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Table representation of search results timeline featuring number of search results per year.

Year Number of Results
1967 2
1968 4
1969 5
1970 4
1971 2
1972 10
1973 7
1974 12
1975 16
1976 14
1977 24
1978 13
1979 7
1980 11
1981 27
1982 20
1983 16
1984 18
1985 10
1986 18
1987 20
1988 8
1989 22
1990 12
1991 25
1992 28
1993 24
1994 32
1995 27
1996 25
1997 22
1998 31
1999 25
2000 23
2001 21
2002 34
2003 31
2004 43
2005 42
2006 55
2007 50
2008 42
2009 36
2010 42
2011 45
2012 55
2013 44
2014 53
2015 50
2016 39
2017 35
2018 33
2019 13
2020 0
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1,232 results
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Page 1
Discovery of a Potent, Long-Acting, and CNS-Active Inhibitor (BIA 10-2474) of Fatty Acid Amide Hydrolase
Kiss LE, et al. ChemMedChem 2018. PMID 30113139 Free PMC article.
Herein we report the design and synthesis of a novel series of heterocyclic-N-carboxamide FAAH inhibitors that have a good alignment of potency, metabolic stability and selectivity for FAAH over monoacylglycerol lipase (MAGL) and carboxylesterases (CEs). Lead optimization efforts carried out with benzotriazolyl- and imidazolyl-N-carboxamide series led to the discovery of clinical candidate 8 l (3-(1-(cyclohexyl(methyl)carbamoyl)-1H-imidazol-4-yl)pyridine 1-oxide; BIA 10-2474) as a potent and long-acting inhibitor of FAAH. ...
Herein we report the design and synthesis of a novel series of heterocyclic-N-carboxamide FAAH inhibitors that have a good alignment …
2-Hydroxypyridine-N-oxide (HOPO): Equivocal in the ames assay.
Dobo KL, et al. Environ Mol Mutagen 2018. PMID 29481708
2-Hydroxypyridine-N-oxide (HOPO) is a useful coupling reagent for synthesis of active pharmaceutical ingredients. It has been reported to be weakly mutagenic in the Ames assay (Ding W et al. []: J Chromatogr A 1386:47-52). ...
2-Hydroxypyridine-N-oxide (HOPO) is a useful coupling reagent for synthesis of active pharmaceutical ingredients. It has been reporte …
An in vitro comparison of the cytotoxic potential of selected dehydropyrrolizidine alkaloids and some N-oxides.
Field RA, et al. Toxicon 2015. PMID 25666399
None of the DHPA-N-oxides were significantly cytotoxic at these concentrations. Using graphic analyses the median cytotoxic concentration (DHPA concentration that produced ½ the maximum response) were estimated. The estimated descending order of cytotoxicity was lasiocarpine, seneciphylline, senecionine, heliotrine, riddelliine, monocrotaline, riddelliine-N-oxide, lycopsamine, intermedine, lasiocarpine-N-oxide and senecionine-N-oxide. ...
None of the DHPA-N-oxides were significantly cytotoxic at these concentrations. Using graphic analyses the median cytotoxic co …
Experimental and theoretical study of the interaction of 3-carboxy-5,6-benzocoumarin with some 1,2,3,4,5,6,7,8-octahydroacridines and the corresponding N-oxides.
Marinescu M, et al. Spectrochim Acta A Mol Biomol Spectrosc 2011. PMID 21763182
The interaction of 3-carboxy-5,6-benzocoumarin (BzCum) with 1,2,3,4,5,6,7,8-octahydroacridine (OHA), 9-amino-1,2,3,4,5,6,7,8-octahydroacridine (H(2)N-OHA) and the corresponding N-oxides (OHA-NO and H(2)N-OHA-NO) was studied by fluorescence (steady state, time resolved) and absorption spectroscopy. The analysis of the fluorescence data in terms of Stern-Volmer plots indicated a predominant dynamic quenching for OHA and OHA-NO, and a more complex process for H(2)N-OHA and H(2)N-OHA-NO. ...
The interaction of 3-carboxy-5,6-benzocoumarin (BzCum) with 1,2,3,4,5,6,7,8-octahydroacridine (OHA), 9-amino-1,2,3,4,5,6,7,8-octahydroacridi …
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