29640-90-2Relevant academic research and scientific papers
MOF Decomposition and Introduction of Repairable Defects Using a Photodegradable Strut
Yan, Jingjing,MacDonald, John C.,Maag, Alex R.,Coudert, Fran?ois-Xavier,Burdette, Shawn C.
, p. 8393 - 8400 (2019/05/28)
Photoswitchable components can modulate the properties of metal organic frameworks (MOFs); however, photolabile building blocks remain underexplored. A new strut NPDAC (2-nitro-1,4-phenylenediacetic acid) that undergoes photodecarboxylation has been prepared and incorporated into a MOF, using post-synthetic linker exchange (PSLE) from the structural analogue containing PDAC (p-phenylenediacetic acid). Irradiation of NPDAC-MOF leads to MOF decomposition and concomitant formation of amorphous material. In addition to complete linker exchange, MOFs containing a mixture of PDAC and NPDAC can be obtained through partial linker exchange. In NPDAC30-MOF, which contains approximately 30 % NPDAC, the MOF retains crystallinity after irradiation, but the MOF contains defect sites consistent with loss of decarboxylated NPDAC linkers. The defect sites can be repaired by exposure to additional PDAC or NPDAC linkers at a much faster rate than the initial exchange process. The photoremoval and replacement process may lead to a more general approach to customizable MOF structures.
Synthesis and biological evaluation of loxoprofen derivatives
Yamakawa, Naoki,Suemasu, Shintaro,Matoyama, Masaaki,Tanaka, Ken-Ichiro,Katsu, Takashi,Miyata, Keishi,Okamoto, Yoshinari,Otsuka, Masami,Mizushima, Tohru
, p. 3299 - 3311 (2011/07/08)
Non-steroidal anti-inflammatory drugs (NSAIDs) achieve their anti-inflammatory actions through an inhibitory effect on cyclooxygenase (COX). Two COX subtypes, COX-1 and COX-2, are responsible for the majority of COX activity at the gastrointestinal mucosa and in tissues with inflammation, respectively. We previously suggested that both gastric mucosal cell death due to the membrane permeabilization activity of NSAIDs and COX-inhibition at the gastric mucosa are involved in NSAID-induced gastric lesions. We have also reported that loxoprofen has the lowest membrane permeabilization activity among the NSAIDs we tested. In this study, we synthesized a series of loxoprofen derivatives and examined their membrane permeabilization activities and inhibitory effects on COX-1 and COX-2. Among these derivatives, 2-{4′-hydroxy-5-[(2-oxocyclopentyl)methyl]biphenyl-2-yl}propanoate 31 has a specificity for COX-2 over COX-1. Compared to loxoprofen, oral administration of 31 to rats produced fewer gastric lesions but showed an equivalent anti-inflammatory effect. These results suggest that 31 is likely to be a therapeutically beneficial and safer NSAID.
8-Substituted 3,4-dihydroquinolinones as a novel scaffold for atypical antipsychotic activity
Singer, Jamie M.,Barr, Bridget M.,Coughenour, Linda L.,Gregory, Tracy F.,Walters, Michael A.
, p. 4560 - 4563 (2007/10/03)
Several new, potent dopamine subtype 2 (DA D2) active compounds with serotonin subtype 2A (5-HT2A) pharmacology are presented. 8-Substituted 3,4-dihydroquinolinones, tetrahydroquinolines, and N-acyl tetrahydroquinolines were evaluated in primary assays. Subtle changes on this novel scaffold translated to large changes in potency and selectivity in vitro. These compounds show promise as novel atypical antipsychotics for the treatment of schizophrenia.
