- Thiazole- and imidazole-containing peptidomimetic inhibitors of protein farnesyltransferase
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Mimetics of the C-terminal CAAX tetrapeptide of Ras protein were designed replacing internal dipeptide AA with 4-amino-2-phenylbenzoic acid and cysteine (C) with 2-amino-4-thiazolyl-, 2-mercapto-4-thiazolyl-, 2-mercapto-4-imidazolyl- and 2-methylmercapto-4-thiazolyl-acetic or propionic acid. The compound in which C is replaced by 2-amino-4-thiazolylacetic acid inhibited FTase activity in the low nanomolar range and showed antiproliferative effect on rat aortic smooth muscle cells interfering with Ras farnesylation. On the basis of these results, 2-aminothiazole can be considered as an alternative to heterocycles, such as pyridine and imidazole, normally used in FTase inhibitors designed as non-thiol CAAX mimetics.
- Bolchi, Cristiano,Pallavicini, Marco,Bernini, Sergio K.,Chiodini, Giuseppe,Corsini, Alberto,Ferri, Nicola,Fumagalli, Laura,Straniero, Valentina,Valoti, Ermanno
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scheme or table
p. 5408 - 5412
(2011/10/12)
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- CARBOXYLIC ACID DERIVATIVE CONTAINING THIAZOLE RING AND PHARMACEUTICAL USE THEREOF
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According to the present invention, a compound represented by the following formula (I) having a superior PPARα, agonist action and concurrently showing a hypolipidemic action can be provided, and further, a compound useful as a synthetic intermediate for the compound can be provided.
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Page/Page column 31
(2010/11/28)
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- MORPHOLINE COMPOUND
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A compound represented by the formula (1) wherein ring A is aryl optionally having substituent(s) and the like; ring B is arylene optionally having substituent(s) and the like; m=0-2; n=1-5; X is a bond and the like; Y is a bond and the like; and Z is hydrogen atom and the like or a pharmaceutically acceptable salt thereof, and a hydrate or solvate thereof have affinity for CCR3, and can be pharmaceutical products for the treatment and/or prophylaxis of immune or inflammatory diseases.
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Page/Page column 27
(2010/11/27)
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- Studies on anti-Helicobacter pylori agents. Part 3: A novel, efficacious cephem derivative, FR193879
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The synthesis, therapeutic efficacy against H. pylori, and preliminary safety of the novel cephem derivative, FR193879 (8a) are described. Compound 8a having a (4-carbamoylmethylthiazol-2-yl)thio moiety at the 3-position and a phenylacetamido at the 7-position was found to have good safety showing a nontoxic dose of 100mg/kg in dogs in a 4-week repeat dose toxicity study and extremely potent therapeutic efficacy against H. pylori, showing 30 times superior activity compared to AMPC, and did not display cross-resistance with CAM or MNZ.
- Yoshida, Yoshiki,Matsuda, Keiji,Sasaki, Hiroshi,Matsumoto, Yoshimi,Matsumoto, Satoru,Tawara, Shuichi,Takasugi, Hisashi
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p. 2627 - 2631
(2007/10/03)
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- REDUCTIVE CLEAVAGE OF SYMMETRICAL DISULFIDES WITH HYDRAZINES
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An efficient method for the reductive cleavage of symmetrical disulfides with hydrazines is described.
- Maiti, Samarendra N.,Spevak, Paul,Singh, Maya Prakash,Micetich, Ronald G.,Reddy, A. V. Narender
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p. 575 - 582
(2007/10/02)
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