Medicinal and Pharmaceutical Chemistry Commons^™

Opioid Codrugs For Pain Management, Ujjwal Chakraborty

Theses and Dissertations--Chemistry

Pain is an unpleasant sensory and emotional experience associated with actual or potential tissus damage or described in terms of such damage. Opioids are effective in treating moderate to severe pain, but opioid alone therapy is associated with several adverse effects, development of tolerance and addiction potential. One way to solve these problems is to administer opioids with adjuvant drugs. In this project several opioid molecules were combined with other adjuvant drugs in a single chemical entity to form a codrug.

A series of codrugs were prepared by conjugation of an opioid with S-(-)-nornicotine, ketamine, norketamine and gabapentin. Several …

Synthesis, Characterization And Biological Activity Of Copper (Ii) And Zinc (Ii) Complexes Of Thiosemicarbazones And Their N(4)-Substituted Derivatives Derived From 2,4-Dihydroxybenzaldehyde., Tan Kong Wai

Student Works (2010-2019)

Four thiosemicarbazones ligands (1-4) have been prepared with good yield by refluxing 2,4-dihydroxybenzaldehyde with thiosemicarbazide or N(4)-substituted thiosemicarbazide in ethanol or methanol. From these four ligands, 16 new ternary metal complexes (5-20) with the general formulation of M(B)L have been prepared from the reactions of metal acetates with 2,4-dihydroxybenzaldehyde N(4)-substituted thiosemicarbazone in the presence of N,N-heterocyclic base (M2+ = Zn2+ or Cu2+; B = 2,2'-bipyridine, (bpy); 1,10-phenanthroline, (phen); L2- = doubly deprotonated thiosemicarbazones = 2,4-dihydroxybenzaldehyde thiosemicarbazonato, (HT); 2,4-dihydroxybenzaldehyde 4-methylthiosemicarbazonato, (HM); 2,4-dihydroxybenzaldehyde 4-ethylthiosemicarbazonato, (HE) and 2,4-dihydroxybenzaldehyde 4-phenylthiosemicarbazonato, (HP)) These compounds have been characterized by elemental analyses, IR, UV-Vis, NMR and magnetic …

Synthesis, Characterization And Biological Activities Of Some Indole Derivatives And Their Metal Complexes., Mohamed Mustafa Mohamed Ibrahim

Student Works (2010-2019)

Tryptamine (1H-indole-3-ethyleneamine) Schiff bases were prepared by the condensation reaction of ethanolic solution of tryptamine with: salicylaldehyde (TS), 5 chlorosalicylaldehyde (TCS), 5-nitrosalicylaldehyde (TNS), 3,5-di-tert-butyl-2-hydroxy benzaldehyde (TTET) and the ketones: 2-hydroxyacetophenone (THAP), 5-methyl-2- hydroxyacetophenone (TMeHAP), 5-methoxy-2 hydroxyacetophenone (TOMeHAP), 5- chloro-2-hydroxyacetophenone (TClHAP) and 5-bromo-2 hydroxyacetophenone (TBrHAP). The ligands were coordinated to Zn(II), Cu(II) and Ni(II) by the reaction of metal acetates with the corresponding ligand in a 1 : 2 metal to ligand ratio. The solid products formed were collected, washed with ethanol and recrystallized from a suitable solvent. All the ligands and complexes prepared have been characterized by spectroscopic methods using …

Analysis Of Residual Solvents In Pharmaceuticals By Comprehensive Two-Dimensional Gas Chromatography, Cristina Marie Crimi

Seton Hall University Dissertations and Theses (ETDs)

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Protein Adducts Of Iso[4]Levuglandin E2, A Product Of The Isoprostane Pathway, In Oxidized Low Density Lipoprotein, Robert G. Salomon, Wei Sha, Cynthia Brame, Kamaljit Kaur, Ganesamoorthy Subbanagounder, June O'Neil, Henry F. Hoff, L. Jackson Roberts Ii

Pharmacy Faculty Articles and Research

Levuglandin (LG) E₂, a cytotoxic seco prostanoic acid co-generated with prostaglandins by nonenzymatic rearrangements of the cyclooxygenase-derived endoperoxide, prostaglandin H₂, avidly binds to proteins. That LGE₂-protein adducts can also be generated nonenzymatically is demonstrated by their production during free radical-induced oxidation of low density lipoprotein (LDL). Like oxidized LDL, LGE₂-LDL, but not native LDL, undergoes receptor-mediated uptake and impaired processing by macrophage cells. Since radical-induced lipid oxidation produces isomers of prostaglandins, isoprostanes (isoPs), via endoperoxide intermediates, we postulated previously that a similar family of LG isomers, isoLGs, is cogenerated with isoPs. Now …

The Synthesis Of Various Substituted 3-Amino-7-Hydroxy-2,2-Dimethyltetralins And Their Opioid-Related Activities, David Alan Lippman

University of the Pacific Theses and Dissertations

A series of aminotetralones and aminotetralins were synthesized from the common intermediate F, 3-amino-2,2-dimethyl-7-methoxy- 1-tetralone. The final compounds derived from F were simple substituted and/or reduced analogues. The products would allow a progressive structure activity relationship to be drawn based on pharmacological testing.

The common intermediate F was synthesized utilizing a six step procedure starting with p-methoxyphenylacetic acid. The overall yield from the precursor to the F:HC1 was 25%. Compound F was either O-demethylated to form 3-amino-2,2-dimethyl-7-hydroxy-l-tetralone (I) or was dimethylated on the amine and subsequently O-demethylated to yield the 3-dimethylamino-7-hydroxy-2,2-dimethyl-l-tetralone (J). The last major modification was the reduction of …

The Pharmacology Of Rodenticides, S. A. Peoples

Vertebrate Pest Conference Proceedings: 4th (1970)

The compounds used as rodenticides are tremendously varied in their chemical structure and mechanism of action. With a few exceptions, these agents are generally poisonous to all animals, including man, and a great deal of study has been directed to their toxicity in animals other than rodents. However, the development of new compounds as Norbormide and certain antifertility drugs which are highly selective in their action may justify the hope that the ideal rodenticide free of secondary toxic hazards will soon be available. Until this happy announcement is made, a review of the pharmacology of the older compounds is in …