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Microwave‐Assisted Synthesis, Antimicrobial, and Cytotoxicity Activity of N ‐ tert ‐butyl‐3‐{[2‐(arylamino)pyrimidin‐4‐yl]amino} Benzenesulfonamides
Author(s) -
Patwari Shivaji B.,
Murali Medari S.,
Jadhav Vivekanand B.
Publication year - 2018
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.3364
Subject(s) - chemistry , antifungal , cytotoxicity , antimicrobial , antibacterial activity , bacteria , combinatorial chemistry , palladium , stereochemistry , catalysis , medicinal chemistry , organic chemistry , in vitro , microbiology and biotechnology , biochemistry , genetics , biology
A novel synthetic method has been developed with palladium‐catalyzed Buchwald–Hartwig‐type reaction for the synthesis of N ‐ tert ‐butyl‐3‐{[2‐(arylamino)pyrimidin‐4‐yl]amino} benzenesulfonamide 5 by the treatment of N ‐ tert ‐butyl‐3‐[(2‐chloropyrimidin‐4‐yl)amino] benzenesulfonamide 4 with different aromatic amines in the presence of Cs 2 CO 3 and in DMF under microwave conditions. All the eight compounds 5a–h were evaluated for their antibacterial, antifungal, and cytotoxic activities. Among the title compounds, 5c and 5d showed potent activity towards both gram‐positive and gram‐negative bacteria. Compounds 5c and 5d displayed good antifungal activity, and the compounds 5c , 5d , and 5f exhibited significant cytotoxicity activity.