106748-24-7Relevant articles and documents
A palladium-catalyzed carbonylative route to primary amides
Morera, Enrico,Ortar, Giorgio
, p. 2835 - 2838 (1998)
The palladium-catalyzed reaction of aryl and vinyl iodides and triflates with carbon monoxide in the presence of hexamethyldisilazane followed by hydrolytic work-up affords aromatic and α,β-unsaturated primary amides in good to high yields under relatively mild conditions.
Design and synthesis of 3-aminophthalazine derivatives and structural analogues as PDE5 inhibitors: anti-allodynic effect against neuropathic pain in a mouse model
Bollenbach, Maud,Lugnier, Claire,Kremer, Mélanie,Salvat, Eric,Megat, Salim,Bihel, Frédéric,Bourguignon, Jean-Jacques,Barrot, Michel,Schmitt, Martine
, p. 269 - 290 (2019/06/05)
Neuropathic pain is a chronic pain caused by a lesion or disease affecting the somatosensory nervous system. To date, no specific treatment has been developed to cure this pain. Antidepressants and anticonvulsant drugs are used, but they do not demonstrate universal efficacy, and they often cause detrimental adverse effects. Some studies highlighted the efficacy of sildenafil, a well-known inhibitor of phosphodiesterase 5 (PDE5, (IC50 = 3.3 nM)), in models of pain. Based on these results, we focused our attention on MY 5445, another known PDE5 inhibitor. Homologues, isosteres and structural analogues of MY 5445 were designed and all synthesized compounds were evaluated for their inhibitory activity toward PDE5. Selectivity profiles towards other PDE1-4 isoenzymes, water solubility and stability in acidic medium of the most potent PDE5 inhibitors were determined and the aminophthalazine 16h and its mimetic 41n (3-aminoindazole)were evaluated in comparison to MY 5445 (4b)in vivo in a model of neuropathic pain induced by sciatic nerve cuffing in mice (3 and 0.5 mg/kg, ip twice a day). Both compounds showed the same efficacy on neuropathic allodynia as MY 5445, and thus produced a significant relief of mechanical hypersensitivity after 12 days of treatment.
Selective aerobic hydrolysis of nitriles to amides using cobalt(II)/zinc
Keshipour, Sajjad,Shaabani, Ahmad
, p. 5071 - 5078 (2015/07/08)
A novel protocol has been developed for the aerobic hydrolysis of nitriles to amides using cobalt(II)/zinc without using any strong acids and bases under solvent-free conditions. The reaction showed good performance for benzonitriles with sensitive groups such as ester and carboxylic acid.
Microwave-assisted N-debenzylation of amides with triflic acid
Rombouts, Frederik,Franken, Dennis,Martínez-Lamenca, Carolina,Braeken, Mirielle,Zavattaro, Chiara,Chen, Jinsheng,Trabanco, Andrés A.
experimental part, p. 4815 - 4818 (2010/10/02)
A new and facile microwave-assisted protocol for the debenzylation of N-benzylamides with triflic acid has been developed. Both secondary and tertiary aliphatic or aromatic amides are obtained in moderate to good yields.
Synthesis and properties of some novel anti-calmodulin drugs
Sakai, Ted T.,Krishna, N. Rama
, p. 1559 - 1565 (2007/10/03)
The preparation and properties of some novel inhibitors of calmodulin function are described. The compounds are cationic derivatives of phenyl-substituted thiazoles which inhibit the calmodulin stimulation of cyclic-AMP phosphodiesterase and are active against animal tumor cells in culture. These derivatives form the basis for the preparation of new, more potent inhibitors of calmodulin function which could take advantage of the reported elevated levels of calcium-bound calmodulin in tumor cells and show preferential anti-tumor activity. Copyright (C) 1999 Elsevier Science Ltd.
