176860-56-3Relevant articles and documents
Synergism of a novel 1,2,4-oxadiazole-containing derivative with oxacillin against methicillin-resistant staphylococcus aureus
Buommino, Elisabetta,D’auria, Maria Valeria,De Marino, Simona,Festa, Carmen,Piccolo, Marialuisa,Sciarretta, Martina
, (2021/11/01)
Staphylococcus aureus is an important opportunistic pathogen that causes many infections in humans and animals. The inappropriate use of antibiotics has favored the diffusion of methicillin-resistant S. aureus (MRSA), nullifying the efforts undertaken in
Investigation around the Oxadiazole Core in the Discovery of a New Chemotype of Potent and Selective FXR Antagonists
Festa, Carmen,Finamore, Claudia,Marchianò, Silvia,Di Leva, Francesco Saverio,Carino, Adriana,Monti, Maria Chiara,Del Gaudio, Federica,Ceccacci, Sara,Limongelli, Vittorio,Zampella, Angela,Fiorucci, Stefano,De Marino, Simona
supporting information, p. 504 - 510 (2019/01/26)
Recent findings have shown that Farnesoid X Receptor (FXR) antagonists might be useful in the treatment of cholestasis and related metabolic disorders. In this paper, we report the discovery of a new chemotype of FXR antagonists featured by a 3,5-disubsti
QUINAZOLINONE-TYPE COMPOUNDS AS CRTH2 ANTAGONISTS
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Page/Page column 105, (2012/05/04)
This application provides for compounds of the formula Formula I or a pharmaceutically acceptable salt thereof, wherein the individual variables are defined herein, as well as processes to prepare these compounds, pharmaceutical compositions comprising the same and their use in treating disease state associated with the CRTH2 receptor.
PURINONE DERIVATIVES AS HM74A AGONISTS
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Page/Page column 59-60, (2008/06/13)
The present invention relates to purinone derivatives which are agonists of the HM74a receptor. Further provided are compositions and methods of using the compounds herein, and their pharmaceutically acceptable salts for the treatment of disease.
Acetic acid aldose reductase inhibitors bearing a five-membered heterocyclic core with potent topical activity in a visual impairment rat model
La Motta, Concettina,Sartini, Stefania,Salerno, Silvia,Simorini, Francesca,Taliani, Sabrina,Marini, Anna Maria,Da Settimo, Federico,Marinelli, Luciana,Limongelli, Vittorio,Novellino, Ettore
supporting information; experimental part, p. 3182 - 3193 (2009/04/06)
A number of 1,2,4-oxadiazol-5-yl-acetic acids and oxazol-4-yl-acetic acids were synthesized and tested for their ability to inhibit aldose reductase (ALR2). The oxadiazole derivatives, 7c, 7f, 7i, and 8h, 8i, proved to be the most active compounds, exhibiting inhibitory levels in the submicromolar range. In this series, the phenyl group turned out to be the preferred substitution pattern, as its lengthening to a benzyl moiety determined a general reduction of the inhibitory potency. The lead compound, 2-[3-(4-methoxyphenyl)-1,2,4- oxadiazol-5-yl]acetic acid, 7c, showed an excellent in vivo activity, proving to prevent cataract development in severely galactosemic rats when administered as an eye-drop solution in the precorneal region of the animals. Computational studies on the ALR2 inhibitors were performed to rationalize the structure-activity relationships observed and to provide the basis for further structure-guided design of novel ALR2 inhibitors.
Discovery of potent and selective SH2 inhibitors of the tyrosine kinase ZAP-70
Vu, Chi B.,Corpuz, Evelyn G.,Merry, Taylor J.,Pradeepan, Selvaluxmi G.,Bartlett, Catherine,Bohacek, Regine S.,Botfield, Martyn C.,Eyermann, Charles J.,Lynch, Berkley A.,MacNeil, Ian A.,Ram, Mary K.,Van Schravendijk, Marie Rose,Violette, Shelia,Sawyer, Tomi K.
, p. 4088 - 4098 (2007/10/03)
A series of 1,2,4-oxadiazole analogues has been shown to be potent and selective SH2 inhibitors of the tyrosine kinase ZAP-70, a potential therapeutic target for immune suppression. These compounds typically are 200- 400-fold more potent than the native,
