Scientists from the Zelinsky Institute published a review on the synthesis of pyridine-containing inhibitors of HIV-1 integrase

The human immunodeficiency virus (HIV) causes one of the most dangerous diseases — acquired immunodeficiency syndrome (AIDS). The high growth rate in the number of HIV-infected people makes it very urgent to develop effective drugs to combat this virus. There are currently about 40 million people living with HIV worldwide, most of whom are already on antiretroviral therapy (ARVT), which consists of taking multiple antiviral drugs continuously. Integrase strand transfer inhibitors (INIs) are an important component of therapy for HIV-1, the most virulent form of the immunodeficiency virus. They are aimed at blocking the enzyme that inserts the viral genome into the DNA of the host cell. To date, five HIV-1 integrase inhibitors have been approved, four of which contain a pyridine moiety. This fact emphasizes the importance of the presence of heterocyclic fragments in the structure of such substances.

Scientists from the Laboratory of Aromatic Nitrogen-Containing Compounds of the ZIOC published a review on methods for the synthesis of inhibitors of HIV-1 integrase containing a pyridine fragment, published over the past 20 years. The considered compounds of various structure are grouped into subsections: monocyclic pyridines, benzoannulated pyridines (quinolines and isoquinolines), pyridines fused with heterocycles. The review shows that the chemistry of monocyclic and annulated pyridines is actively developing: the synthesis of known INIs is being improved and optimized, new synthetic methods are being published, and new pyridine-containing molecules are being created and studied. The presented results can serve as a basis for the development and search for new anti-HIV drugs.

Source:

Alexey M. Starosotnikov and Maxim A. Bastrakov Recent Developments in the Synthesis of HIV-1 Integrase Strand Transfer Inhibitors Incorporating Pyridine Moiety // Int. J. Mol. Sci. 2023, 24, 9314. DOI: 10.3390/ijms24119314.