RELATIONSHIPS BETWEEN STRUCTURE AND ANTIRETROVIRAL ACTIVITY OF THIOSEMICARBAZONE DERIVATIVES

In an attempt to develop anti-AIDS drugs, the compound isatin P-thiose micarbazone has been subjected to systematic structural modifications. The resulting synthesized thiosemicarbazone derivatives (TSCDs) were examined for their ability to act as antiretrovirus agents in a model system - 2M3/M cell system - consisting of B lymphocytes transformed b y the v-abl oncogene and chronically infected with a retrovirus, the M oloney leukemia virus (M-MuLV). The efficacy of the synthesized TSCDs against retroviruses was determined by assaying the therapeutic index (TI) values of the compounds. The results enabled the classification o f TSCD groups based on the relationship between chemical structure and antiretroviral activity. The compound N-allylisatin-beta':4'-diallylt hiosemicarbazone showed the highest TI value and efficiently suppresse d the chronic infection of M-MuLV in continuous long-term treatment.