Academic literature on the topic 'Biological and Medical Chemistry'

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Journal articles on the topic "Biological and Medical Chemistry"

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Stechenko, Olena. "BIOLOGICAL AND BIOORGANIC CHEMISTRY IN THE MEDICAL CURRICULA." Science and Education 2019, no. 2 (February 2019): 5–12. http://dx.doi.org/10.24195/2414-4665-2019-2-1.

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The issue of academic mobility was actualized after the accession of Ukraine to the European educational and scientific environment. However, implementation of this principle of providing real credit transfer and learning outcomes according to the methodology of ECTS is quite challenging even today if applied to training of medical students. Several reasons can be indicated for that. Firstly, systems of higher education in the countries of European Union and in Ukraine differ in educational levels, anticipated results as well as in the mechanisms of regulation by the state. Thus, the search of opportunities for creating conditions of the gradual equalization of educational content between different players in the educational market in Europe is urgent. Secondly, implementation of the transition of higher medical education to the training of masters of medicine in accordance with the provisions of the Law of Ukraine "On Higher Education" and introduction of new curriculum by the Ministry of Health of Ukraine has created the basis for differences with the previous curriculum of training specialists on the specialty "General medicine". Thus, comparison of the volume of teaching disciplines for students of the same specialties in different countries is extremely relevant from the point of view of harmonization of efforts for further development of joint educational environment. But equally important is the analysis of changes in the distribution of academic hours from the disciplines that took place during the transition of higher medical education in our country to training specialists in the specialty "General Medicine" for the training of specialists of the second (master's) level of higher education in the specialty "Medicine". In the article the outcomes of comparative analysis of curricula for training medical students in HEIs of Ukraine and some countries of Europe is presented in terms of the number of credits from biological and bioorganic chemistry – one of the key medical biological disciplines. Comparing the educational load from the biological chemistry in HEIs in Ukraine and abroad provides additional grounds for predicting the possibility of recognition credits in the context of academic mobility of medical students.
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Kornberg, Arthur. "Chemistry — the lingua franca of the medical and biological sciences." Chemistry & Biology 3, no. 1 (January 1996): 3–5. http://dx.doi.org/10.1016/s1074-5521(96)90075-7.

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Lesyk, Roman. "Drug design: 4-thiazolidinones applications. Part 1. Synthetic routes to the drug-like molecules." Journal of Medical Science 89, no. 1 (March 31, 2020): e406. http://dx.doi.org/10.20883/medical.406.

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4-Thiazolidinones, as examples of privileged scaffolds, have been the focus of medicinal chemistry since 60th. Among them, 5-substituted thiazolidinones with a C5 exocyclic bond (5-ene derivatives) are of special interest due to chemical characteristics and pharmacological profiles, possessing anticancer, antimicrobial, and antiviral properties, as well as being high-affinity ligands to a number of biological targets. A new medicinal chemistry trend claims that the aforementioned compounds are frequent hitters or pan assay interference compounds, which are useless because of the possible low selectivity. This is argued by the Michael acceptor property of 5-ene-4-thiazolidinones, which is actively discussed in the literature and requires further investigation. Based on SAR analysis, the main vectors for the design of 5-ene-4-thiazolidinone-based molecules were proposed: complication of C5 fragment; introduction of the substituents in the N3 position; synthesis of isosteric heterocycles; combination with other pharmacologically attractive fragments; annealing of thiazolidinone core; utilisation of 5-ene-thiazolidinones in synthesis of other compounds. The affinity of 5-ene-4-thiazolidinones toward various targets can be regarded as an advantage in polypharmacological approaches. Michael acceptors are considered as the “new old tool” for new drug creation, especially anticancer agents. One of the possible solutions within privileged substructure-based diversity-oriented synthesis is the fixation of 5-ene-4-thiazolidinone fragment in the fused heterocycles, for example, thiopyrano[2,3-d]thiazoles obtained from 5-ene-thiazolidinones.
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Hogg, Neil. "Biological chemistry and clinical potential of S-nitrosothiols." Free Radical Biology and Medicine 28, no. 10 (May 2000): 1478–86. http://dx.doi.org/10.1016/s0891-5849(00)00248-3.

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Koppenol, W. H. "Superoxide ion: Chemistry and biological implications, volume I." Free Radical Biology and Medicine 9, no. 6 (January 1990): 541. http://dx.doi.org/10.1016/0891-5849(90)90132-3.

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Koppenol, W. H. "Superoxide ion: Chemistry and biological implications, volume II." Free Radical Biology and Medicine 12, no. 5 (January 1992): 449. http://dx.doi.org/10.1016/0891-5849(92)90094-w.

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Kawase, Masami, Setsuo Saito, and Noboru Motohashi. "Chemistry and biological activity of new 3-benzazepines." International Journal of Antimicrobial Agents 14, no. 3 (April 2000): 193–201. http://dx.doi.org/10.1016/s0924-8579(99)00155-7.

