Open Access. Powered by Scholars. Published by Universities.®

Medicinal-Pharmaceutical Chemistry Commons

Open Access. Powered by Scholars. Published by Universities.®

690 Full-Text Articles 1,841 Authors 91,278 Downloads 92 Institutions

All Articles in Medicinal-Pharmaceutical Chemistry

Faceted Search

690 full-text articles. Page 9 of 30.

Naloxone Therapy In Opioid Overdose Patients: Intranasal Or Intravenous?, Leiah Carney 2017 Parkland College

Naloxone Therapy In Opioid Overdose Patients: Intranasal Or Intravenous?, Leiah Carney

Natural Sciences Poster Sessions

This slide presentation for the Natural Science Poster Session at Parkland College describes the chemical makeup and effect of Naloxone, an opioid antagonist used in the treatment opioid overdose and summarizes a study comparing intravenous and intranasal delivery methods. Concludes that although there are conflicting studies, evidence supports intranasal delivery.


Clozaril, Gillian Jones 2017 Parkland College

Clozaril, Gillian Jones

Natural Sciences Poster Sessions

This is a poster presented at the Natural Sciences Poster Session at Parkland College, which provides the chemical makeup, dosage, and the body's response to Clozaril (Clozapine, Fazaclo, Versacloz) an atypical antipsychotic used to manage schizophrenia and schizoaffective disorder as well as bipolar disorder, dementia-related behavior disorders, and tremors.


Aricept, Colleen M. Westburg 2017 Parkland College

Aricept, Colleen M. Westburg

Natural Sciences Poster Sessions

This poster, presented at the Natural Sciences Poster Session at Parkland College, provides the chemical makeup, dosage, and effects of Donepizil Hydrocholide, trade name Aricept, used to treat the symtoms of mild, moderate, or severe dementia of Alzheimer’s type. Unlabeled uses include treatment of symptoms of vascular dementia, poststroke aphasia, and memory improvement in multiple sclerosis patients.


Synthesis Of Multifunctional Polyacrylates And A Binding Group To Hemoglobin For The Treatment Of Traumatic Brain Injuries, Marina Michaud 2017 Georgia Southern University

Synthesis Of Multifunctional Polyacrylates And A Binding Group To Hemoglobin For The Treatment Of Traumatic Brain Injuries, Marina Michaud

University Honors Program Theses

Hemoglobin based oxygen carriers (HBOCs) hold promise as an effective emergency treatment of severe traumatic brain injuries (TBI). In the latest generation of HBOCs, polynitroxyl-pegylated hemoglobin (PNPH), cell-free hemoglobin is modified with TEMPO and PEG which reduce the toxicities associated with earlier generations of HBOCs. In our efforts to optimize the economic and therapeutic impacts of PNPH’s we have synthesized polydimethylaminoethyl methacrylate (poly-DMAEMA) under controlled living conditions via reverse addition-fragmentation chain transfer (RAFT) polymerization. The poly-DMAEMA was then successfully functionalized via quaternization of its NMe2 groups using chloroacetate derivatives of the TEMPO and PEG. This process was quantitative ...


Development Of Diverse Size And Shape Rna Nanoparticles And Investigation Of Their Physicochemical Properties For Optimized Drug Delivery, Daniel L. Jasinski 2017 University of Kentucky

Development Of Diverse Size And Shape Rna Nanoparticles And Investigation Of Their Physicochemical Properties For Optimized Drug Delivery, Daniel L. Jasinski

Theses and Dissertations--Pharmacy

RNA nanotechnology is an emerging field that holds great promise for advancing drug delivery and materials science. Recently, RNA nanoparticles have seen increased use as an in vivo delivery system. RNA was once thought to have little potential for in vivo use due to biological and thermodynamic stability issues. However, these issues have been solved by: (1) Finding of a thermodynamically stable three-way junction (3WJ) motif; (2) Chemical modifications to RNA confer enzymatic stability in vivo; and (3) the finding that RNA nanoparticles exhibit low immunogenicity in vivo.

In vivo biodistribution and pharmacokinetics are affected by the physicochemical properties, such ...


