279231-56-0Relevant academic research and scientific papers
Bicyclic compounds
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, (2008/06/13)
The present invention is directed to new bicyclic compounds of the formula [I], and pharmaceutically acceptable salts thereof wherein R1, R2, R3, R4, R5, R6, R7, Q1Q2and Q3are as defined in the claims. The compounds have N-myristoyltransferase inhibitory and antifungal activity.
Design and synthesis of novel benzofurans as a new class of antifungal agents targeting fungal N-myristoyltransferase. Part 1
Masubuchi, Miyako,Kawasaki, Ken-ichi,Ebiike, Hirosato,Ikeda, Yoshihiko,Tsujii, Shinji,Sogabe, Satoshi,Fujii, Toshihiko,Sakata, Kiyoaki,Shiratori, Yasuhiko,Aoki, Yuko,Ohtsuka, Tatsuo,Shimma, Nobuo
, p. 1833 - 1837 (2007/10/03)
Potent and selective Candida albicans N-myristoyltransferase (CaNmt) inhibitors have been identified through optimization of a lead compound 1 discovered by random screening. The inhibitor design is based on the crystal structure of the CaNmt complex with compound (S)-3 and structure-activity relationships (SARs) have been clarified. Modification of the C-4 side chain of 1 has led to the discovery of a potent and selective CaNmt inhibitor 11 (RO-09-4609), which exhibits antifungal activity against C. albicans in vitro.
