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2,4‐ and 2,5‐Disubstituted Arylthiazoles: Rapid Synthesis by C–H Coupling and Biological Evaluation
Author(s) -
Lohrey Lilia,
Uehara Takahiro N.,
Tani Satoshi,
Yamaguchi Junichiro,
Humpf HansUlrich,
Itami Kenichiro
Publication year - 2014
Publication title -
european journal of organic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.825
H-Index - 155
eISSN - 1099-0690
pISSN - 1434-193X
DOI - 10.1002/ejoc.201402129
Subject(s) - antibiotics , chemistry , bacteria , combinatorial chemistry , staphylococcus aureus , antibiotic resistance , stereochemistry , microbiology and biotechnology , biochemistry , biology , genetics
Life‐threatening infections caused by bacteria that have developed resistance to common antibiotics, such as methicillin‐resistant Staphylococcus aureus (MRSA), have become a serious problem in hospitals and other areas all over the world. Thus, the development of an effective class of antibiotics against these bacteria is an urgent subject. Herein, we report a step‐economical and diversity‐oriented synthesis of a series of 2‐arylidenehydrazinyl‐4‐arylthiazole and 2‐arylidenehydrazinyl‐5‐arylthiazole analogues that utilizes C–H coupling methodologies. A library of 54 new congeners were synthesized and tested for their biological potential. Moreover, new knowledge regarding the structure–activity relationships (SARs) of these heterobiaryl compounds was collected.