3361-72-6Relevant articles and documents
HYDANTOIN DERIVATIVES USEFUL AS KV3 INHIBITORS
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Paragraph 0561-0563, (2013/10/22)
The invention provides compounds of formula (I): Said compounds being inhibitors of Kv3 channels and of use in the prophylaxis or treatment of related disorders.
Synthesis of propiophenone derivatives as new class of antidiabetic agents reducing body weight in db/db mice
Kumar, Atul,Sharma, Siddharth,Gupta, Lalit Prakash,Ahmad, Pervez,Srivastava, Swayam Prakash,Rahuja, Neha,Tamrakar,Srivastava, Arvind K.
scheme or table, p. 2172 - 2179 (2012/04/23)
A series of propiophenone derivatives (6-23) have been synthesized and evaluated for their in vivo antihyperglycemic activities in sucrose loaded model (SLM), sucrose challenged streptozotocin (STZ-S) induced diabetic rat model and C57BL/KsJ db/db diabetic mice model. Compound 15 and 16 were emerged as potent antihyperglycemics and lipid lowering agents. These compounds (15, 16) further validate the potency by reducing body weight and food intake in db/db mice model. Possible mechanism of action for the propiophenone derivatives was established by the evaluation in various in vitro models. Interestingly some of the compounds were efficiently inhibiting PTP-1B.
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.