Franklin C

References (3)

Title : 4,5-Dimethoxy-2-nitrobenzohydrazides and 1-(1-Benzylpiperidin-4-yl)ethan-1-ones as Potential Antioxidant\/Cholinergic Endowed Small Molecule Leads - Banu_2017_Sci.Pharm_86_
Author(s) : Banu R , Gerding J , Franklin C , Sikazwe D , Horton W , Torok M , Davis J , Cheng KH , Nakazwe M , Mochona B
Ref : Sci Pharm , 86 : , 2017
Abstract : The objective of this research is to generate leads for developing our ultimate poly-active molecules with utility in central nervous system (CNS) diseases. Indeed, poly-active molecules capable of mitigating brain free radical damage while enhancing acetylcholine signaling (via cholinesterase inhibition) are still being sought for combating Alzheimer's disease (AD). We differentiate "poly-active" agents from "multi-target" ones by defining them as single molecular entities designed to target only specific contributory synergistic pharmacologies in a disease. For instance, in AD, free radicals either initiate or act in synergy with other pharmacologies, leading to disease worsening. For this preliminary report, a total of 14 (i.e., 4,5-dimethoxy-2-nitrobenzohydrazide plus 1-(1-benzylpiperidin-4-yl)ethan-1-one) derivatives were synthesized and screened, in silico and in vitro, for their ability to scavenge free radicals and inhibit acetylcholinesterase (AChE)/butyrylcholinesterase (BuChE) enzymes. Overall, six derivatives (4a, 4d, 4e, 4f, 4g, 9b) exhibited potent (>30%) antioxidant properties in the oxygen radical absorbance capacity (ORAC) assay. The antioxidant values were either comparable or more potent than the comparator molecules (ascorbic acid, resveratrol, and trolox). Only three compounds (4d, 9a, 9c) yielded modest AChE/BuChE inhibitions (>10%). Please note that a SciFinder substance data base search confirmed that most of the compounds reported herein are new, except 9a and 9c which are also commercially available.
ESTHER : Banu_2017_Sci.Pharm_86_
PubMedSearch : Banu_2017_Sci.Pharm_86_
PubMedID: 29267246

Title : A tiered approach to systemic toxicity testing for agricultural chemical safety assessment - Doe_2006_Crit.Rev.Toxicol_36_37
Author(s) : Doe JE , Boobis AR , Blacker A , Dellarco V , Doerrer NG , Franklin C , Goodman JI , Kronenberg JM , Lewis R , McConnell EE , Mercier T , Moretto A , Nolan C , Padilla S , Phang W , Solecki R , Tilbury L , van Ravenzwaay B , Wolf DC
Ref : Crit Rev Toxicol , 36 :37 , 2006
Abstract : A proposal has been developed by the Agricultural Chemical Safety Assessment (ACSA) Technical Committee of the ILSI Health and Environmental Sciences Institute (HESI) for an improved approach to assessing the safety of crop protection chemicals. The goal is to ensure that studies are scientifically appropriate and necessary without being redundant, and that tests emphasize toxicological endpoints and exposure durations that are relevant for risk assessment. The ACSA Systemic Toxicity Task Force proposes an approach to systemic toxicity testing as one part of the overall assessment of a compound's potential to cause adverse effects on health. The approach is designed to provide more relevant data for deriving reference doses for shorter time periods of human exposure, and includes fewer studies for deriving longer term reference doses-that is, neither a 12-month dog study nor a mouse carcinogenicity study is recommended. All available data, including toxicokinetics and metabolism data and life stages information, are taken into account. The proposed tiered testing approach has the potential to provide new risk assessment information for shorter human exposure durations while reducing the number of animals used and without compromising the sensitivity of the determination of longer term reference doses.
ESTHER : Doe_2006_Crit.Rev.Toxicol_36_37
PubMedSearch : Doe_2006_Crit.Rev.Toxicol_36_37
PubMedID: 16708694

Title : Hypotension and cardiac arrest in rats after infusion of mono(2-ethylhexyl)phthalate (MEHP), a contaminant of stored blood -
Author(s) : Rock G , Labow RS , Franklin C , Burnett R , Tocchi M
Ref : N Engl J Med , 316 :1218 , 1987
PubMedID: 3574376