Structural requirements of some derivatives based on natural alkaloid lycorine for their dengue inhibitory activity to accelerate dengue drug discovery efforts
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Title Statement |
Structural requirements of some derivatives based on natural alkaloid lycorine for their dengue inhibitory activity to accelerate dengue drug discovery efforts |
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Added Entry - Uncontrolled Name |
Awasthi, Monika ; Dr. Harisingh Gour University Amin, Sk. Abdul ; Dr. Harisingh Gour University Shukla, Vijaya ; Dr. Harisingh Gour University Jain, Sanskar ; Dr. Harisingh Gour University Patil, Umesh Kumar; Dr. Harisingh Gour University Gayen, Shovanlal ; Dr. Harisingh Gour University UGC, India |
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Uncontrolled Index Term |
utilization of plants and animals in broader sense, multidisciplinary especially of applied nature ADMET, Dengue, Lycorine, MLR, Natural alkaloid, NS4A, QSAR. |
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Summary, etc. |
<p><span>Dengue virus (DENV) is one of the life threatening problems in tropical countries including India. During the last few decades, 50-100 million dengue viral infections were reported specially in Asia and Pacific region. In search of novel DENV inhibitor, the present study tried to correlate the DENV inhibitory data with a series of natural alkaloid lycorine derivatives. A statistically robust QSAR model is generated [</span><em>R</em><span> = 0.944; = 0.865; </span><em>Q<span>2</span> </em><span>= 0.741; = 0.51593; = 0.826] with five descriptors such as </span><em>GATS2c</em><span>, </span><em>ZMIC3</em><span>, </span><em>T_N_O_7</em><span>, </span><em>Quadrupole1</em><span> and </span><em>nHsNH2</em><span>. The reliability of the model was confirmed by Golbraikh and Tropsha acceptable model criteria. The QSAR result suggests that the hydroxyl group as well as linear aliphatic at R</span><span>1</span><span> position is very important for the biological potency, whereas, amino and ether substituent at the R</span><span>2 </span><span>is detrimental. The study also revealed that bulky esterification at the R</span><span>2</span><span> is not tolerable. Additionally, lead molecule showed good absorption, distribution, metabolism, excretion and toxicity (ADMET) properties. The findings may be useful to design potent lycorine-based anti-dengue compounds in future.</span></p> |
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Publication, Distribution, Etc. |
Indian Journal of Natural Products and Resources (IJNPR) [Formerly Natural Product Radiance (NPR)] 2016-11-28 13:23:53 |
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Electronic Location and Access |
application/pdf application/pdf http://op.niscair.res.in/index.php/IJNPR/article/view/13494 |
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Data Source Entry |
Indian Journal of Natural Products and Resources (IJNPR) [Formerly Natural Product Radiance (NPR)]; ##issue.vol## 7, ##issue.no## 3 (2016): September 2016 |
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Language Note |
en |
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Nonspecific Relationship Entry |
http://op.niscair.res.in/index.php/IJNPR/article/download/13494/46808 |
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Terms Governing Use and Reproduction Note |
Except where otherwise noted, the Articles on this site are licensed underCreative Commons License: CC Attribution-Noncommercial-No Derivative Works 2.5 India© 2012. The Council of Scientific & Industrial Research, New Delhi. |
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