3361-72-6Relevant academic research and scientific papers
HYDANTOIN DERIVATIVES USEFUL AS KV3 INHIBITORS
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, (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.
HYDANTOIN DERIVATIVES USEFUL AS KV3 INHIBITORS
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, (2012/06/30)
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.
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.
Method of preparing 2-acylresorcinols
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, (2008/06/13)
A method of preparing a 2-acylresorcinol which comprises dehydrogenating a 2-acyl-1,3-cyclohexanedione of the general formula wherein R1 represents an alkyl, aralkyl or aryl group, and RZrepresents hydrogen, or an alkyl, alkoxy or acylamino group, in the presence of a dehydrogenation catalyst (such as a Group VIII metal) or a dehydrogenation agent (such as sulphur or selenium) at an elevated temperature, to provide a 2-acylresorcinol of the general formula wherein R1 and R2 are as defined.
Fluoro-sulfones
-
, (2008/06/13)
Compounds of Formula I are described. They are antagonists of leukotrienes and SRS-A.
Fluoro-sulfones
-
, (2008/06/13)
Compounds of Formula I STR1 the pharmaceutically acceptable salts, and the gamma-lactone form thereof are described. They are antagonists of leukotrienes and SRS-A.
A Convenient Synthesis of 2-Alkyl-mono-O-alkylated and 2-Alkyl Resorcinols
Stealey, M.A.,Shone, R.L.,Miyano, M.
, p. 1869 - 1876 (2007/10/02)
The title C,O-dialkylated resorcinols have seldom been prepared.We have developed a practical synthesis of this class of compounds starting with cyclohexane-1,3-dione.The key features of the synthesis are mono-O-alkylation of a 2-alkyl cyclohexane-1,3-dio
REARRANGEMENT OF 2-ACYL-2-CHLORO-1,3-CYCLOHEXANEDIONES INTO 2-ACYLRESORCINOLS AND 2-ACYL-4-CHLORO-1,3-CYCLOHEXANEDIONES
De Buyck, L.,Seynaeve, D.,De Kimpe, N.,Verhe, R.,Schamp, N.
, p. 363 - 370 (2007/10/02)
2-Acetylresorcinol was prepared in 80-88percent yield from 2-acetyl-1,3-cyclohexanedione by 2-chlorination (excess of NCS in boiling carbon tetrachloride or one equivalent of molecular chlorine in the cold solvent) followed by aromatization in a heated dry solution of hydrogen chloride in dimethylformamide.The scope of the method was extended to the preparation of 2-propionyl- and 2-isobutyrylresorcinol (resp. 79percent and 66percent yield).Application of the method on 2-acryl-5,5-dimethyl-1,3-cyclohexanediones (acyl=acetyl, propionyl, n-butyryl, i-butyryl) affrded the corresponding 2-acyl-4-chlorodimedone derivatives in 40-77percent yields.
