Singh Jyoti, Shaik Basheerulla, Singh Shalini, Agrawal Vijay K, Khadikar Padmakar V, Deeb Omar, Supuran Claudiu T
QSAR and Computer Chemical Laboratories, A.P.S. University, Rewa-486 003, India.
Chem Biol Drug Des. 2008 Mar;71(3):244-59. doi: 10.1111/j.1747-0285.2007.00625.x. Epub 2008 Jan 19.
Comparative quantitative structure-activity relationship studies on para-substituted aromatic sulphonamides carbonic anhydrase II (CAII) inhibitors are reported in this paper. The study is made utilizing (i) information indices along; (ii) distance-based and connectivity indices and (iii) combination of information, distance-based and connectivity type topological indices. The study has shown that distance-based and connectivity type indices are superior for modelling, monitoring and estimating CAII inhibition. The results are critically discussed using a variety of statistical parameters. Our results show that starting from the mono-parametric regression itself, our results are superior: Furthermore, our methodology allowed carrying out much higher-parametric regressions, yielding a nine-parametric model with R2 as high as 0.8375. The eight-parametric regression, gave R2= 0.8343. As there is not much difference, we have considered the eight-parametric regression the best.
本文报道了对对位取代芳基磺酰胺碳酸酐酶II(CAII)抑制剂的比较定量构效关系研究。该研究利用了:(i)信息指数;(ii)基于距离和连接性的指数;(iii)信息、基于距离和连接性类型拓扑指数的组合。研究表明,基于距离和连接性类型的指数在CAII抑制的建模、监测和估计方面更具优势。使用各种统计参数对结果进行了批判性讨论。我们的结果表明,从单参数回归开始,我们的结果就更优:此外,我们的方法允许进行更高参数的回归,得到一个九参数模型,R2高达0.8375。八参数回归得到R2 = 0.8343。由于差异不大,我们认为八参数回归是最佳的。