Biological planning, synthesis and evaluation of novel hybrid coumarins inhibitors of transciptase
revins and enzyme integrated for the treatment of HIV-1HIV, Integrase, Reverse TranscriptaseAIDS (acquired immunodeficiency syndrome) is a complex of symptoms and
diseases that manifest themselves after infection of the human body with HIV (
immunodeficiency). HIV is a retrovirus of the Retroviridae family, as in
other retroviruses, the HIV genome is composed of two single strands of positive RNA
and identical with each other that cause in the body a chronic immune dysfunction and
progressive decline due to the decline in levels of CD4 + T lymphocytes that are defense cells
of the human organism. There are currently two types of HIV identified called
of HIV-1 and HIV-2. HIV is an infection that represents one of the biggest problems
public health, due to its pandemic and seriousness. By 2017, there were in the world
36.9 million adults living with HIV. Despite the growth of the
world, the development of antiretrovirals (ARVs) has changed the lives of individuals
living with HIV / AIDS. Morbidity and mortality declined between 60 and 80%,
mainly due to the availability of different classes of ARV drugs and the use in
combination of three or more of them. However, the development of resistance to
continues to be one of the most serious obstacles to halting the spread of
of HIV during highly active antiretroviral therapy and this has been of great
throughout the world. In this way, considering the deficiencies of the therapies
currently available, in terms of side effects and resistance to the virus, there are
need to discover new molecules that are effective against viruses
resistant and also have fewer side effects. Thus, this project has
as an objective the planning of coumarin hybrid compounds planned
as inhibitors of the reverse transcriptase and integrase enzymes. The bioactivity profile
of the synthesized compounds will be carried out in in vitro models of inhibition of enzymes
reverse transcriptase and integrase.