DIDEOXYNUCLEOSIDES AS POTENTIAL ANTI-AIDS DRUGS

本工作的目的是发现2‘，3’-双脱氧核苷 (DDO)，这些药物优于已知的HTLV-III病毒抑制剂。 DDO-5-氮胞苷具有活性，但毒性略高于DDO-C。这个 DDO-C的5-氟类似物与母体一样有效和有效 化合物对HTLV-III感染细胞的保护作用。然而，5-溴和 5-甲基类似物无效。DDO-环戊烯基异构体(奈普洛辛 类似物)被证明是无活性和无毒的。

The objective of this work is the discovery of 2',3'-dideoxynucleosides (DDO) which are superior to known inhibitors of the HTLV-III virus. DDO-5-azacytidine was active but somewhat more toxic than DDO-C. The 5-fluoro analog of DDO-C was just as effective and potent as the parent compound in protecting HTLV-III infected cells. However, the 5-bromo and 5-methyl analogs were ineffective. DDO-cyclopentenyl isosteres (neplanocin analogs) proved to be inactive and nontoxic.