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Abstract
Integrase (IN) represents a clinically validated target for the development of antivirals against human immunodeficiency virus (HIV). In recent years our research group has been engaged in the stucture-function study of this enzyme and in the development of some three-dimensional pharmacophore models which have led to the identification of a large series of potent HIV-1 integrase strand-transfer inhibitors (INSTIs) bearing an indole core. To gain a better understanding of the structure-activity relationships (SARs), herein we report the design and microwave-assisted synthesis of a novel series of 1-H-benzylindole derivatives.
Highlights
Human Immunodeficiency Virus 1 (HIV-1) is the etiological agent of Acquired Immune DeficiencySyndrome (AIDS) which has caused a large number of deaths for over 20 years
These can be divided into seven groups: Nucleoside reverse transcriptase inhibitors (NRTIs), nucleotide reverse transcriptase inhibitors (NtRTIs), non-nucleoside reverse transcriptase inhibitors (NNRTIs), protease inhibitors (PIs), fusion inhibitors (FIs), co-receptor inhibitors (CRIs), and integrase inhibitors (INIs) [1]
This current therapy has been successful in substantially decreasing in morbidity and mortality rates, the use of this arsenal of drugs is limited by toxicity, adverse effects, drug resistance, and more worryingly by the fact that some newly human immunodeficiency virus (HIV)-infected patients carry viruses that are already resistant to currently approved Acquired Immune DeficiencySyndrome (AIDS) treatments [2,3]
Summary
Human Immunodeficiency Virus 1 (HIV-1) is the etiological agent of Acquired Immune Deficiency. The U.S Food and Drug Administration (FDA) has approved drugs that are often used in combination regimens in the well-known Highly Active Antiretroviral Therapy (HAART) These can be divided into seven groups: Nucleoside reverse transcriptase inhibitors (NRTIs), nucleotide reverse transcriptase inhibitors (NtRTIs), non-nucleoside reverse transcriptase inhibitors (NNRTIs), protease inhibitors (PIs), fusion inhibitors (FIs), co-receptor inhibitors (CRIs), and integrase inhibitors (INIs) [1]. This current therapy has been successful in substantially decreasing in morbidity and mortality rates, the use of this arsenal of drugs is limited by toxicity, adverse effects, drug resistance, and more worryingly by the fact that some newly HIV-infected patients carry viruses that are already resistant to currently approved AIDS treatments [2,3]. (i) controlled heating conditions; (ii) reaction time and solvent reduction; (iii) faster exploration of SARs
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