143659-19-2Relevant articles and documents
Synthesis of Nanostructured Organosilicon Luminophores Based on Phenyloxazoles
Skorotetcky,Borshchev,Cherkaev,Ponomarenko
, p. 25 - 41 (2019/04/27)
A series of nanostructured organosilicon luminophores (NOLs) composed of a central 1,4-bis(5-phenyl-1,3-oxazol-2-yl)benzene (POPOP) acceptor chromophore and various peripheral p-terphenyl and 2,5-diphenyl-1,3-oxazole donor fragments have been synthesized for the first time using van Leusen reaction and direct palladium-catalyzed C-arylation of oxazole ring. Due to different functionalities of the silicon branching centers, NOLs with different donor-acceptor ratios have been obtained. The synthesized structures are expected to possess good optical characteristics for use in photonics and optoelectronics.
Targeted Polypharmacology: Discovery of a Highly Potent Non-Hydroxamate Dual Matrix Metalloproteinase (MMP)-10/-13 Inhibitor
Senn, Nicole,Ott, Michael,Lanz, Jan,Riedl, Rainer
, p. 9585 - 9598 (2017/12/26)
Matrix metalloproteinases (MMPs) play a key role in many diseases like cancer, atherosclerosis or arthritis. Interest in MMP inhibition has been revitalized very recently as the knowledge on the underlying network of biological pathways is steadily growing. On the basis of this new insight into the relevance of MMP-10 and MMP-13 within the MMP network and the ban of hydroxamate inhibitors from clinical development, the discovery of non-hydroxamate multitarget drugs against specific MMPs is of foremost interest. Here, we disclose the discovery of a very potent and selective non-hydroxamate MMP-10/-13 inhibitor. The high potency (IC50 of 31 nM [MMP-10] and 5 nM [MMP-13]) and selectivity over MMP-1, -2, -3, -7, -8, -9, -12, and -14 enable this compound to decipher disease causing MMP networks and to generate new treatment options through targeted polypharmacology.
A One-Pot Tandem Approach for the Synthesis of 5-(Het)aryloxazoles from Substituted (Het)aryl Methyl Alcohols and Benzyl Bromides
Vinay Kumar, Koravangala S.,Swaroop, Toreshettahally R.,Rajeev, Narasimhamurthy,Vinayaka, Ajjampura C.,Lingaraju, Gejjalagere S.,Rangappa, Kanchugarakoppal S.,Sadashiva, Maralinganadoddi P.
supporting information, p. 1363 - 1366 (2016/06/01)
A new modified van Leusen strategy has been developed for the synthesis of biologically significant 5-substituted oxazoles by the reaction of (het)aryl methyl alcohols or benzyl bromides as precursors with tosylmethylisocyanide (TosMIC) under basic conditions. This method is efficient, takes place under mild reaction conditions, and is tolerant of various functional groups with high yield.