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Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
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Showing 1 to 20 of 26 for “"SAR study"”.
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Synthesis and SAR study of Meperidine Analogues as Selective Serotonin Reuptake Inhibitors (SSRIs)
Meperidine has been shown to have potent binding affinity for serotonin transporters (SERT) (Ki = 41 nM) and be an inhibitor of serotonin reuptake. Based upon these pharmacological results meperidine has been identified as a lead compound for the development of a novel class of serotonin-selective …
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Design, Synthesis and Evaluation of Covalent Inhibitors for Tissue Transglutaminase and Factor XIIIa
… inhibitors, a structure-activity relationship (SAR) study was conducted. In this work, >20 novel irreversible inhibitors were prepared and kinetically evaluated. Our lead inhibitors allosterically inhibited GTP binding by locking the enzyme in its open conformation, as demonstrated both in vitro …
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Discovery of Novel Tubulin Inhibitors and Selective Survivin Inhibitors for Advanced Melanoma and Total Synthesis of Bioactive 20S-hydroxyvitamin D3
… Extensive structure-activity relationship (SAR) studies of lead molecules ABI-231 and UC-112 have been performed.</p> <p>Chapter 1 will introduce the current situation of advanced or metastatic melanoma, its clinical drug treatments, as well as problems in current drug treatments. …
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Identification and investigation of RNA-binding ligands
… to perform a structure-activity relationship (SAR) study on one of the lead molecules, NSC657704. Based on the results of the SAR, I designed a set of derivatives, synthesized them, and ascertained their inhibitory activity and RNA binding affinity.
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Semi-Synthesis of Melodinine, Taberyunine, and Melosuavine Bis-Indole Alkaloids Through Chemical and Biological Methods
… to conduct a structure activity relationship (SAR) study of the bis-indole framework against colon cancer and melanoma cell lines. Alkaloid aryl trifluoroborates were synthesized to increase nucleophilicity of arenes for unfavored alpha-arylations of tertiary amines on route to melosuavine …
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Design, synthesis and biological evaluation of antidiabetic agents
… inhibit the formation of the RBP4-TTR complex. A SAR study of compound 1 uncovered compound 4 which was more active than its parent compound in the SPR assay. A subsequent SAR study performed on the new lead compound 4 to identify the functional groups necessary for its biological activity. The …
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Design, Synthesis and Evaluation of Organic and Metal Based Antimicrobial Agents
… Firstly, a structure-activity relationship (SAR) study of a thiourea-based, bifuctional organocatalyst, which was found to exhibit bacteriostatic activity (MIC90 of 4.69- 6.25 g/mL against E. coli) comparable to that of vancomycin hydrochloride, was used to assess the structural components …
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Synthesis and structure-activity relationship of a series of sigma receptor ligands
… and electronic characteristics, in order to study the effect of those properties on the biological activity. Structure-activity relationships (SAR) were evaluated qualitatively to describe the effect of the systematic benzyl substitution in comparison to the phenylpropyl substitution. High …
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Building a rational model for the identification of allosteric sites
… through a structure activity relationship (SAR) which enabled the synthesis of three compounds that showed a higher stabilization than the initial hit (Tm > 1.2 °C). A second library was synthesized based on the same core, but with an amide functionality instead of an oxyamidine. From this …
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Novel Neuroblastoma Differentiating Agents
… by use of a Structure-Activity Relationship (SAR) study, the pharmacophore of the hit compound has begun to be elucidated. Understanding the chemical groups necessary for activity can give rise to more potent compounds as well as assist in future mode of action studies. Cell viability assays …
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Synthesis and Antifungal Evaluation of Barbiturate Saponins And Progress Towards Cysteinyl Metal Peptides
… novel antifungal agents. The need for extensive SAR studies and to better understand these compounds efforts were directed to synthesize novel saponin barbiturates.</p> <p>Glycosylation of barbiturates was achieved under basic conditions to synthesize mono and disaccharide barbiturates. …
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Novel Design Strategy for Potent and Selective CDPK1 Inhibitors for Cryptosporidiosis
… kinases. The structure-activity relationship (SAR) study of pyridopyrimidinone analogs also provided insights into CDPK1 inhibitor optimization. These efforts produced WIN1-158 as a 2nd - generation pyridopyrimidinone based CDPK1 inhibitor that provided greater selectivity (> 1,000-fold) …
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Synthesis and Structure-Activity Relationship Studies of 3-(N-Butylethanimidoyl)-4-hydroxy-2H-chromen-2-one (BHC) Analogues for Myosin II Inhibition
… myosin II. The structure-activity relationship (SAR) study of BHC analogues are performed in this study. To implement the SAR studies of BHC analogues, the synthetic route to complete the Schiff base was developed. The synthesis of 3-acetyl-4-hydroxycoumarin allows for a convenient source to …
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Design and Synthesis of Antimycobacterial Agents
… of its structure-activity relationship (SAR). The first generation of compounds successfully produced a compound which improved on previous activity, and established that the degree to which the ester linkage impacts activity is more substrate specific than previously recognised. Further …
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Investigation of bioactive scaffolds as antimicrobials
… acid as the core cyclic fragment. The extensive SAR study of polyamino-podocarpic acid derivatives identified the necessary scaffolds to elicit anti-MRSA, antifungal, and potentiating activity for this compound class. During an antimicrobial screening program of Copp-group compounds from previous …
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Synthesis and Structure Activity Relationship Studies of a Natural Product-Derived Compound Library
… iterations of a Structure Activity Relationship study in an effort to maximize antimicrobial activity. Antimicrobial activity of the compounds from the SAR study against <italic>Bacillus subtilis</italic> was increased nearly 200-fold from the initial leads and spectrum of activity was expanded …
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Synthesis and Structure Activity Relationship Studies of a Natural Product-Derived Compound Library
… iterations of a Structure Activity Relationship study in an effort to maximize antimicrobial activity. Antimicrobial activity of the compounds from the SAR study against <italic>Bacillus subtilis</italic> was increased nearly 200-fold from the initial leads and spectrum of activity was expanded …
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Design and synthesis of indole-based analogues of OXi8006 as inhibitors of tubulin polymerization and their incorporation as payloads in drug-linker constructs.
… site, a structure-activity relationship (SAR) study was conducted by replacing the carbonyl moiety with various one-atom and two-atom bridging functionalities. Among the analogues synthesized, compounds bearing a sulfide bridge (KGP555) and a methylene bridge (KGP608) demonstrated potent …
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Synthesis and cytotoxity of oxysterols:studies on the A,B ring polyoxygenated sterols
… studies, the structure-activity relationship (SAR) study in particular, have been hampered by the limited availability of structurally diverse OS in numbers and amounts. The aim of this project was to develop robust synthetic methods for the preparation of polyhydroxyl sterols, thereof, …
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Fused Heterocycles as Spinster Homolog 2 Inhibitors and Regio- and Stereoselective Copper-Catalyzed Borylation-Protodeboronation of 1,3-Diynes: Access to (Z)-1,3-Enynes
… An extensive structure-activity relationship (SAR) study of these scaffolds was performed to analyze the impact of various amine head groups, regioisomers, and alkyl tails on performance. It was determined that 2-aminobenzoxazoles with secondary amines were potent inhibitors of the transporter. …
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