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

Year Number of Results
1966 1
1967 1
1968 2
1969 5
1970 1
1971 2
1972 4
1973 10
1974 6
1975 8
1976 4
1977 3
1978 8
1979 3
1980 1
1981 7
1982 2
1983 1
1984 2
1985 3
1986 4
1987 2
1989 3
1990 3
1991 6
1992 1
1993 1
1994 11
1995 5
1996 8
1997 10
1998 8
1999 10
2000 8
2001 13
2002 15
2003 17
2004 24
2005 28
2006 27
2007 26
2008 30
2009 38
2010 29
2011 26
2012 37
2013 36
2014 24
2015 37
2016 39
2017 33
2018 15
2019 8
2020 0
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588 results
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Page 1
Heterocyclic N-Oxides - An Emerging Class of Therapeutic Agents.
Mfuh AM and Larionov OV. Curr Med Chem 2015 - Review. PMID 26087764 Free PMC article.
Heterocyclic N-oxides have emerged as potent compounds with anticancer, antibacterial, antihypertensive, antiparasitic, anti-HIV, anti-inflammatory, herbicidal, neuroprotective, and procognitive activities. The N-oxide motif has been successfully employed in a number of recent drug development projects. This review surveys the emergence of this scaffold in the mainstream medicinal chemistry with a focus on the discovery of the heterocyclic N-oxide drugs, N-oxide-specific mechanisms of action, drug-receptor interactions and synthetic avenues to these compounds. ...
Heterocyclic N-oxides have emerged as potent compounds with anticancer, antibacterial, antihypertensive, antiparasitic, anti-H …
Heterocyclic N-oxides - A Promising Class of Agents against Tuberculosis, Malaria and Neglected Tropical Diseases.
Dos Santos Fernandes GF, et al. Curr Pharm Des 2018 - Review. PMID 29663875
Heterocyclic N-oxides have emerged as promising agents against a number of diseases and disorders, especially infectious diseases. ...A number of heterocyclic N-oxides are described herein, nevertheless, the following chemical classes deserve to be highlighted due to a large number of reports in the literature about their promising pharmacological effects: furoxan, benzofuroxan, quinoxaline 1,4-di-N-oxide, indolone N-oxide and benzimidazole N-oxide. ...
Heterocyclic N-oxides have emerged as promising agents against a number of diseases and disorders, especially infectious disea …
Activity-based protein profiling reveals off-target proteins of the FAAH inhibitor BIA 10-2474
van Esbroeck ACM, et al. Science 2017. PMID 28596366 Free PMC article.
Here we use activity-based proteomic methods to determine the protein interaction landscape of BIA 10-2474 in human cells and tissues. ...
Here we use activity-based proteomic methods to determine the protein interaction landscape of BIA 10-2474 in human cells and tissues …
TGN-1412 and BIA-2474 Trials with Tragic End: Lessons Learnt To Make Clinical Trials Safer
Kaur RJ, et al. Rev Recent Clin Trials 2018 - Review. PMID 29779485
METHODS: Some stipulated measures to improve safety of clinical trial participants include inclusion of patients instead of healthy volunteers in phase I clinical trials, all compounds which are used for first time in humans should be considered as high risk compounds, amendments in first in human clinical trial design to N of 1 randomized control trial in place of 6+2 design with the sequential dosing of subjects both within and between cohorts and the individual patient pharmacokinetic and pharmacodynamic data should be used to calculate sequential dosing. Besides these, there should be appropriate process for systematic risk assessment involving the use of statistical techniques to select pertinent risk factors with high predictive values of studies or sites that may be procumbent to non-compliance. ...
METHODS: Some stipulated measures to improve safety of clinical trial participants include inclusion of patients instead of healthy voluntee …
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 …
Take Care of the Fast-in-Human Study
van Hoogdalem EJ. Clin Transl Sci 2017. PMID 27981812 Free PMC article.
Reactive oxygen species scavengers ameliorate mechanical allodynia in a rat model of cancer-induced bone pain
Zhou YQ, et al. Redox Biol 2018. PMID 29055283 Free PMC article.
Our results found that intraperitoneal injection of N-tert-Butyl-α-phenylnitrone (PBN, 50 and 100mg/kg) and 4-hydroxy-2,2,6,6-tetramethylpiperidine-1-oxyl (Tempol, 100 and 200mg/kg) significantly suppressed the established mechanical allodynia in CIBP rats. ...
Our results found that intraperitoneal injection of N-tert-Butyl-α-phenylnitrone (PBN, 50 and 100mg/kg) and 4-hydroxy-2,2,6,6-tetrame …
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