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Liang, Pi-Hui, Chung-Yi Wu, William A. Greenberg, and Chi-Huey Wong. "Glycan arrays: biological and medical applications." Current Opinion in Chemical Biology 12, no. 1 (February 2008): 86–92. http://dx.doi.org/10.1016/j.cbpa.2008.01.031.

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Ali, Fayaz, Narayan S Hosmane, and Yinghuai Zhu. "Boron Chemistry for Medical Applications." Molecules 25, no. 4 (February 13, 2020): 828. http://dx.doi.org/10.3390/molecules25040828.

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Boron compounds now have many applications in a number of fields, including Medicinal Chemistry. Although the uses of boron compounds in pharmacological science have been recognized several decades ago, surprisingly few are found in pharmaceutical drugs. The boron-containing compounds epitomize a new class for medicinal chemists to use in their drug designs. Carboranes are a class of organometallic compounds containing carbon (C), boron (B), and hydrogen (H) and are the most widely studied boron compounds in medicinal chemistry. Additionally, other boron-based compounds are of great interest, such as dodecaborate anions, metallacarboranes and metallaboranes. The boron neutron capture therapy (BNCT) has been utilized for cancer treatment from last decade, where chemotherapy and radiation have their own shortcomings. However, the improvement in the already existing (BPA and/or BSH) localized delivery agents or new tumor-targeted compounds are required before realizing the full clinical potential of BNCT. The work outlined in this short review addresses the advancements in boron containing compounds. Here, we have focused on the possible clinical implications of the new and improved boron-based biologically active compounds for BNCT that are reported to have in vivo and/or in vitro efficacy.
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Amirov, N. K., and Т. A. Abdullin. "70th anniversary of the Department of Inorganic Chemistry of Kazan State Medical University." Kazan medical journal 80, no. 2 (March 25, 1999): 158–59. http://dx.doi.org/10.17816/kazmj66496.

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One of the fundamental disciplines in the training of doctors and pharmacists is bioinorganic and physical colloidal chemistry. Knowledge of the basics of biophysical chemistry and the properties of biogenic elements serve as the basis for the subsequent study of bioorganic and biological chemistry, pharmacology, physiology, sanitation and hygiene, anesthesiology and other disciplines.
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Dissertations / Theses on the topic "Biological and Medical Chemistry"

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Nichols, Alexander J. "Optical Molecular Sensing in Complex Biological Environments." Thesis, Harvard University, 2014. http://nrs.harvard.edu/urn-3:HUL.InstRepos:14226087.

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Although techniques in molecular imaging have advanced considerably over the past several decades, there remain numerous categories of biological molecular targets that are refractory to straightforward imaging. Among these is molecular oxygen, which is vital to a host of physiological as well as pathological processes, as well as the amorphous pigment pheomelanin, which may play a formerly unappreciated role in melanoma carcinogenesis. This thesis describes two related bodies of work that advance techniques in oxygen and pheomelanin imaging, respectively. First, inspired by a desire to understand how hypoxia affects cancer chemotherapy on a cellular level, we designed and synthesized a novel oxygen-sensitive, dendritic nanoconstruct that is capable of spontaneously penetrating through hundreds of microns of multiple cellular layers. After demonstrating our nanoconjugate's oxygen sensitivity using time-domain phosphorescence lifetime measurements, we demonstrate that it retains its oxygen sensitivity in a 3D spheroid in vitro model of ovarian cancer through the use of a custom-made, near infrared-optimized confocal phosphorescence imaging system. Drawing from this approach, we then describe the fabrication and calibration of a separate oxygen-sensing bandage platform for use in wound-healing applications, and demonstrate its use in ex vivo and in vivo animal systems. The second body of work describes the use of non-linear four-wave mixing techniques to facilitate straightforward imaging of the molecular pigment pheomelanin. Recent findings suggest that pheomelanin may play a previously unappreciated role in melanoma carcinogenesis, even in the complete absence of an ultraviolet light insult. However, due to its pale color, pheomelanin is difficult to visualize against a skin background, making its study challenging. After constructing a femtosecond-pulsed coherent anti-Stokes Raman scatter (CARS) microscopy imaging system, we use imaging and spectroscopy to provide proof-of-concept that pheomelanin can be imaged through a combination of CARS microscopy and electronically-enhanced four-wave mixing. We then use our non-linear imaging system to specifically observe pheomelanin in isolated "redhead" mouse melanocytes, and show through an siRNA gene knock-down strategy that our system can be used to observe changes in pheomelanin signal upon modification of biological pathways known to affect pheomelanin synthesis.
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Pokhrel, Laxman. "Design, synthesis, and biological evaluation of tricyclic pyrones and thiouridine nucleosides." Diss., Kansas State University, 2013. http://hdl.handle.net/2097/16233.

