Antiviral for AIDS

Azidothymidine The FDA approves azidothymidine (AZT), a potent antiviral, for AIDS patients. 

Efavirenz [154598-52-4], antiviral for AIDS, reverse transcriptase inhibitor, 88. Either phosgene or CDI can be employed to form the key intermediate, (4S)-6methoxyphenyl)methyl]-4-trifluoromethyl-2H-3,l-benzoxazin-2-one [56-67]. 

As for AIDS, the disease was first recognized in 1981, and the causative agent, HIV, was isolated in 1983. By the end of 1986, the first partially effective antiviral, AZT, was developed. Thus, the rate of progress in AIDS research has actually been very rapid in historical terms. 

Although any of these seven steps could be a druggable target, most of the antiviral agents clinically employed for non-AIDS infections act on the synthesis or assembly of either purines or pyrimidines (steps 3 and 4). For AIDS, reverse transcriptase inhibitors block transcription of the HIV RNA genome into DNA, thereby preventing synthesis of viral mRNA and protein protease inhibitors act on the synthesis of late proteins (steps 5 and 6). 

A large fraction of polytungstates that have been tested prove to have potent antitumoral and antiviral activity (rabies, influenza, scrapie, and the retroviruses responsible for AIDS and SAIDS). Toxicity varies widely, bnt some species are less toxic than azidothymidine (AZT) and are effective against AZT-resistant cell lines. The polyoxoanions bind to the gpl20 envelope glycoprotein of the retrovirus, and in some cases inhibit the function of the rus reverse transcriptase (cf AZT). Reviews of Structure and Reactivity of Polyoxometalates have recently appeared. ... 

CMV retinitis is the most common opportunistic eye infection in patients with AIDS and immunocompromised transplant patients. Antiviral medications used in the treatment of CMV are generally administered in two stages induction therapy, to achieve disease regression, followed by maintenance therapy. The incidence of CMV retinitis has decreased significantly with the advent of HAART for AIDS, and antiviral therapy for CMV may often be discontinued in patients who respond favorably to HAART and achieve an elevation in CD4 cell levels above lOO/pl. Refer to Chapter 32 fiar the drug treatment of ocular CMV infections. 

Acquired immunodeficiency syndrome (AIDS), a degenerative disease of the immune system, is caused by the human immunodeficiency virus (HIV) and results in life-threatening opportunistic infections and malignancies. Antiviral and im-munomodulating natural products have been investigated as treatments for AIDS (111). 

Weislow, O. S., Kiser, R., Fine, D. L., Bader, J., Shoemaker, R. H. and Boyd, M. R. (1989). New soluble-formazan assay for HIV-1 cytopathic effects application to high-flux screening of synthetic and natural products for AIDS-antiviral activity J. Natl. Cancer Inst. 81, 577-586 (published erratum appears in J. Natl. Cancer Inst. 81, 963). 

Castanosp ermine has been shown to have in vitro antiviral activity against human immunodeficiency virus (HIV) [99] and human cytomegalovirus (CMV) [100], which is an opportunistic pathogen in AIDS. Alterations in viral coat glycoproteins in the presence of castanospermine are associated with a loss of infectivity. 6-0-acyl derivatives of castanospermine are more potent inhibitors of HIV growth than the natural product with the 6-O-butyryl-derivative (MDL 28,374) currently in clinical trials for AIDS. The lipophilic nature of the acyl derivative improves uptake by cells but the compound appears to be intracellularly converted to castanospermine [101]. 

Antiviral agent active exclusively against retroviruses, esp. AIDS virus and leukaemias. Drug of choice (1986) for AIDS treatment. Needles (Et20). Mp 106-112°, Mp 119-121° (after drying). 

Anti-cancer Antiviral (incl. AIDS) Antiarthritic Agent for Cognition Disorders Non-Opioid Analgesic Antipsychotic Agent for Autoimmune Diseases Nootropic Agent Antidiabetic Antiobesity Anxiolytic... 

Yamamoto, N., Nakashima, H., Yoshida, O., Kaneko, Y, Matsuzaki, K., and Uryu, T. (1989) Effect of the sulfated polysaccharides on HIV a novel strategy of chemical modification for HIV antivirals. Arch. AIDS Res., 1,45-56. 

Viruses are small infectious agents composed of a nucleic acid genome (DNA or RNA) encased by structural proteins and in some cases a lipid envelope. They are the causative agents of a number of human infectious diseases, the most important for public health today being acquired immunodeficiency syndrome (AIDS), hepatitis, influenza, measles, and vituses causing diarrhoea (e.g., rotavirus). In addition, certain viruses contribute to the development of cancer. Antiviral drugs inhibit viral replication by specifically targeting viral enzymes or functions and are used to treat specific virus-associated diseases. 

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