3D QSAR analysis on quinoxaline derivatives as anti-malarial using K-nearest neighbour molecular field analysis
NOPR - NISCAIR Online Periodicals Repository
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Title |
3D QSAR analysis on quinoxaline derivatives as anti-malarial using K-nearest neighbour molecular field analysis
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Creator |
Mishra, Achal
Vaishnav, Yogesh Jha, Arvind Kumar Verma, Shekhar |
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Subject |
3D-QSAR
kNN-MFA Antimalarial Quinoxaline derivatives Sphere exclusion (SE) algorithm |
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Description |
727-731
In the present article, k nearest neighbour molecular field analysis (kNN-MFA) method was used to develop a three dimensional quantitative structure activity relationship (3D-QSAR) model. In this study 37 derivatives of quinoxaline having antimalarial activity were used. Sphere exclusion (SE) algorithm was used to create the biological activity data set in to into training and test set. For model generation kNN-MFA method has coupled with stepwise, simulated annealing and genetic algorithm this method provides various models, in which the most significant model developed by stepwise backward-forward method with predictive internal q2=0.7589 and external predictivity (pred_r2 = 0.4752). In the presented model electrostatic descriptors play crucial role for activity. Electrostatic descriptor (E_137) indicates regions in which electron withdrawing groups are favourable and descriptor (E_939) represents electron rich or electron donating groups are advantageous in particular region. The counter map/ plot of this model further helps to understand the relationship of structural feature of derivative of quinoxaline and its biological activity this would be applied for designing of new potent antimalarial containing quinoxaline as lead. |
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Date |
2021-06-25T07:41:46Z
2021-06-25T07:41:46Z 2021-05 |
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Type |
Article
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Identifier |
0975-0983(Online); 0376-4699(Print)
http://nopr.niscair.res.in/handle/123456789/57586 |
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Language |
en_US
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Rights |
CC Attribution-Noncommercial-No Derivative Works 2.5 India
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Publisher |
NISCAIR-CSIR, India
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Source |
IJC-B Vol.60B(05) [May 2021]
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