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Showing 1 to 20 of 184 for “"structure-activity relationships"”.
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Structure-activity relationships in Werner clathrates
… symmetry, which is a key factor in yielding structures of a particular type. The structures of seventeen compounds have been elucidated by single crystal x-ray analysis. The difficulty has been found to lie in refining disordered guest molecules. Other techniques employed in the initial …
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Structure activity relationships of 1,8-disubstituted thioxanthenones.
… Schistosoma mansoni infections in man. The structure-activity relationships of lucanthone and related compounds have been extensively investigated and the need for a 1-dialkylaminoalkylamino substituent and 4-methyl group established. The symmetrical nature of the thioxanthenone ring …
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Structure-activity relationships of PAI-1 inhibitors
<p>The inhibition of plasminogen activator inhibitor-1 (PAI-1) is anticipated to increase our understanding of various human ailments with which high levels of PAI-1 have been associated, including diabetes, stroke, and atherosclerosis. Previous accounts have reported the synthesis of inhibitors …
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STRUCTURE-ACTIVITY RELATIONSHIPS IN FUNCTIONALIZED PLATINUM-ACRIDINE ANTICANCER AGENTS
… new platinum-based chemotherapies with improved activity and reduced toxicity has become a pressing goal. Many second- and third-generation derivatives of cisplatin have been successful in decreasing toxicity, enhancing delivery, and showing a broader spectrum of antitumor activity. Recently, a …
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Structure-activity relationships of niclosamide to overcome colistin resistance
… niclosamide, known to enhance colistin activity in combination therapy. Despite its potential, niclosamide faces limitations due to poor solubility, bioavailability, and off-target toxicity. Thus, repurposing it as an antibacterial agent necessitates the synthesis of new derivatives …
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Antischistosomal structure-activity relationships of nitrated n-phenyl benzamide derivatives.
… emerging drug resistance, lacks antischistosomal activity against juvenile worms, does not provide a 100% cure, and does not prevent re-infection. N-phenylbenzamides have shown potential as antischistosomal agents although they have not been extensively studied. This study was inspired by one …
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Antischistosomal structure-activity relationships of nitrated n-phenyl benzamide derivatives.
… emerging drug resistance, lacks antischistosomal activity against juvenile worms, does not provide a 100% cure, and does not prevent re-infection. N-phenylbenzamides have shown potential as antischistosomal agents although they have not been extensively studied. This study was inspired by one …
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Quantitative structure-activity relationships of comparative toxicity to aquatic organisms.
Quantitative Structure-Activity relationship (QSAR) attempt statistically to relate the physico-chemical properties of a molecule to its biological activity. A QSAR analysis was performed on the toxicities of up to 75 organic chemicals to two aquatic species, Photobacterium phospherum (known as the …
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Structure-activity relationships of serotonin receptors in isolated smooth muscle
This document only includes an excerpt of the corresponding thesis or dissertation. To request a digital scan of the full text, please contact the Ruth Lilly Medical Library's Interlibrary Loan Department (rlmlill@iu.edu).
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Protein engineering of Heparinase I : elucidation of structure-activity relationships
Thesis (Sc. D.)--Massachusetts Institute of Technology, Dept. of Chemical Engineering, 1996.
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Detailed Characterization of Structure-Activity Relationships in the Human Adiponectin Molecule
… to lead to important new insights concerning its structure and function, and possible roles as a candidate molecule for the experimental treatment of adiponectin-deficiency states. In this thesis, expression constructs for human adiponectin were stably transfected into CHO-S cells, and resulting …
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An investigation of phase transfer catalysis employing quantitative structure-activity relationships
The application of quantitative structure activity relationships to phase transfer catalysis (PTC) has been explored. The primary focus was on hydroxide-initiated PTC reactions, such as enolate alkylations. The tandem [4+2]/[3+2] cycloaddition of nitroalkenes was applied as the key transformation …
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Synthesis and structure activity relationships of ring D modified steroidal hormones
… of high field NMR techniques. A X-ray crystal structure determination of the strained ring D 14α, 17-methano bridged estriol analogue corroborated its structure. The minimum energy conformation of novel estradiol analogues were superimposed on estradiol, and their least square fit values …
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Synthesis and structure-activity relationships of ring D alkyl 19-norsteroids
… but these compounds showed no sigmatropic reactivity and failed to undergo anionic oxy-Cope rearrangement. Hydride reduction of the 16-oxo group gave the corresponding At4-16-alcohols. The stereoselectivity was dependant on the choice of reagent. The ∆¹⁴-l6α-alcohol underwent ·stereodirected …
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Antimalarial imidazopyridazines and aminopyrazines: synthesis, physicochemical optimization and structure-activity relationships
… reported the impressive in vitro antiplasmodial activity and in vivo antimalarial efficacy of the imidazopyridazine lead compound 19 (Figure 1). However, this compound was plagued by poor solubility and a cardiotoxicity risk as shown from its inhibition of the hERG (human ether-a-go-go-related …
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Structure Activity Relationships for Intracellular Loop 2 of the 5HT1A Serotonin Receptor
… Pharmacology/Pharmaceutical Sciences</p> <p> Structure Activity Relationships for Intracellular Loop 2 of the 5HT1A Serotonin Receptor</p> <p>Chairperson: Dr. Keith Parker </p> <p> The human (H) serotonin (5-hydroxytrptamine; 5HT) 1a receptor (R) has been implicated in various physiological …
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Structure Activity Relationships for Intracellular Loop 2 of the 5HT1A Serotonin Receptor
… Pharmacology/Pharmaceutical Sciences</p> <p> Structure Activity Relationships for Intracellular Loop 2 of the 5HT1A Serotonin Receptor</p> <p>Chairperson: Dr. Keith Parker </p> <p> The human (H) serotonin (5-hydroxytrptamine; 5HT) 1a receptor (R) has been implicated in various physiological …
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Aspects of structure-activity relationships and physiology of gastrin and related peptides
… hormone to study with regard to investigation of structure-activity relationships and physiology of a peptide hormone. Gastrin was best known at that stage as a linear peptide comprising 17 amino acids, which was stable at room temperature and was resistant to degradation by vigorous treatments …
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STRUCTURE-ACTIVITY RELATIONSHIPS OFHETEROGENEOUS CATALYSTS FOR THE LIQUID-PHASE H2PRODUCTION FROM NITROGEN-HYDRIDES
… specifically designed to address selected structure-performance relationships for the rational design of materials in the conversion of hydrazine hydrate and ammonia borane to hydrogen. As outlined in Chapter 1, the unique properties of heterogenous catalysts are determined by their …
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