Abstract
Quinoline moiety is an important scaffold in the field of drug discovery and drug development, with a wide range of pharmacological activities. Quinoline derivatives are potent inhibitors for reverse transcriptase, which is responsible for the conversion of single-stranded viral RNA into double-stranded viral DNA.In the present study, we have designed and synthesized 2 series, namely pyrazoline and pyrimidine containing quinoline derivatives as non nucleoside reverse transcriptase inhibitors (NNRTIs). Eleven compounds were synthesized and characterized by 1H and 13C NMR and mass spectrophotometry. The synthesized compounds were also docked on an HIV reverse transcriptase binding site (PDB: 4I2P); most of these compounds showed good binding interactions with the active domain of the receptor. Most of the compounds displayed a docking score higher than those of standard drugs. Among the synthesized quinoline derivatives, compound 4 exhibited the highest docking score (–10.675).
Highlights
It has been over three decades since HIV, the causative agent for acquired immunodeficiency syndrome (AIDS), was identified
Compound (1) and substituted acetophenones were taken as starting material for the synthesis of chalcones from which 2 series of compounds were synthesized
Quinoline derivatives were designed concerning the structures of standard anti-HIV drugs and synthesized via chalcones as intermediates
Summary
It has been over three decades since HIV, the causative agent for acquired immunodeficiency syndrome (AIDS), was identified. From the beginning of the global pandemic of HIV in the early 1980s, an estimated 78 million people have been infected with HIV; about 39 million people have died of AIDS-related causes [1]. HIV reverse transcriptase enzyme synthesizes double-stranded DNA from single-stranded viral RNA and is an important target for anti-HIV drug development. In the early 1990s, potent HIV reverse transcriptase inhibitors (RTIs) with significant clinical activity were developed. Nonnucleoside reverse transcriptase inhibitors (NNRTIs) are leading drugs in the treatment of HIV-1 infections [2]. Highly active antiretroviral therapy (HAART) combination therapy is used for the treatment of HIV to avoid the development of resistance against a single drug, but it causes psychiatric and neurological side effects [3]. There is a dire need for novel anti-HIV agents with fewer side effects
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