- Identification of bivalent ligands with melatonin receptor agonist and fatty acid amide hydrolase (FAAH) inhibitory activity that exhibit ocular hypotensive effect in the rabbit
-
Activation of melatonin receptors and inhibition of fatty acid amide hydrolase (FAAH) have both shown potential benefits for the treatment of glaucoma. To exploit the combination of these biological activities in single therapeutic agents, we designed dua
- Spadoni, Gilberto,Bedini, Annalida,Furiassi, Lucia,Mari, Michele,Mor, Marco,Scalvini, Laura,Lodola, Alessio,Ghidini, Andrea,Lucini, Valeria,Dugnani, Silvana,Scaglione, Francesco,Piomelli, Daniele,Jung, Kwang-Mook,Supuran, Claudiu T.,Lucarini, Laura,Durante, Mariaconcetta,Sgambellone, Silvia,Masini, Emanuela,Rivara, Silvia
-
p. 7902 - 7916
(2018/09/18)
-
- Synthesis of Some Selectively N-Protected (1S,2S)-p-Nitrophenylserinol-Based Diamino-1,3-dioxanes and Tripodands
-
The unconventional methodology for the non-epimerizable cycloacetalization of optically active (1S,2S)-2-amino-1-(4-nitrophenyl)propane-1,3-diol (p-nitrophenylserinol) (condensed H2SO4 96% as solvent and catalyst, i.e., sulfuric transacetalization) producing (2R,4S,5S) diamino-1,3-dioxanes was enlarged by the use of N-protected forms of 2,2-dimethoxyethylamine (DMEA, aminoacetaldehyde dimethylacetal). Conversely, N-protected derivatives of p-nitrophenylserinol were successfully cyclocondensed with DMEA in the same sulfuric conditions. N-Functionalization of DMEA upon treatment with trimesic acid trichloride and cyanuric chloride yielded the corresponding triple amide and melamine, respectively. Their adapted sulfuric transacetalization in triplicate in reaction with arylserinols (aryl: phenyl, p-nitrophenyl) afforded a new series of optically active tripodands.
- Nagy, Iulia,Moldovan, Oana,Popa, Flavia,Lameiras, Pedro,Morar, Cristina,Sacalis, Carmen,Darabantu, Mircea
-
supporting information
p. 2319 - 2330
(2015/10/12)
-
- PROCESS FOR THE PREPARATION OF 5-(2-AMINO-PYRIMIDIN-4-YL)-2-ARYL-1H-PYRROLE-3-CARBOXAMIDES
-
The invention relates to a process for the preparation of 5-(2-amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carboxamides and to the useful intermediate compounds of such process. The process allows to obtain the desired products in high yields and purity. Th
- -
-
Page/Page column 5
(2012/09/10)
-
- PROCESS FOR THE PREPARATION OF 5-(2-AMINO-PYRIMIDIN-4-YL)-2-ARYL-1H-PYRROLE-3-CARBOXAMIDES
-
The invention relates to a process for the preparation of 5-(2-amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3- carboxamides and to the useful intermediate compounds of such process. The process allows to obtain the desired products in high yields and purity. T
- -
-
Page/Page column 7
(2011/06/11)
-
- Direct, one-pot reductive alkylation of anilines with functionalized acetals mediated by triethylsilane and tfa. straightforward route for unsymmetrically substituted ethylenediamine
-
A new, robust, and reliable method has been developed for the selective reductive N-alkylation of primary and secondary aromatic amines with some functionalized acetals using TFA/Et3SiH as a reagent combination. A variety of unsymmetrically sub
- Righi, Marika,Bedini, Annalida,Piersanti, Giovanni,Romagnoli, Federica,Spadoni, Gilberto
-
supporting information; experimental part
p. 704 - 707
(2011/03/22)
-
- Sialidase inhibitors related to GG167: Synthesis of analogues via an inverse demand hetero Diels Alder reaction
-
An inverse demand hetero Diels Alder strategy has been utilised for the synthesis of novel dihydropyrans as potential inhibitors of influenza virus sialidase. Cyclisation of 1-methoxy-2-acetamido ethene with 2-oxo-4-butoxycarbonylamino but-3-(Z)-enoic acid t-butyl ester in the presence of tin (IV) chloride afforded a mixture of regio- and stereochemical isomers which were further elaborated to analogues of GG167.
- Howes, Peter D.,Smith, Paul W.
-
p. 6595 - 6598
(2007/10/03)
-
- Derivatives of 2-aminoalkyl-5-arylalkyl-1,3-dioxanes, their preparation and their therapeutic application
-
A compound which is a 2-aminoalkyl-5-arylalkyl-1,3-dioxane of general formula (I) STR1 in which m represents 0 or 1; n represents 1, 2, 3 or 4; R1 represents hydrogen or methyl; R2 represents hydrogen, methyl or an alkanoyl group of the general formula COR' in which R' represents a hydrogen atom or a linear or branched C1 -C4 -alkyl group, or an alkoxycarbonyl group of the general formula COOR" in which R" represents a linear or branched C1 -C4 -alkyl group; and Ar represents either a phenyl group optionally carrying one or two substituents selected from halogen, C1 -C4 alkyl, methoxy and trifluoromethyl, or a naphthalen-1-yl or naphthalen-2-yl group optionally carrying a substituent selected from halogen, methyl, methoxy and cyclopropylmethoxy groups, in the form of a cis- or trans-stereoisomer, and in the form of a free base or an acid addition salt thereof and its therapeutic use.
- -
-
-
- Thiohemiacetal formation by inhibitory aldehydes at the active site of papain.
-
Papain is strongly inhibited by aldehydes resembling carboxylic acids, released by hydrolysis of specific substrates (Westerik, J. O''C., and Wolfenden, R. (1972), J. Biol. Chem. 247, 8195-8197). Inhibitory complexes might involve binding of the aldehyde intact or as a covalent hydrate, or the aldehyde might undergo covalent addition of an active site sulfhydryl group to form a thiohemiacetal derivative. In an attempt to distinguish between these possibilities, benzamidoacetaldehyde-1-d has been synthesized, and its properties compared with those of the undeuterated inhibitor. After correction for differences in hydration, the observed effect on inhibition is found to be compatible with formation of a thiohemiacetal. In keeping with this conclusion, benzamidoethanol (a partial analogue of the covalent hydrate) and benzamide, N-methylbenzamide and N-ethylbenzamide (somewhat similar to the free aldehyde in size and hydrophobic character) are found to exhibit negligible affinity for the active site.
- Lewis,Wolfenden
-
p. 4890,4891
(2007/10/05)
-