Anti-HIV-1 Activity of Benzothiadiazine Dioxide
Author(s) -
Ana Martı́nez,
Carmen Gil,
Ana Castro,
Concepción Pérez,
Myriam Witvrouw,
Christophe Pannecouque,
Jan Balzarini,
Erik De Clercq
Publication year - 2001
Publication title -
antiviral chemistry and chemotherapy
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.919
H-Index - 51
eISSN - 2040-2066
pISSN - 0956-3202
DOI - 10.1177/095632020101200604
Subject(s) - benzothiadiazine , reverse transcriptase , human cytomegalovirus , mechanism of action , biology , nucleoside , nucleotidyltransferase , virology , nucleoside reverse transcriptase inhibitor , reverse transcriptase inhibitor , biological activity , virus , chemistry , antiretroviral therapy , in vitro , biochemistry , viral load , rna , organic chemistry , gene
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.
Accelerating Research
Robert Robinson Avenue,
Oxford Science Park, Oxford
OX4 4GP, United Kingdom
Address
John Eccles HouseRobert Robinson Avenue,
Oxford Science Park, Oxford
OX4 4GP, United Kingdom