TY - JOUR
T1 - Design, Synthesis, DNA Binding, and Docking Studies of Thiazoles and Thiazole-Containing Triazoles as Antibacterials
AU - Santosh, Rangappa
AU - Mukunthan, KS
AU - Kanekar, Saptami U.
AU - Nagaraja, Gundibasappa K.
AU - Kumar, Madan
N1 - Publisher Copyright:
© 2018 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim
PY - 2018/4/17
Y1 - 2018/4/17
N2 - A series of thiazoles 4 a-g and thiazole clubbed triazoles 5 a-f were synthesized and showed good antibacterial activity against, Pseudomonas aeruginosa, Escherchia coli, Staphylococcus aureus and Bacillus subtilis. Particularly, 4 a (methyl), 5 b (nitro) and 5 d (fluoro) derivatives demonstrated a broad range of activity over other derivatized compounds. In addition, Computational interaction, ADMET (absorption, distribution, metabolism, and excretion - toxicity in pharmacokinetics), Lipinski's rule and DNA binding studies of all the results stacked together indicated that 5 b can be further developed as lead molecule against bacterial pathogens.
AB - A series of thiazoles 4 a-g and thiazole clubbed triazoles 5 a-f were synthesized and showed good antibacterial activity against, Pseudomonas aeruginosa, Escherchia coli, Staphylococcus aureus and Bacillus subtilis. Particularly, 4 a (methyl), 5 b (nitro) and 5 d (fluoro) derivatives demonstrated a broad range of activity over other derivatized compounds. In addition, Computational interaction, ADMET (absorption, distribution, metabolism, and excretion - toxicity in pharmacokinetics), Lipinski's rule and DNA binding studies of all the results stacked together indicated that 5 b can be further developed as lead molecule against bacterial pathogens.
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U2 - 10.1002/slct.201800222
DO - 10.1002/slct.201800222
M3 - Article
AN - SCOPUS:85045650022
SN - 2365-6549
VL - 3
SP - 3892
EP - 3898
JO - ChemistrySelect
JF - ChemistrySelect
IS - 14
ER -