

Fourteen novel N,N'' - disubstituted thiourea derivatives were synthesized by Hugersbof reaction. Antitubercular activities of ten compounds against Mycobacterium tuberculosis H37Rv were tested and was found that 1-cyclohexyl-3-(4-benzenesulfonepiperidide)-2-thiourea was considerably active at 1mg/ml and 1-alpha-naphthyl-3-(4-benzenesulfonepiperidide)-2-thiourea was slightly active at 1mg/ml. Antibacterial activity of the newly synthesized compounds against E.coli, Sta. aureus and Streptococcus hemolyticus were also tested. 1-cyclohexyl-3-(4-benzenesulfonepiperidide)-2-thiourea was makedly active against E. coli, Sta. aureus and Streptococcus hemolyticus: Phenol coefficients against E. coli, Sta. aureus and Streptococcus hemolyticus were 30, 17.5 and 21.3, respectively. 1, 1''-p-phenylene-3, 3''bis [N - (2-thiazolyl)-sulfamylphenyl)-2,2''-dithiourea and 1-alpha-naphthyl-3-(4-benzenesulfonepiperidide)-2-thiourea were considerably active against E.coli: phenol coefficients, 18.8 and 37.5 respectively. 1-(4-ethoxyphenyl)-3-(4-sulfamylphenyl)-2-thiourea was active against Streptococcus hemolyticus: phenol coefficients, 22.5. 1-alpha-naphthyl-3-(4-sulfamylphenyl)-2-thiourea, 1-beta-naphthyl-3-[4-N-(2-thiazolyl)-sulfamylphenyl]-2-thiourea and 1-alpha-naphthyl-3-(4-benzenesulfonepiperidide)-2-thiourea were active aganist Sta. aureus: phenol coefficients, 17.5, 20.0 and 18.8 respectively.