Synthesis, biological evaluation and 3D-QSAR studies of 3-keto salicylic acid chalcones and related amides as novel HIV-1 integrase inhibitors

HIV-1 integrase is one of the three most important enzymes required for viral replication and is therefore an attractive target for anti retroviral therapy. We herein report the design and synthesis of 3-keto salicylic acid chalcone derivatives as novel HIV-1 integrase inhibitors. The most active co...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2011-03, Vol.19 (6), p.2030-2045
Hauptverfasser:	Sharma, Horrick, Patil, Shivaputra, Sanchez, Tino W., Neamati, Nouri, Schinazi, Raymond F., Buolamwini, John K.
Format:	Artikel
Sprache:	eng
Schlagworte:	3-Keto salicylic acids 3D-QSAR amides Amides - chemical synthesis Amides - chemistry Amides - pharmacology Antibiotics. Antiinfectious agents. Antiparasitic agents Antiviral activity Antiviral agents benzoic acid Biological and medical sciences Cells, Cultured chalcone Chalcones Chalcones - chemical synthesis Chalcones - chemistry Chalcones - pharmacology chemistry CoMFA CoMSIA Enzymes HIV integrase HIV Integrase - chemistry HIV Integrase - metabolism HIV Integrase Inhibitors - chemical synthesis HIV Integrase Inhibitors - chemistry HIV Integrase Inhibitors - pharmacology HIV-1 HIV-1 - enzymology Human immunodeficiency virus 1 Humans inhibitory concentration 50 Integrase Integrase inhibitors Medical sciences Models, Molecular pharmacology Pharmacology. Drug treatments pharmacophores Quantitative Structure-Activity Relationship Replication Salicylic acid Salicylic Acid - chemistry Strand transfer inhibitors Synthesis therapeutics virus replication
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