Design, synthesis and in-vitro evaluation of novel tetrahydroquinoline carbamates as HIV-1 RT inhibitor and their antifungal activity
文献类型：期刊论文
| 作者 | Chander S1; Ashok P1; Taneja A1; Murugesan S[*]1; Zheng YT2; Wang P2; Raja KS1 |
| 刊名 | BIOORGANIC CHEMISTRY
 |
| 出版日期 | 2016 |
| 卷号 | 64期号:X页码:66-73 |
| 关键词 | Antifungal Antiretroviral Cytotoxicity Docking Drug-likeness Reverse transcriptase Tetrahydroquinoline |
| 通讯作者 | subhashsaininiper@gmail.com |
| 英文摘要 | Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs) are vital class of drugs in treating HIV-1 infection, but drug resistance and toxicity drive the need for effective new inhibitors with potent antiviral activity, less toxicity and improved physicochemical properties. In the present study, twelve novel 1-(4-chlorophenyl)-2-(3,4-dihydroquinolin-1(2H)-yl)ethyl phenylcarbamate derivatives were designed as inhibitor of HIV-1 RT using the ligand based drug design approach and in-silico evaluated for drug-likeness properties. Designed compounds were synthesized, characterized and in-vitro evaluated for RT inhibitory activity against wild HIV-1 RT. Among these, four compounds (6b, 6i, 6j and 6l) exhibited significant inhibition of HIV-1 RT (IC50⩽20μM). Among four compounds, most active compounds 6b and 6j inhibited the RT activity with IC50 8.12 and 5.42μM respectively. Docking studies of compounds 6b and 6j were performed against wild HIV-1 RT in order to predict their putative binding mode with selected target. Further, cytotoxicity and anti-HIV activity of compounds 6b and 6j were evaluated on T lymphocytes (C8166 cells). All the synthesized compounds were also evaluated for antifungal activity against Candida albicans and Aspergillus niger fungal strains. |
| 收录类别 | SCI |
| 资助信息 | Authors gratefully acknowledge BITS-Pilani for providing the necessary facilities to do this work. This work was carried out under a grant from Science and Engineering Research Board of Department of Science and Technology, New Delhi. (Ref. No: SR/FT/LS-58/2011), the STS Program of CAS (KFJ-EW-STS-026) and Collaborative Innovation Center for Natural Products and Bio- logical Drugs of Yunnan. |
| 语种 | 英语 |
| 源URL | [http://159.226.149.26:8080/handle/152453/9516]  |
| 专题 | 昆明动物研究所_分子免疫药理学 昆明动物研究所_动物模型与人类重大疾病机理重点实验室 |
| 作者单位 | 1.Medicinal Chemistry Research Laboratory, Department of Pharmacy, Birla Institute of Technology & Science, Pilani 333031, Rajasthan, India 2.Laboratory of Molecular Immunopharmacology, Key Laboratory of Animal Models and Human Disease Mechanisms of Chinese Academy of Sciences and Yunnan Province, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming, Yunnan 650223, PR China |
| 推荐引用方式 GB/T 7714 | Chander S,Ashok P,Taneja A,et al. Design, synthesis and in-vitro evaluation of novel tetrahydroquinoline carbamates as HIV-1 RT inhibitor and their antifungal activity[J]. BIOORGANIC CHEMISTRY,2016,64(X):66-73. |
| APA | Chander S.,Ashok P.,Taneja A.,Murugesan S[*].,Zheng YT.,...&Raja KS.(2016).Design, synthesis and in-vitro evaluation of novel tetrahydroquinoline carbamates as HIV-1 RT inhibitor and their antifungal activity.BIOORGANIC CHEMISTRY,64(X),66-73. |
| MLA | Chander S,et al."Design, synthesis and in-vitro evaluation of novel tetrahydroquinoline carbamates as HIV-1 RT inhibitor and their antifungal activity".BIOORGANIC CHEMISTRY 64.X(2016):66-73. |
入库方式： OAI收割
来源：昆明动物研究所
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