Zoloft/Sertraline Hcl, Loretta Banks 2017 Parkland College

Zoloft/Sertraline Hcl, Loretta Banks

Natural Sciences Poster Sessions

This poster, presented at the Natural Sciences Poster Session at Parkland College, provides the chemical makeup, dosage, and effects of Sertraline Hydrochloride, trade name Zoloft, used to treat the symptoms of depression, obsessive compulsive disorder, panic disorder, social anxiety disorder, premenstual dysphoric disorder, generalized anxiety, and post-traumatic stress disorder.


Citalopram Hydrobromide, Maria Parks 2017 Parkland College

Citalopram Hydrobromide, Maria Parks

Natural Sciences Poster Sessions

This poster, presented at the Natural Sciences Poster Session at Parkland College, provides the chemical makeup, dosage, and effects of Citalopram Hydrobromide, trade name Celexa, used to treat depression.


Sertraline Hydrochloride, Michelle L. Fehr 2017 Parkland College

Sertraline Hydrochloride, Michelle L. Fehr

Natural Sciences Poster Sessions

This poster, presented at the Natural Sciences Poster Session at Parkland College, provides the chemical makeup, dosage, and effects of Sertraline Hydrochloride, trade name Zoloft, used to treat the symptoms of depression, obsessive compulsive disorder, panic disorder, social anxiety disorder, premenstual dysphoric disorder, generalized anxiety, and post-traumatic stress disorder.


Nortriptyline Hyrdochloride, Israel R. Gomez Raffoul 2017 Parkland College

Nortriptyline Hyrdochloride, Israel R. Gomez Raffoul

Natural Sciences Poster Sessions

This poster, presented at the Natural Sciences Poster Session at Parkland College, provides the chemical makeup, dosage, and effects of Nortriptyline Hydrochloride, trade names Acetexa, Allegron, Aventyl, Noritren, Nortrilen, Sensaval, and Vividyl, used to treat endogenous drpression. Unlabeled uses include treatment of nocturnal enuresis in children, ADJD, and diabetic neuropathy.


Synthesis And Biological Activity Of Novel Tu100 Derivatives, Oladotun J. Alao 2017 Georgia Southern University

Synthesis And Biological Activity Of Novel Tu100 Derivatives, Oladotun J. Alao

Electronic Theses and Dissertations

In an attempt to create more effective chemotherapeutic compounds, the naphthoquinone adduct, 12,13-dihydro-N-methyl-6,11,13-trioxo-5H-benzo[4,5]cyclohepta [1,2 b]naphthalen-5,12-imine (hereafter called TU100) was synthesized. Inspired by its unique and novel mechanism of action, a series of structural derivatives were synthesized to explore structure-activity relationships. The analogues exhibited different cytotoxicity profiles, revealing the indicated regions are involved in cell death induction. Furthermore, the analogues had dramatically different effects on cellular ATP production, suggesting different molecular targets. Synthesis, biological activity, and SAR study of these analogues will be revealed.


A Potential Improved Anti-Hiv Drug: Using A Bivalent Design To Increase Specificity And Potency, Theo Koelsch 2017 University of Colorado Boulder

A Potential Improved Anti-Hiv Drug: Using A Bivalent Design To Increase Specificity And Potency, Theo Koelsch

Undergraduate Honors Theses

In this thesis, the synthesis of a potentially improved HIV entry inhibitor is presented. HIV has infected millions of people, and yet there is no fully effective treatment for the infection and the subsequent, high mortality disease AIDS. This is due in large part to the virus’s rapid development of resistance to any drug used to treat the infection. The best way to combat this is to use multiple drugs with different inhibition targets and so prevent the virus from developing resistance. In order to contribute to the effective treatment of HIV infection, it is therefore important to develop ...


