02398nas a2200301   4500008004100000022001400041245011400055210006900169260000800238300001400246490000700260520143100267653002001698653002901718653001901747653001901766653000901785653002701794100002001821700001901841700002101860700001801881700002001899700001901919700002001938700001901958856011901977       2019                        eng d  a1570-180800aRecursive partitioning analysis and anti-tubercular screening of 3-aminopyrazine-2-carbohydrazide derivatives0 aRecursive partitioning analysis and antitubercular screening of   cAPR  a1264-12750 v163 a<p>Background: Treating tuberculosis is a challenge due to the development of drug resistance. Hence, it is imperative to develop novel leads having high potency and efficacy to curb drug resistance. Methods: The present research work is focused on microwave-assisted synthesis of novel twenty-six 3-amino-N'-benzylidenepyrazine-2-carbohydrazide derivatives (3a-z), where, lyophilization technique was used for isolation of the major intermediate, 3-aminopyrazin-2-carbohydrazide. All synthesized compounds were subjected for anti-tubercular screening against Mycobacterium tuberculosis H37Ra by using XTT Reduction Menadione Assay (XRMA) protocol. Results: Out of 26 synthesized compounds, four N'-substitutedbenzaldehyde-3-amino-pyrazine-2-carbohydrazide derivatives viz. 3i, 3j 3v and 3z showed significant activity against M. tuberculosis H37Ra. The compounds 3i, 3j, 3v and 3z showed 99, 98, 92 and 87 % inhibition respectively as compared to 94% inhibition shown by the standard drug rifampicin. The MIC and IC50 values were in the range of 24.3-110 and 5.9-20.8 mu g/ml respectively. Conclusion: A classification model called Recursive Partitioning (RP) based on binary Quantitative Structure-Activity Relationship (QSAR) was derived for the establishment of structure-activity relationship (SAR). The predictions derived on the basis of RP model were found to be in agreement with anti-tubercular screening data.</p>
10a3-aminopyrazine10aanti-tubercular activity10aCarbohydrazide10alyophilization10aQSAR10arecursive partitioning1 aMiniyar, Pankaj1 aMahajan, Anand1 aAnuse, Dattatray1 aKumar, Ashish1 aBarmade, Mahesh1 aSarkar, Dhiman1 aArkile, Manisha1 aKhedkar, Vijay  uhttps://library.ncl.res.in/content/recursive-partitioning-analysis-and-anti-tubercular-screening-3-aminopyrazine-2