Retroviral enzymes inhibitor

V-Aminoimidazole derivatives, (IV), prepared by De Clercq (5) were effective as retroviral enzyme inhibitors and used in treating HIV. 

The pandemic of HIV and the discovery of inhibitors of viral and retroviral enzymes (e.g., AZT, which is an inhibitor of the reverse transcriptase of HIV RT-HIV) have given rise to considerable research. In this connection, deoxynucleosides, which were previously studied as potential antitumor drugs, are receiving renewed attention by researchers. Among these latter compounds, fluorodeoxynucleosides have been the focus of many investigations. ... 

Thiourea compounds have been observed to inhibit human immunodeficiency virus (HIV) reverse transcriptase, a viral enzyme that is responsible for the reverse transcription of the retroviral RNA to proviral DNA. Phenethylthiazoylthiourea (PETT) compounds were discovered as potent inhibitors of HIV type 1 and display certain structure-activity relationships among various substituents in their structure.199 207 Furthermore, thiourea derivatives have been found to be potent and selective viral inhibitors, antifungal and antibacterial compounds.208 215... 

The rapid spread of acquired immune deficiency syndrome (AIDS) has prompted numerous efforts to develop therapeutic agents against the human immunodeficiency virus type 1 (HIV-1) [2351. Efforts have focused on inhibition of the virally encoded reverse transcriptase (RT) enzyme, which is responsible for the conversion of retroviral RNA to proviral DNA. The nucleoside RT inhibitors 3 -azidothymidine (AZT) and dideoxyinosine (ddl) have proven to be clinically useful anti HIV-1 agents [236], but due to their lack of selectivity versus other DNA polymerases, these compounds are flawed by their inherent toxi-... 

REVERSE TRANSCRIPTASE INHIBITORS are used in the treatment of retroviral infections, including AIDS. In RNA retroviruses (e.g. AIDS and T-cell leukaemia), the virion contains a reverse transcriptase enzyme that makes a DNA copy of the viral RNA, and this copy is incorporated into the host genome, and is termed a provirus. The proviral DNA is transcribed into new genomic RNA. and mRNA for translation into viral proteins. Such viruses replicate by budding, which does not kill the host cell. Furthermore, some RNA retroviruses can transform normal host cells into malignant cells (e.g. with some sarcoma viruses). In the treatment of AIDS, a number of drugs are being, or have... 

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