Design, Synthesis, And Biological Activity Of 1,2,3-Triazolobenzodiazepine Bet Bromodomain Inhibitors [Accepted Manuscript], Phillip P. Sharp, Jean-Marc Garnier, Tamas Hatfaludi, Zhen Xu, David Segal, Kate E. Jarman, Hélène Jousset, Alexandra Garnham, John T. Feutrill, Anthony Cuzzupe, Peter Hall, Scott Taylor, Carl Walkley, Dean Tyler, Mark A. Dawson, Peter Czabotar, Andrew F. Wilks, Stefan Glaser, David C. S. Huang, Christopher J. Burns 2017 Australian Catholic University

Design, Synthesis, And Biological Activity Of 1,2,3-Triazolobenzodiazepine Bet Bromodomain Inhibitors [Accepted Manuscript], Phillip P. Sharp, Jean-Marc Garnier, Tamas Hatfaludi, Zhen Xu, David Segal, Kate E. Jarman, Hélène Jousset, Alexandra Garnham, John T. Feutrill, Anthony Cuzzupe, Peter Hall, Scott Taylor, Carl Walkley, Dean Tyler, Mark A. Dawson, Peter Czabotar, Andrew F. Wilks, Stefan Glaser, David C. S. Huang, Christopher J. Burns

Faculty of Health Sciences Publications

A number of diazepines are known to inhibit bromo- and extra-terminal domain (BET) proteins. Their BET inhibitory activity derives from the fusion of an acetyl-lysine mimetic heterocycle onto the diazepine framework. Herein we describe a straightforward, modular synthesis of novel 1,2,3-triazolobenzodiazepines and show that the 1,2,3-triazole acts as an effective acetyl-lysine mimetic heterocycle. Structure-based optimization of this series of compounds led to the development of potent BET bromodomain inhibitors with excellent activity against leukemic cells, concomitant with a reduction in c-MYC expression. These novel benzodiazepines therefore represent a promising class of therapeutic BET inhibitors.


Peptidylarginine Deiminase 1-Catalyzed Histone Citrullination Is Essential For Early Embryo Development, Xiaoqian Zhang, Xiaoqiu Liu, Mei Zhang, Tingting Li, Aaron Muth, Paul R. Thompson, Scott A. Coonrod, Xuesen Zhang 2016 Nanjing Medical University

Peptidylarginine Deiminase 1-Catalyzed Histone Citrullination Is Essential For Early Embryo Development, Xiaoqian Zhang, Xiaoqiu Liu, Mei Zhang, Tingting Li, Aaron Muth, Paul R. Thompson, Scott A. Coonrod, Xuesen Zhang

Thompson Lab Publications

Peptidylarginine deiminase (PADI) enzymes are increasingly being associated with the regulation of chromatin structure and gene activity via histone citrullination. As one of the PADI family members, PADI1 has been mainly reported to be expressed in the epidermis and uterus, where the protein in keratinocytes is thought to promote differentiation by citrullinating filament proteins. However, the roles of PADI1 in preimplantation development have not been addressed. Using a PADI1-specific inhibitor and Padi1-morpholino knockdown, we found that citrullination of histone tails at H4R3 and H3R2/8/17 were markedly reduced in the 2- and 4-cell embryos. Consistent with this observation, early ...


Design, Synthesis, And Evaluation Of Dasatinib-Amino Acid And Dasatinib-Fatty Acid Conjugates As Protein Tyrosine Kinase Inhibitors, Rakesh Tiwari, Alex Brown, Neda Sadeghiani, Amir Nasrolahi Shirazi, Jared Bolton, Amanda Tse, Gennady M. Verkhivker, Keykavous Parang, Gongqin Sun 2016 Chapman University

Design, Synthesis, And Evaluation Of Dasatinib-Amino Acid And Dasatinib-Fatty Acid Conjugates As Protein Tyrosine Kinase Inhibitors, Rakesh Tiwari, Alex Brown, Neda Sadeghiani, Amir Nasrolahi Shirazi, Jared Bolton, Amanda Tse, Gennady M. Verkhivker, Keykavous Parang, Gongqin Sun

