Blog

2,4- and 2,5-Disubstituted Arylthiazoles: Rapid Synthesis by C–H Coupling and Biological Evaluation

Lilia Lohrey, Takahiro N. Uehara, Satoshi Tani,  Junichiro Yamaguchi, Hans-Ulrich Humpf and Kenichiro Itami

Eur. J. Org. Chem. 2014, Early View. DOI: 10.1002/ejoc.201402129

Life-threatening infections caused by bacteria that have developed resistance to common antibiotics, such as methicillin-resistantStaphylococcus 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.

Related post

  1. Pd-Catalyzed Direct C–H Bond Fun…
  2. Synthesis and Properties of [8]-…
  3. Nickel-Catalyzed α-Arylation of …
  4. Synthesis of Thiophene-Based TAK…
  5. Decarbonylative Diaryl Ether Syn…
  6. Rapid Access to Kinase Inhibitor…
  7. Synthesis of Cycloiptycenes from…
  8. Regioselective Unsymmetrical Tet…

最近の記事

Flickr@Itamilab

天池先輩からコーヒースープ伴夫妻からのお歳暮です!潤さん、宮村さん、ありがとうございます!!武藤さん、ビールありがとうございます!平賀大都わーいやなさん、あつしさん、ありがとうございます!!だいぶ前だけど、Stripes look #ootdHalloween lookラインを洗う時ですら格好良く。戸谷先生教育実習!imageけいしゅう、誕生日おめでとう!誕生日は英吉家!!3年生に名古屋ぼろ勝ちアピール中!!アリシア卒業おめでとう女子会!
PAGE TOP