Synthesis and biological evaluation of HQCAs with aryl or benzyl substituents on N-1 position as potential HIV-1 integrase inhibitors
| Autor: | Hai-Qiu Wu, Liu-Meng Yang, Xuan Zhang, Yong-Tang Zheng, Shuang-Xi Gu, Fen-Er Chen, Qiu-Qin He, Xiao-Dong Ma |
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| Rok vydání: | 2011 |
| Předmět: |
Models
Molecular medicine.drug_class Stereochemistry Anti-HIV Agents Clinical Biochemistry Mutant Pharmaceutical Science Integrase inhibitor HIV Integrase Microbial Sensitivity Tests Quinolones Biochemistry Virus chemistry.chemical_compound Structure-Activity Relationship Drug Discovery medicine Potency Humans HIV Integrase Inhibitors Molecular Biology Cell Line Transformed Dose-Response Relationship Drug Molecular Structure Chemistry Aryl Organic Chemistry Stereoisomerism Quinolone Docking (molecular) Cell culture HIV-1 Molecular Medicine |
| Zdroj: | Bioorganicmedicinal chemistry. 19(18) |
| ISSN: | 1464-3391 |
| Popis: | A series of new 5-hydroxylquinolone-3-carboxylic acids (HQCAs) with various aryl or benzyl substituents on N-1 position were synthesized and evaluated for their anti-HIV activity in C8166 cell culture. Most of the target compounds displayed activity against wide-type HIV-1 in the low micromolar range in infected C8166 cells. The most active compound 5g exhibited activity against wild-type HIV-1 and HIV-1 mutant virus A17 with an EC 50 value of 3.17 and 17.88 μM, respectively. The biological results and the docking study revealed that the substitution pattern on N-1 position of the quinolone core might contribute to physicochemical properties of HQCAs and resulted in great influence on their antiviral potency. |
| Databáze: | OpenAIRE |
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