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Anti-HIV-1 activity of benzothiadiazine dioxide

AuthorsMartínez, Ana ; Gil, Carmen ; Castro, Ana ; Pérez, Concepción; Witvrouw, M.; Pannecouque, C.; Balzarini, Jan; De Clercq, Erik
Issue Date2001
PublisherMedical Press
CitationAntiviral Chemistry and Chemotherapy 12: 347- 351 (2001)
AbstractAntiviral assays carried out on the potent benzothiadiazine dioxide (BTD) human cytomegalovirus (HCMV) inhibitors have led us to find marginal but selective anti-HIV-1 activity. Specific pharmacological studies, such as time of addition experiments and assays on specific viral strains with mutations on its reverse transcriptase, have indicated that BTD compounds act as nonnucleoside reverse transcriptase inhibitors. Theoretical calculations showed a butterfly conformation for the active derivatives that are compatible with their mechanism of action. Therefore, BTD derivatives can be considered as potential lead compounds for the treatment of opportunistic HCMV infections in immunocompromised individuals such as AIDS patients.
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