Synthesis and Biological Activity Determinations of Some N- aminotetrahydropyridines The primary objective is the design, synthesis and pharmacological evaluation of novel and medicinally important N-amino-1,2,3,6- tetrahydropyridine derivatives. We reported the synthesis of novel N- iminopyridinium ylides using the method employed by Tamura and modified in our laboratory. Sodium borohydride reduction of the ylides afforded preliminary pharmacological test results of a few tetrahydropyridines that exhibited analgesic and anti-inflammatory activities with no observed toxicity, even at very high dose levels. Our earlier work provides the basis for new and exciting studies so that a series of compounds related to athe most active analogs could be prepared, and retested and the octanol-water partition coefficient determined. Once sufficient data are accumulated, the compounds prepared will be subjected to structure activity analysis to study the electronic, steric and lipophilic effects of substituents. The physical and pharmacological data obtained in this study will then be used to design drugs with more beneficial biological activity. The primary focus of the pharmacological studies will be to develop an easily synthesized, effective and safe nonsteroidal anti-inflammatory agent for the treatment of rheumatic diseases, including rheumatoid arthritis, osteoarthritis, gout and rheumatic fever.

Project Start
1998-05-01
Project End
1999-04-30
Budget Start
1998-10-01
Budget End
1999-09-30
Support Year
27
Fiscal Year
1999
Total Cost
Indirect Cost
Name
Florida Agricultural and Mechanical University
Department
Type
DUNS #
City
Tallahassee
State
FL
Country
United States
Zip Code
32307
Johnston, Jermaine G; Pollock, David M (2018) Circadian regulation of renal function. Free Radic Biol Med 119:93-107
Adams, Mark K; Lee, Seung-Ah; Belyaeva, Olga V et al. (2017) Characterization of human short chain dehydrogenase/reductase SDR16C family members related to retinol dehydrogenase 10. Chem Biol Interact 276:88-94
Mochona, Bereket; Jackson, Timothy; McCauley, DeCoria et al. (2016) Synthesis and Cytotoxic Evaluation of Pyrrole Hetarylazoles Containing Benzimidazole/Pyrazolone/1,3,4-Oxadiazole Motifs. J Heterocycl Chem 53:1871-1877
Engel, Krysta L; French, Sarah L; Viktorovskaya, Olga V et al. (2015) Spt6 Is Essential for rRNA Synthesis by RNA Polymerase I. Mol Cell Biol 35:2321-31
Ayuk-Takem, Lambert; Amissah, Felix; Aguilar, Byron J et al. (2014) Inhibition of polyisoprenylated methylated protein methyl esterase by synthetic musks induces cell degeneration. Environ Toxicol 29:466-77
Chougule, Mahavir B; Patel, Apurva R; Patlolla, Ram et al. (2014) Epithelial transport of noscapine across cell monolayer and influence of absorption enhancers on in vitro permeation and bioavailability: implications for intestinal absorption. J Drug Target 22:498-508
Culpepper, Bonnie K; Webb, William M; Bonvallet, Paul P et al. (2014) Tunable delivery of bioactive peptides from hydroxyapatite biomaterials and allograft bone using variable-length polyglutamate domains. J Biomed Mater Res A 102:1008-16
Errahali, Younes J; Thomas, Leeshawn D; Keller 3rd, Thomas C S et al. (2013) Inhibition by new glucocorticoid antedrugs [16?, 17?-d] isoxazoline and [16?, 17?-d]-3'-hydroxy-iminoformyl isoxazoline derivatives of chemotaxis and CCL26, CCL11, IL-8, and RANTES secretion. J Interferon Cytokine Res 33:493-507
Stephenson, Adrienne P; Schneider, Jeffrey A; Nelson, Bryant C et al. (2013) Manganese-induced oxidative DNA damage in neuronal SH-SY5Y cells: attenuation of thymine base lesions by glutathione and N-acetylcysteine. Toxicol Lett 218:299-307
Godugu, Chandraiah; Patel, Apurva R; Doddapaneni, Ravi et al. (2013) Inhalation delivery of Telmisartan enhances intratumoral distribution of nanoparticles in lung cancer models. J Control Release 172:86-95

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