Pharmacy Faculty Articles and Research

Derivatives of dasatinib were synthesized via esterification with 25 carboxylic acids including amino acids and fatty acids by extending the inhibitor to interact with more diverse sites and to improve specificity. Dasatinib-L-arginine derivative (Das-R, 7) was the most potent of the inhibitors tested with IC50 values of 4.4 nM, <0.25 nM, and <0.45 nM against Csk, Src, and Abl kinases, respectively. The highest selectivity ratio obtained in our study, 91.4 Csk/Src belonged to compound 18 (Das-C10) with an IC50 of 3.2 μM for Csk compared to 35 nM for Src. Furthermore, many compounds displayed increased selectivity toward Src, as compared with Abl. Compounds 15 (Das-E) and 13 (Das-C) demonstrated the largest gains (10.2 and 10.3 Abl/Src IC50 ratios). Das-R (IC50 = 2.06 μM) was significantly more potent than Das (IC50 = 26.3 μM) against Panc-1 cells while they both showed an IC50 < 51.2 pM against BV-173 and K562 cells. Molecular modeling and binding free energy simulations revealed a good agreement with the experimental results and rationalized differences in selectivity of the studied compounds. Integration of experimental and computational approaches in the design and biochemical screening of dasatinib derivatives facilitated rational engineering and diversification of dasatinib scaffold, providing useful insights into mechanisms of kinase selectivity.


Synthesis Of Orthogonally Protected Thioamide Dipeptides For Use In Solid-Phase Peptide Synthesis, Fintan Kelleher, Kim Manzor 2016 Institute of Technology, Tallaght

Synthesis Of Orthogonally Protected Thioamide Dipeptides For Use In Solid-Phase Peptide Synthesis, Fintan Kelleher, Kim Manzor

Articles

Orthogonally protected thioamide-containing dipeptides were efficiently and cleanly prepared from the precursor dipeptides using Curphey’s method (P4S10, hexamethyldisiloxane (HMDO), reflux, DCM) in 67-96% isolated yield. This was in contrast to the use of Lawesson’s or Berzelius’ reagents where significant issues with reaction non-completion, decomposition and purification were observed. Subsequent clean removal of the dipeptides’ t-butyl ester protecting groups gave thioamide dipeptide acids which were suitable for use in solid-phase peptide synthesis (SPPS).


Discovery And Characterization Of A Potent And Selective Inhibitory Of Aedes Aegypti Inward Rectifier Potassium Channels, Matthew F. Rouhier, Et Al. 2016 Kenyon College

Discovery And Characterization Of A Potent And Selective Inhibitory Of Aedes Aegypti Inward Rectifier Potassium Channels, Matthew F. Rouhier, Et Al.

Matthew F Rouhier

Vector-borne diseases such as dengue fever and malaria, which are transmitted by infected female mosquitoes, affect nearly half of the world's population. The emergence of insecticide-resistant mosquito populations is reducing the effectiveness of conventional insecticides and threatening current vector control strategies, which has created an urgent need to identify new molecular targets against which novel classes of insecticides can be developed. We previously demonstrated that small molecule inhibitors of mammalian Kir channels represent promising chemicals for new mosquitocide development. In this study, high-throughput screening of approximately 30,000 chemically diverse small-molecules was employed to discover potent and selective inhibitors ...


Polymeric Prodrug Combination To Exploit The Therapeutic Potential Of Antimicrobial Peptides Against Cancer Cells., Graeme J. Kelly, A Foltyn-Arfa Kia, F Hassan, S O'Grady, Maria P. Morgan, B S. Creaven, S McClean, Judith H. Harmey, Marc Devocelle 2016 Royal College of Surgeons in Ireland

Polymeric Prodrug Combination To Exploit The Therapeutic Potential Of Antimicrobial Peptides Against Cancer Cells., Graeme J. Kelly, A Foltyn-Arfa Kia, F Hassan, S O'Grady, Maria P. Morgan, B S. Creaven, S Mcclean, Judith H. Harmey, Marc Devocelle

Chemistry Articles

Antimicrobial Peptides (AMPs) have unique anticancer properties, but their clinical application is currently limited by an inadequate margin of safety. A prodrug strategy associated with a combination therapy approach could address this limitation by increasing their therapeutic index and their efficacy. Accordingly, the first targeted anticancer polymeric prodrug candidates of AMPs, intended for combination therapy with another polymeric prodrug of an approved antineoplastic agent (doxorubicin), were synthesized as either a PEG-based dual-release prodrug or two individual pegylated prodrugs. The latter are based on a cathepsin B-labile peptide linker and an acid-sensitive acyl hydrazone bond for the AMP and doxorubicin prodrugs ...