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Doctor of Philosophy
Department of Chemistry
Duy H. Hua
The first chapter in this thesis includes the design, synthesis, and evaluation of anti-Alzheimer and anti-norovirus activities of tricyclic pyrones (TPs). Alzheimer’s disease is a major cause of dementia and sixth leading cause of death; it is a growing problem all over the world. On the other hand, norovirus, a highly contagious agent is responsible for more than 90% of non-bacterial gastroenteritis causing severity mainly in the closed environments. No drugs exist to eradicate the symptoms developed by both of these disorders. Studies have shown that the development of Alzheimer’s disease and the infection of norovirus are dependent on cholesterol metabolism. More specifically, the inhibition of acyl-CoA: cholesterol acyltrasferase (ACAT) led to the reduction of plaques in Alzheimer’s disease as well as reduced the infection of norovirus. Mimicking the structure of CP2, a TP with promising anti-Alzheimer activities, a library of tricyclic pyrones containing phenyl, naphthyl, heterocyclic, and dipeptidyl moieties were synthesized and evaluated for their anti-Alzheimer and anti-norovirus efficacies. Several TPs containing phenyl and naphthyl groups showed sub-micromolar to nanomolar potencies for the protection of neuronal MC65 cells from Aβ-oligomers induced death. Similarly, the TPs containing pyrrolyl, imidazolyl, and quinolinyl moieties were effective to inhibit the norovirus replication in low micromolar range. The most effective TPs from MC65 cells protection assay were also effective in the inhibition ACAT and up-regulation ABCA1 gene. The second chapter in this thesis includes the design, synthesis, and anti-norovirus activity of thiouridine nucleosides. Many nucleosides have demonstrated effective inhibition of viral RNA polymerase, and some are progressing at different level of clinical trials for the treatment of hepatitis C virus. Some of the nucleosides, including 2’-C-methyl and 2’-amino substituted analogs, were found to effectively inhibit the norovirus replication. In the search of more potent anti-noroviral compounds, two thiouridine nucleosides were synthesized and evaluated as anti-norovirus agents. Both of these analogs were ineffective up to 50 μM for the inhibition of norovirus replication in cell based assay. Proposed work of converting these nucleosides to their phosphoramidate derivatives is also described.
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Njaria, Paul Magutu. "Antimycobacterial 2-aminoquinazolinones and benzoxazole-based oximes: synthesis, biological evaluation, physicochemical profiling and supramolecular derivatization." Doctoral thesis, University of Cape Town, 2017. http://hdl.handle.net/11427/26954.

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Tuberculosis (TB) is a life-threatening infectious disease caused by Mycobacterium tuberculosis (Mtb). Globally, TB is a major public health burden with an estimated 10.4 million new cases and 1.8 million deaths reported in 2015. Although TB is curable, the treatment options currently available are beset by numerous shortcomings such as lengthy and complex treatment regimens, drug-drug interactions, drug toxicities, as well as emergence of widespread multi-drug resistance. Therefore, there is an urgent and compelling need to develop new, more effective, safer drugs with novel mechanisms of action, and which are capable of shortening treatment duration. This study focused on hit-to-lead optimization of two new classes of compounds with potential anti-TB properties: 2-aminoquinazolinones (AQZs) and benzoxazole-based oximes (BZOs). A hit compound for each of these classes with low micromolar antimycobacterial activity had previously been identified through phenotypic whole-cell in vitro screening.
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Forsyth, Andrea N. "Synthesis and Biological Evaluation of Rigid Analogues of Methamphetamines." ScholarWorks@UNO, 2012. http://scholarworks.uno.edu/td/1436.

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A series of rigid azetidenyl-based methamphetamine analogs were synthesized from commercially available N-Boc-azetidinone. The benzylideneazetidine analogs were prepared via a Wittig olefination via the ylides generated from the corresponding triphenylphosphonium benzylhalide salts. The substituted benzylazetidine analogs were synthesized from the corresponding benzylideneazetidienes via hydrogention over palladium and platinum catalysts. The benzylideneazetidine and benzyliazetidine analogs were evaluated at monoamine transporters as a part of preliminary structure-activity study for the development of novel monoamine transporter ligands. The binding affinities of the azetidine analogs were determined at dopamine (DAT) and serotonin (SERT) transporters in rat brain tissue preparations. The preliminary in vitro binding studies revealed that the rigid scaffold of the azetidine ring system was an effective substitution for the 2-aminopropyl group of methamphetamine and led to compounds with nanomolar binding affinity at dopamine and serotonin. In general, the benzylideneazetidine analogs were more potent than the corresponding benzylazetidine analogs. In addition, the azetidine analogs were more selective for the serotonin transporter than the dopamine transporter. The 3-(3,4-dichlorobenzylidene)azetidine (24m) was the most potent analog of the series with Ki values of 139 nM for SERT and 531 nM for DAT (DAT/SERT = 3.8).
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Zhu, Chongyu. "Polymeric drug delivery systems for biological antimicrobial agents." Thesis, University of Warwick, 2017. http://wrap.warwick.ac.uk/91996/.

