Premium
Exploiting the Thiobarbituric Acid Scaffold for Antibacterial Activity
Author(s) -
Sharma Anamika,
Noki Sikabwe,
Zamisa Sizwe J.,
Hazzah Heba A.,
Almarhoon Zainab M.,
ElFaham Ayman,
de la Torre Beatriz G.,
Albericio Fernando
Publication year - 2018
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201800414
Subject(s) - moiety , knoevenagel condensation , thioamide , chemistry , antimicrobial , enamine , thiobarbituric acid , acylation , combinatorial chemistry , schiff base , organic chemistry , antibacterial activity , bacteria , myristoylation , stereochemistry , biochemistry , antioxidant , catalysis , biology , lipid peroxidation , genetics , phosphorylation
Thiobarbituric acid (TBA) has been considered a privileged structure for developing antimicrobial agents. Diversity was obtained at positions N and at C5 through acylation, Schiff base formation, Knoevenagel condensation, and thioamide and enamine formation. The present work describes the synthesis of small libraries based on the TBA moiety and above‐mentioned reactions. Preliminary antimicrobial activity screening of the prepared compounds against selected bacteria (both Gram‐positive and ‐negative) showed the best results for the Boc‐Phe‐TBA derivative. These results could be useful for designing and building libraries based on other amino acids with distinct protecting groups.