68266-50-2Relevant academic research and scientific papers
Design of noncompetitive interleukin-8 inhibitors acting on CXCR1 and CXCR2
Moriconi, Alessio,Cesta, Maria Candida,Cervellera, Maria Neve,Aramini, Andrea,Coniglio, Silvia,Colagioia, Sandro,Beccari, Andrea Rosario,Bizzarri, Cinzia,Cavicchia, Michela Rita,Locati, Massimo,Galliera, Emanuela,Di Benedetto, Paola,Vigilante, Paolo,Bertini, Riccardo,Allegretti, Marcello
, p. 3984 - 4002 (2008/02/11)
Chemokines CXCL8 and CXCL1 play a key role in the recruitment of neutrophils at the site of inflammation. CXCL8 binds two membrane receptors, CXCR1 and CXCR2, whereas CXCL1 is a selective agonist for CXCR2. In the past decade, the physiopathological role of CXCL8 and CXCL1 has been investigated. A novel class of small molecular weight allosteric CXCR1 inhibitors was identified, and reparixin, the first drug candidate, is currently under clinical investigation in the prevention of ischemia/reperfusion injury in organ transplantation. Reparixin binding mode to CXCR1 has been studied and used for a computer-assisted design program of dual allosteric CXCR1 and CXCR2 inhibitors. In this paper, the results of modeling-driven SAR studies for the identification of potent dual inhibitors are discussed, and three new compounds (56, 67, and 79) sharing a common triflate moiety have been selected as potential leads with optimized pharmacokinetic characteristics.
Synthesis and Antiinflammatory Activity of acetic Acids and Related Compounds
Terada, Atsusuke,Naruto, Shunji,Wachi, Kazuyuki,Tanaka, Shigeru,Iizuka, Yoshio,Misaka, Eiichi
, p. 212 - 216 (2007/10/02)
acetic acid derivatives and related compounds were synthesized to test their antiinflammatory and analgesic activities.Some of the compounds in this series were found to have good activity in the carrageenan edema test.Among them, sodium 2-phenyl>propionate dihydrate (15) and 2-phenyl>propionic acid (13b) showed potent analgesic and antiadjuvant arthritis activities with excellent antipyretic properties.
Novel phenylacetic acid derivatives
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, (2008/06/13)
Phenylacetic acid derivatives of the formula STR1 wherein n is an integer of 2 to 5; STR2 R1 is hydrogen, halogen, trifluoromethyl, nitro or amino; R2 and R3 each independently is hydrogen or lower alkyl; or together form an ethylene group; X1 represents two hydrogen atoms or an oxo group; and Y1 is cyano, hydroxyamidocarbonyl, carbamoyl, 5-tetrazolyl or carboxyl; and for derivatives wherein Y is carboxyl, salts thereof with physiologically compatible bases, esters thereof from physiologically acceptable alcohols and amides thereof from physiologically acceptable amines have valuable pharmacological activity, e.g., as antiinflammatory agents.
