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Showing 1 to 20 of 284 for “"Structure-Activity Relationship"”.

  1. BIOISOSTERES OF AMPA: CONFORMATIONAL ANALYSIS AND STRUCTURE ACTIVITY RELATIONSHIP

    RAJALE, TRIDEEP

    Glutamate is the major excitatory neurotransmitter in the mammalian central nervous system (CNS). Concentrations of L-glutamate in the CNS are regulated by a family of excitatory amino acid transporters (EAATs) that rapidly sequester and concentrate glutamate in glia and neurons, and thereby …

    montana-tech Repository record

  2. BIOISOSTERES OF AMPA: CONFORMATIONAL ANALYSIS AND STRUCTURE ACTIVITY RELATIONSHIP

    RAJALE, TRIDEEP

    Glutamate is the major excitatory neurotransmitter in the mammalian central nervous system (CNS). Concentrations of L-glutamate in the CNS are regulated by a family of excitatory amino acid transporters (EAATs) that rapidly sequester and concentrate glutamate in glia and neurons, and thereby …

    montana Repository record

  3. Synthesis, structure-activity relationship and solubility profiling of antimycobacterial aminoquinazolinones

    Akester, Jessica NicoleDepartment of Chemistry2017

    … compounds with potent antimycobacterial activity were previously identified. Poor solubility was recognized as a major issue requiring improvement. To this end, structure-activity relationship (SAR) studies were performed around the 2-aminoquinazolinone core in order to optimize these …

    cape-town Repository record

  4. Structure-Activity Relationship Studies of Mitochondrial Uncouplers and PilB Inhibitors

    Quinlan, Joseph Edward IIIVirginia Tech2025

    … high uncoupling nature of these compounds. Our structure-activity relationship (SAR) studies demonstrated that the hydroxylamine BAM15 analogs are more potent than hydrazine ones, with particular note of hydroxylamine ester derivatives being the most efficacious of all structures assayed. For …

    vt Repository record

  5. Structure Activity Relationship Studies on Isoform Selective Sphingosine Kinase Inhibitors

    Congdon, Molly D.Virginia Tech2016

    … described in detail. Key discoveries from this structure-activity relationship study include SLC5111312 (hSphK2 Ki = 0.90 μM, dual hSphK inhibitor), SLC5091592 (hSphK2 Ki = 1.02 μM, > 20-fold hSphK2 selective) and SLC5121591 (hSphK2 Ki = 0.61 μM, >16-fold hSphK2 selective). Molecular modeling …

    vt Repository record

  6. Establishing a structure-activity-relationship for small molecule non-sugar glycomimetics

    Dobiecki-Davies, J2021

    … assays did not show any reasonable biological activity. HGF/SF has been shown to activate downstream signalling of the oncogene product c-Met which is a biomarker for cancer(s) and can be associated with poorer outcomes for patients.

    salford Repository record

  7. A Structure-Activity Relationship Study of Dihydroajoenes as Anti-Cancer Agents

    Biwi, James TapiwaDepartment of Chemistry2014

    … known to possess in vitro and in vivo anticancer activity based on the presence of a vinyl disulfide as its pharmacophore. This thesis reports on the synthesis of dihydroajoenes, a novel set of ajoene analogues, containing a saturated double bond, in which the intention was to study the influence …

    cape-town Repository record

  8. Structure-Activity Relationship Studies of Sphingosine Kinase Inhibitors and Mitochondrial Uncouplers

    Childress, Elizabeth SaundersVirginia Tech2017

    … which differ with respect to their cellular activity and localization. As the key mediators in the synthesis of S1P, SphKs have attracted attention as viable targets for pharmaceutical inhibition. To validate their potential as therapeutic targets, we aimed to develop potent, selective, and …

    vt Repository record

  9. Further Exploring the Structure Activity Relationship (SAR) of MMV008138 and MMV1803522

    Li, HaiboVirginia Tech2023

    … falciparum. However, this lead showed no activity in mouse models. This lack of activity may be due to poor metabolic stability of the compound. However, a significant increase in in vitro potency could also improve in vivo activity. Towards that end, I focused on further variation of the …

    vt Repository record

  10. Synthesis and structure-activity relationship of a series of sigma receptor ligands

    Nahas, Roger I., 1978-University of Missouri--Columbia2007

    … drugs. In an attempt to elucidate effectual structure-activity relationships, a series of N-phenylpropyl- N'-benzylpiperazine and N-phenylpropyl-4-benzylpiperidine analogs systematically substituted on both phenyl rings was synthesized. These ligands were specifically designed to have certain …

