旨在提高活性苯并咪唑核苷TCRB的稳定性和抗病毒活性（针对人巨细胞病毒）的研究。
Studies designed to increase the stability and antiviral activity (HCMV) of the active benzimidazole nucleoside, TCRB.
作者信息
Townsend L B, Gudmundsson K S, Daluge S M, Chen J J, Zhu Z, Koszalka G W, Boyd L, Chamberlain S D, Freeman G A, Biron K K, Drach J C
机构信息
University of Michigan, Department of Medicinal Chemistry, College of Pharmacy, Ann Arbor 48109, USA.
出版信息
Nucleosides Nucleotides. 1999 Apr-May;18(4-5):509-19. doi: 10.1080/15257779908041486.
The potent activity of 2,5,6-trichloro-1-(beta-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 TCRB in vivo. These studies suggested that the instability was due to a cleavage of the glycosidic bond in vivo which 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.
2,5,6-三氯-1-(β-D-呋喃核糖基)苯并咪唑(TCRB)对人巨细胞病毒具有强大的活性，在抑制病毒生长的浓度下细胞毒性较低，这引发了该研究领域的广泛关注。然而，TCRB在大鼠和猴子体内的药代动力学研究表明其在体内不稳定，这使得这种关注有所缓和。这些研究表明，不稳定是由于体内糖苷键断裂，释放出杂环(2,5,6-三氯苯并咪唑)进入血液。这促使我们开展合成研究，旨在提高TCRB和BDCRB糖苷键的稳定性。本文介绍了几种解决这一问题及其他问题的合成方法。
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