Synthesis, Self-Assembly, And Immunological Activity Of Α-Galactose-Functionalized Dendron–Lipid Amphiphiles, John Trant, Namrata Jain, D. M. Mazzuca, J Trevor McIntosh, Bo Fan, S M Mansour Haeryfar, Sebastien Lecommandoux, Elizabeth Gillies 2016 Western University

Synthesis, Self-Assembly, And Immunological Activity Of Α-Galactose-Functionalized Dendron–Lipid Amphiphiles, John Trant, Namrata Jain, D. M. Mazzuca, J Trevor Mcintosh, Bo Fan, S M Mansour Haeryfar, Sebastien Lecommandoux, Elizabeth Gillies

Chemistry Publications

Nanoassemblies presenting multivalent displays of biologically active carbohydrates are of significant interest for a wide array of biomedical applications ranging from drug delivery to immunotherapy. In this study, glycodendronlipid hybrids were developed as a new and tunable class of dendritic amphiphiles. A modular synthesis was used to prepare dendronlipid hybrids comprising distearylglycerol and 0 through 4th generation polyester dendrons with peripheral protected amines. Following deprotection of the amines, an isothiocyanate derivative of C-linked α-galactose (α-Gal) was conjugated to the dendron peripheries, affording amphiphiles with 1 to 16 α-Gal moieties. Self-assembly in water through a ...


Strained Alkyne Substituted Near Infrared Bf2 Azadipyrromethene Fluorochrome, Dan Wu, Shane Cheung, Corry James O'Sullivan, Yinghua Gao, Zhi-Long Chen, Donal F. O'Shea 2016 Royal College of Surgeons in Ireland

Strained Alkyne Substituted Near Infrared Bf2 Azadipyrromethene Fluorochrome, Dan Wu, Shane Cheung, Corry James O'Sullivan, Yinghua Gao, Zhi-Long Chen, Donal F. O'Shea

Chemistry Articles

The contribution of imaging with near infrared (NIR) fluorophores to the elucidation of complex biological processes continues to rapidly expand. New tools for mild selective bioconjugation are strongly desirable for the construction of NIR labelled biomolecules. This work presents the synthesis and evaluation of a strained alkyne substituted NIR BF2-azadipyrromethene (NIR-AZA) which can conjugate in water with azido-homoalanine and cRGD peptide within 30 min at rt. Imaging analysis of the NIR-AZA–cRGD conjugate in vitro and in vivo showed efficient cellular uptake and good in vivo tumor targeting properties, illustrating the potential for translation to clinical imaging.


Synthesis Of Polymeric Bismuth Chlorido Hydroxamato Complexes; X-Ray Crystal Structure And Antibacterial Activity Of A Novel Bi(Lll) Salicylhydroxamato Complex, Donal M. Keoghan, Lauren E. Fagan, Thayse Marques Passos, Helge Müller-Bunz, Bríd Quilty, Darren M. Griffith 2016 Royal College of Surgeons in Ireland

Synthesis Of Polymeric Bismuth Chlorido Hydroxamato Complexes; X-Ray Crystal Structure And Antibacterial Activity Of A Novel Bi(Lll) Salicylhydroxamato Complex, Donal M. Keoghan, Lauren E. Fagan, Thayse Marques Passos, Helge Müller-Bunz, Bríd Quilty, Darren M. Griffith

Chemistry Articles

Reaction of salicylhydroxamic acid (Sha) and 2-aminophenyl hydroxamic acid (2-NH2-pha) with BiCl3 affords the corresponding novel polymeric bismuth chlorido hydroxamato complexes; [BiCl2(-Sha-1H)]∞ and [BiCl3(--Pha-1H)]∞ respectively. The X-ray crystal structure of the THF-solvated polymeric bismuth chlorido salicylhydroxamato complex, [BiCl2(-Sha-1H)(THF)]∞ was solved, confirming the polymeric structure of this class of compounds and the (O,μ-O’)-bidentate bridging coordination mode of the hydroxamato ligand. The antibacterial activity of the THF-free polymeric bismuth chlorido salicylhydroxamato complex, [BiCl2(-Sha-1H)]∞, was investigated against a broad panel of bacteria, further highlighting the antibacterial properties of Bi-based compounds against Gram-positive and Gram-negative pathogenic and ...


Digital Commons powered by bepress