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Articles 1 - 7 of 7
Full-Text Articles in Chemicals and Drugs
Design And Synthesis Of Novel Sultams As Non-Nucleoside Inhibitors Of Hiv Reverse Transcriptase, Brian Chadwick Lecroix
Design And Synthesis Of Novel Sultams As Non-Nucleoside Inhibitors Of Hiv Reverse Transcriptase, Brian Chadwick Lecroix
Doctoral Dissertations
The compound 2-methyl-3-phenyl-2,3-dihydro-1,2-benzisothiazole 1,1-dioxide (NSC 108406) was identified as an HIV-1 reverse transcriptase inhibitor by the National Cancer Institute. Using this lead, the Baker group has developed a series of analogues with various groups at the 3-position that show a spectrum of biological activities. In the end, the substituents used could not compare to the biological activity of the inhibitor efavirenz (Sustiva® [trademark]), and so it was decided to synthesize sultams with alkylethynyl substituents at the 3-position of the sultams in an attempt to mimic the activity of efavirenz.
Previous research analyzed the proposed novel sultams in the modeling …
Formulation Development Of A Polymer-Drug Matrix With A Controlled Release Profile For The Treatment Of Glaucoma, Eric W. Tsoi
Formulation Development Of A Polymer-Drug Matrix With A Controlled Release Profile For The Treatment Of Glaucoma, Eric W. Tsoi
Master's Theses
Glaucoma is the leading cause of blindness in the United States accounting for 9-12% of all cases of blindness. Currently, the front line treatment for glaucoma are prostaglandins that may have to be taken up to several times a day. Even with proper treatment, roughly 11% of the patients using the treatment are non-compliant and lose their vision. In this project, ForSight Laboratories has developed a pharmaceutical drug delivering implant with the capability of sustaining long-term release of a prostaglandin as a new way to treat the condition. This project reports the product development of a polymer drug matrix with …
Developing A Presumptive Test For Select Synthetic Cannabinoids, Carrie Snyder
Developing A Presumptive Test For Select Synthetic Cannabinoids, Carrie Snyder
Graduate Theses and Dissertations
Synthetic cannabinoids (SC's) began to gain popularity around the world in 2009. Since then, many of the compounds have been outlawed and methods developed to detect them and their metabolites using mass spectrometry. Our work investigated the possibility of developing a colorimetric presumptive test. The SC JWH-019 was synthesized and its ketone targeted as a possible reaction site. Many SC's contain ketones and thus a reaction at this site would be applicable to many of the compounds. Since JWH-019 is costly and time consuming to synthesize, much of the experimental work was done using benzophenone (BP). BP contains a diaryl …
Developing Thyronamine Analog Pharmaceuticals Targeting Taar1 To Treat Methamphetamine Addiction, Troy Andrew Wahl
Developing Thyronamine Analog Pharmaceuticals Targeting Taar1 To Treat Methamphetamine Addiction, Troy Andrew Wahl
Dissertations and Theses
As a part of the overall program in the Grandy laboratory at Oregon Health & Science University (OHSU), studying the underlying chemical biology of methamphetamine (Meth) addiction, this dissertation reports on the development of six new thyronamine analogs which were synthesized and assayed against trace amine associated receptor 1 (TAAR1), giving preliminary results consistent with the analogs being inverse agonists. Due to highly variable TAAR1 expression levels in the assays, based on inter-assay response to control Meth stimulation as well as other possible factors, kinetic models were developed to qualitatively explain the assay results. The models set approximate limits on …
Comparison Of Methodologies For Synthesis Of 3-(Cyclopropylethynyl)Benzisothiazole 1,1-Dioxide, Rachel Lee Naramore
Comparison Of Methodologies For Synthesis Of 3-(Cyclopropylethynyl)Benzisothiazole 1,1-Dioxide, Rachel Lee Naramore
Chancellor’s Honors Program Projects
No abstract provided.
Development Of A Rapid Spme/Gc-Ms Method For The Detection And Quantification Of Synthetic Cathinones In Oral Fluid, David Correll
Development Of A Rapid Spme/Gc-Ms Method For The Detection And Quantification Of Synthetic Cathinones In Oral Fluid, David Correll
Senior Theses and Projects
The recent emergence and widespread abuse of new classes of compounds on the designer drug market as “legal” alternatives to scheduled drugs such as Ecstasy has prompted interest in the development of analytical methods for their detection and characterization. Synthetic cathinones, which are structurally similar to amphetamines, are commonly advertised as a “legal highs” or “herbal highs,” and are marketed under names such as “bath salts” and “plant food.” To avoid drug abuse legislation, a “not for human consumption” warning is typically printed on the label. Their ready availability on the Internet and in “head” shops, convenience stores, and even …
Turning Stealth Liposomes Into Cationic Liposomes For Anticancer Drug Delivery, Vijay Gyanani
Turning Stealth Liposomes Into Cationic Liposomes For Anticancer Drug Delivery, Vijay Gyanani
University of the Pacific Theses and Dissertations
Targeting the anticancer agents selectively to cancer cells is desirable to improve the efficacy and to reduce the side effects of anticancer therapy. Previously reported passive tumor targeting by PEGylated liposomes (stealth liposomes) have resulted in their higher tumor accumulation. However their interaction with cancer cells has been minimal due to the steric hindrance of the PEG coating. This dissertation reports two approaches to enhance the interaction of stealth liposomes with cancer cells. First, we designed a lipid-hydrazone-PEG conjugate that removes the PEG coating at acidic pH as in the tumor interstitium. However, such a conjugate was highly unstable on …