Abstract
In the search of new HIV-1 integrase (IN) inhibitors, we synthesized a series of multimeric 5,6-dihydroxyindole-2-carboxylic acid (DHICA) derivatives. Preliminary results indicate that hyperbranched architectures could represent a peculiar molecular requisite for the development of new antiviral lead compounds.
Highlights
In the search for new HIV-1 IN inhibitors, we synthesized and evaluated the biological activity of 5,6-dihydroxyindole-2-carboxylic acid (DHICA, II), an intermediate in the pathway of eumelanin production, and a series of its derivatives (IIIa-i, Figure 1)
In the search of new HIV-1 integrase (IN) inhibitors, we synthesized a series of multimeric 5,6-dihydroxyindole-2-carboxylic acid (DHICA) derivatives
Detailed cytotoxicity and antiviral activity as well as inhibition activities toward cellular targets of these compounds are under investigation and will be discussed in due course
Summary
In the search for new HIV-1 IN inhibitors, we synthesized and evaluated the biological activity of 5,6-dihydroxyindole-2-carboxylic acid (DHICA, II), an intermediate in the pathway of eumelanin production, and a series of its derivatives (IIIa-i, Figure 1). AB2 monomers have been widely used as starting materials for the synthesis of dendritic structures [2,3] This macromolecular family comprises dendrimers and hyperbranched polymers. The synthetic chemistry efforts in modern drug research have been focused on the drive to discover orally bioavailable small-molecule drugs, the study of macromolecular entities could reveal novel and significant scenarios It is well-known that many of the biological targets are macromolecules which rely heavily on polyvalent/multivalent interactions in their binding and signalling cascades. With the hope of identifying an original class of antiviral agents, all title compounds will be tested against HIV1 viral strain
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