Clyde D F, McCarthy V C, Rebert C C, Miller R M
Antimicrob Agents Chemother. 1973 Feb;3(2):220-3. doi: 10.1128/AAC.3.2.220.
WR 33063 (3-bromo-10-[alpha-hydroxy-beta-(n, n-diheptylamino)ethyl]-phenanthrene hydrochloride) and WR 30090 (6,8-dichloro-2,3,4-dichlorphenyl-di-n-butylaminoethyl-4- quinolinemethanol hydrochloride) were tested for suppressive prophylactic effect on induced malaria in nonimmune volunteers living in an area where malaria is not naturally transmitted. Doses of 800 mg of WR 33063 and 690 or 460 mg of WR 30090 were given at weekly intervals to men exposed on the day of the first dose to mosquitoes heavily infected with chloroquine- and pyrimethamine-resistant strains of Plasmodium falciparum. WR 33063 did not interfere with early development of infection, but WR 30090 given for 8 weeks provided suppressive cures in 20 of 26 men. P. vivax infections similarly induced broke through WR 30090 treatment in 4 of 15 men, and most of the remainder experienced malaria after completion of the prophylactic course. No side effects of treatment were observed.
对居住在无疟疾自然传播地区的非免疫志愿者,测试了WR 33063(3-溴-10-[α-羟基-β-(N,N-二庚基氨基)乙基]菲盐酸盐)和WR 30090(6,8-二氯-2,3,4-三氯苯基-二正丁基氨基乙基-4-喹啉甲醇盐酸盐)对诱发疟疾的抑制预防作用。对在首剂给药当天接触感染了氯喹和乙胺嘧啶耐药恶性疟原虫株的蚊子的男性,每周间隔给予800毫克WR 33063以及690或460毫克WR 30090。WR 33063不干扰感染的早期发展,但给予8周的WR 30090使26名男性中的20名获得抑制性治愈。间日疟感染同样在15名男性中的4名中突破了WR 30090治疗,其余大多数人在预防疗程结束后患上疟疾。未观察到治疗的副作用。