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Volume 59, Issue 6, Pages 622-625 (12 November 2002)


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Theoretical mechanistic basis of the toxic effects and efficacy of AZT in HIV: AIDS

Dunstan A.A AkintonwaCorresponding Author Information

Received 11 June 2001; accepted 13 February 2002.

Abstract 

Toxic effects and efficacy of azidothymidine (AZT) in human immunodeficiency virus were evaluated by theoretical mechanistic biochemistry (TMB) techniques based on the structure of AZT and on the structure of HIV. AZT was positive (1+) for epoxide; (2+) for hydroxl free radical (); (1+) for () azide free radical and (1+) for azide (N3) generations, respectively. AZT was negative (−) for areneimine, and nitroso generations, respectively, for toxic effects totalling 5+ compared with dideoxycytidine (ddc) of 3+ and artesunate (At) of 0.

Therefore for toxic effects the trend is AZT(5+)>ddc(3+)>At(0). TMB efficacy of AZT was based on the generations of from the 1-NH (1+) and the 31-azido (N3)(1+) and azide free radical (), (1+) totalling 3+ compared with ddc of 1+ and At of 1+. Therefore for efficacy, the trend is AZT(3+)>ddc(1+)=At(1+). In combination drug therapy, TMB postulates the following for HIV : AIDS: At(1+)+AZT(3+)+ddc(1+)>AZT(3+)+ddc(1+)=AZT(3+)+At(1+)>AZT(3+)>At(1+)+ddc(1+)>ddc(1+)=At(1+).

Cross River State, Nigeria

Corresponding Author InformationCorrespondence to: Dunstan A.A. Akintonwa, Centre for Theoretical Mechanistic Biochemistry(CTMB), Amazing Grace, 150 Anansa Road, P.O. Box 3129, Calabar, Cross River State, Nigeria

PII: S0306-9877(02)00146-9


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