Journal of Medicinal Chemistry p. 1042 - 1049 (1983)
Update date:2022-08-04
Topics:
Grehn
Ragnarsson
Eriksson
Oberg
Several new analogues of the antiviral antibiotic distamycin A were synthesized and assayed for their effects on influenza and herpes simplex virus. The new compounds 5b-j (R1-3 = H, CH3, and C2H5, R(4,5) = H and CH3) were obtained via stepwise prepared formylated trimeric benzyl 4-aminopyrrole-2-carboxylates 3a-h, which after catalytic hydrogenolysis were coupled as N-succinimidyl esters directly with the proper β-aminopropionamidine, unsubstituted or substituted with one or two methyl groups in the aminidine function. Most of the new analogues did not exhibit significant effects on the viruses studied, but three compounds (5f-h) displayed activity on herpes virus as demonstrated in plaque formation and virus yield assays. Elevated cytotoxicity was simultaneously observed for 5g and 5h. For compound 5f, a partial separation of antiherpes activity and cytotoxicity was accomplished. The differences in antiherpes activity did not correspond to the differences in the inhibition of herpes virus DNA polymerase.
View MoreContact:0086-22-23410962
Address:17-201, Ningfuli, Shuishanggongyuandong road,Nankai district, Tianjin, China
Jinhua City Mingzhu Pharmaceutical Co.,Ltd.
Contact:15857995878 0579-82207761
Address:No.169 Shenze Road, New Area,Jinpan Development Zone, Jinhua
Contact:0512-62706911
Address:No.289 Yinzhong South Road Wuzhong Economic Development District,Suzhou,China
Shanghai Yuanding Chem. Sci. & Tech. Co., Ltd.
website:http://www.shydtec.com
Contact:86-21-57721279
Address:Science and Technology Park, Songjiang District, Shanghai, China
Jiangsu Chiatai Qingjiang Pharmaceutical Co.,Ltd
Contact:+86-517-86283327
Address:9 North Hantai Road, Huaian, China
Doi:10.1021/ic800294c
(2008)Doi:10.1007/BF00819968
(1993)Doi:10.1039/jr9380000401
(1938)Doi:10.1007/BF00513253
(1983)Doi:10.1002/chem.201603630
(2016)Doi:10.1055/s-2006-950423
(2006)