Anti-HIV-1 activity of benzothiadiazine dioxide.
Antiviral 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 non-nucleoside 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.
Martinez
A
A
Instituto de Química Médica (CSIC), Madrid, Spain. iqmam06@pinar2.csic.es
Gil
C
C
Castro
A
A
Perez
C
C
Witvrouw
M
M
Pannecouque
C
C
Balzarini
J
J
De Clercq
E
E
D000998:Antiviral Agents / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D001581:Benzothiadiazines / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D002460:Cell Line; D003587:Cytomegalovirus / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D015497:HIV-1 / Q000187:drug effects* / Q000235:genetics / Q000502:physiology; D006801:Humans; D008958:Models, Molecular; D008968:Molecular Conformation; D013997:Time Factors
D000998:Antiviral Agents; D001581:Benzothiadiazines