    missouri Repository record

  11. Structure-activity relationship of octreotide analogues labeled with rhenium and technetium-99m

    Dannoon, Shorouk, 1982-University of Missouri--Columbia2009

    … was determined via three-dimensional molecular structure calculation, using two-dimensional NMR experiments as experimental constraints. From the obtained structures, it was concluded that the metal-cyclized Tyr³-octreotate's receptor binding site configuration was, to some extent, similar to …

    missouri Repository record

  12. The design of cyclodextrins for delivery of siRNA - a structure-activity relationship

    Kont, AyseUniversity College Cork2024

    … chemistry of the incorporated CD. The chemical structure significantly influenced the degree of gene knockdown. The primary amine showed superior efficiency in both monomeric amphiphilic cationic CDs and polymeric cationic CDs. Results indicate that further functionalisation of the CD is …

    cork Repository record

  13. Design, Synthesis, and Structure-Activity Relationship Investigation of Selective Sphingosine Kinase Inhibitors

    Li, HaoVirginia Tech2019

    … including inflammatory responses. Elevated SphK1 activity as well as upregulated S1P levels is linked to various diseases such as cancer, fibrosis and sickle cell disease. Therefore, there is a growing interest in studying SphK1 as a potential target for these diseases. Through high-throughput …

    vt Repository record

  14. Structure-activity relationship studies and biological evaluation of selective sphingosine kinase inhibitors

    Morris, Emily A.Virginia Tech2015

    … Herein, we document our efforts in profiling the structure-activity relationships (SAR) of SphK2 through an iterative process of synthesis and biological testing. First, an SAR structured around the head and linker region of our lead molecule, SLR080811, was performed. SLR080811 has a Ki of 1.3 µM …

    vt Repository record

  15. Structure-Activity Relationship and Mitochondrial Actions of Ionic Liquids as Potential Anticancer Agents

    Roy, Ritik2023

    … agents. For these reasons, a well-defined structure-activity relationship (SAR) describing IL anticancer activity is important, however the current SAR is limited due in part to the low structural diversity of reported ILs. One of the aims of this project was to expand the SAR of ILs by …

    uts Repository record

  16. Synthesis and Structure Activity Relationship Studies of a Natural Product-Derived Compound Library

    Swain III, Paul Whitney

    … of finding a new compound with antimicrobial activity.</p> <p>Herein is described a compound library derived from the natural product, nonactin. A preliminary library was previously synthesized by Phillips that yielded two lead compounds that were the starting points for this work. The lead …

    montana-tech Repository record

  17. Synthesis and Structure Activity Relationship Studies of a Natural Product-Derived Compound Library

    Swain III, Paul Whitney

    … of finding a new compound with antimicrobial activity.</p> <p>Herein is described a compound library derived from the natural product, nonactin. A preliminary library was previously synthesized by Phillips that yielded two lead compounds that were the starting points for this work. The lead …

    montana Repository record

  18. Structure-activity relationship studies of 2-phenylbenzimidazoles and related organometallic complexes as antiplasmodial agents

    Rylands, Laa-iqaDepartment of Chemistry2018

    … candidates, displaying potent antiplasmodial activity. Furthermore, benzimidazoles can be chemically transformed into metal-containing organometallic complexes that elevate generally flat benzimidazoles to the third dimension. To date, examples of metal-containing benzimidazoles are extremely …

    cape-town Repository record

  19. Structure-Activity Relationship and Mechanistic Studies on the Chemopreventive Activity of Dipyridamole and Its Analogues

    Grant, Ja’Wanda Shavon2016

    … showed potent chemopreventive activity against JB6 P<sup>+</sup>cells (tumor promotion sensitive). To probe the effects of <strong>DPM</strong> structural features on its antitumor promotion activity, the soft-agar colony forming efficiency assay was used to screen an in-house …

    tenn-hsc Repository record

  20. Isolation, Synthesis and Structure-Activity Relationship Study of Anticancer and Antimalarial Agents from Natural Products

    Dai, YuminVirginia Tech2013

    … fourteen novel compounds with antiproliferative activity against the A2780 human ovarian cancer line. One extract with antimalarial activity was studied, which led to the isolation of two new natural products with antiplasmodial activity against a drug-resistant Dd2 strain of Plasmodium …

    vt Repository record

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