Studies designed to increase the stability and antiviral activity (HCMV) of the active benzimidazole nucleoside, TCRB.
Studies designed to increase the stability and antiviral activity (HCMV) of the active benzimidazole nucleoside, TCRB.
复制标题
旨在提高活性苯并咪唑核苷 TCRB 的稳定性和抗病毒活性 (HCMV) 的研究。
DOI：
10.1080/15257779908041486
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发表时间：
1999
期刊：
影响因子：
--
通讯作者：
Drach,JC
中科院分区：
文献类型：
--
作者：
Townsend,LB;Gudmundsson,KS;Daluge,SM;Chen,JJ;Zhu,Z;Koszalka,GW;Boyd,L;Chamberlain,SD;Freeman,GA;Biron,KK;Drach,JC
The potent activity of 2,5,6-trichloro-1-(ß-D-ribofuranosyl)benzimidazole (TCRB) against Human Cytomegalovirus with the concomitant low cellular toxicity at concentrations that inhibit viral growth prompted considerable interest in this research area. This interest was moderated by the pharmacokinetic studies of TCRB in rats and monkeys that revealed the instability of TCRBin vivo. These studies suggested that the instability was due to a cleavage of the glycosidic bondin vivowhich released the heterocycle (2,5,6-trichlorobenzimidazole) into the bloodstream. This prompted us to initiate synthetic studies designed to increase the stability of the glycosidic bond of TCRB and BDCRB. Several synthetic approaches to address this and other problems are presented.