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The objective of this work was to develop suitable delivery systems for biological agents that have antimicrobial activities using biocompatible polymers, aiming to reduce their toxicity when administered. Two biological agents, colistin as an antibacterial agent and nystatin (Nys) as an antifungal agent, are the focus of this thesis as they are potent treatments for current pathogen infections, especially to the multidrug-resistant (MDR) bacteria/fungi, but have potential toxicity to human. Polymeric drug delivery systems, including prodrug, hydrogel and micelle formulations, have been developed and discussed for their potential as topical and systemic regimes. The majority of the work was focused on the effect of the covalently attachment of synthetic polymers onto the biological agents upon their antimicrobial activities and the toxicity. The conjugation between colistin and polymers was achieved successfully through either irreversible or releasable linkages. Although irreversible polymer modifications on colistin showed no antimicrobial activity (chapter 2), an acceptable antibacterial activity was observed from the polymer-colistin conjugates with a releasable linkage through either ‘grafting-to’ (chapter 3) or ‘grafting-from’ (chapter 4) approaches. On the other hand, even though the pure polymer-Nys conjugate with a releasable imine linkage cannot be obtained due to the nature of the labile imine bond, the crude conjugate showed an excellent antifungal activity and a reduced toxicity compared to the native Nys (chapter 6). Other polymeric delivery systems were also discussed in this thesis. The incorporation of colistin within a developed hydrogel delivery system as an antibacterial patch for burn infections was investigated through in vitro and in vivo studies, showing a similar antibacterial activity as the native colistin solution against MDR Gram-negative bacteria with no systemic toxicity (chapter 5). Finally, an amphiphilic polymer containing boronic acid groups on the side chains was synthesised and used to target the hydroxyl groups on Nys, expecting to build up an environmental responsive micelle through dynamic boronate ester bond (chapter 7). Although more work is still needed, this system showed a potential to improve Nys solubility.
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Shi, Fengjian. "LASER ELECTROSPRAY MASS SPECTROMETRY: INSTRUMENTATION AND APPLICATION FOR DIRECT ANALYSIS AND MOLECULAR IMAGING OF BIOLOGICAL TISSUE." Diss., Temple University Libraries, 2017. http://cdm16002.contentdm.oclc.org/cdm/ref/collection/p245801coll10/id/445496.

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Chemistry
Ph.D.
This dissertation elucidates the instrumentation and application of a hybrid ambient ionization source, laser electrospray mass spectrometry (LEMS), for the direct analysis and molecular imaging of biological tissue without matrix deposition. In LEMS, laser pulses from a Ti:Sapphire laser amplifier (60 fs, 800 nm, and 1 mJ) interact with surface analytes and transfer them from the condensed phase into the gas phase without the requirement of either exogenous matrix or endogenous water in the sample. The laser vaporized analytes are captured and ionized by an electrospray source, and finally detected by a mass analyzer. It was found that a turn-key, robust femtosecond fiber laser with longer wavelength, longer duration, and lower pulse energy at 1042 nm, 425 fs, and 50 µJ, respectively, provided comparable results with the Ti:Sapphire laser. Vaporization of intact, dried or aqueous cytochrome c and lysozyme samples was demonstrated by the fiber laser. A charge states distribution at lower charge states indicating folded conformation of proteins and the hemoglobin α subunit-heme complex from whole blood was observed. Endogenous anthocyanins, sugars, and other metabolites were detected and revealed the anticipated metabolite profile for the flower petal and leaf samples by the fiber laser. Phospholipids, especially phosphatidylcholine, were identified from a fresh mouse brain section sample. These lipid features were suppressed in both the fiber laser and Ti:Sapphire LEMS measurement in the presence of optimal cutting temperature compounds which are commonly used in animal tissue cryosectioning. This dissertation also details the design of an automated mass spectrometry imaging source based on the Ti:Sapphire LEMS. The laser, translation stage, and mass analyzer are synchronized and controlled using a customized user interface to enable step-by-step scanning of the area of interest on a given tissue sample. The imaging source is coupled with a high resolution accurate mass quadrupole time-of-flight (QTOF) mass analyzer with tandem mass analysis capability. A lateral resolution of 60 µm was demonstrated on a patterned ink film by LEMS imaging. Plant metabolites including sugar and anthocyanins were directly imaged from a leaf sample. Small metabolites, lipids and proteins were simultaneously imaged from a single tissue section of a pig liver sample. Biomarkers of blood-brain barrier damage and traumatic brain injury (TBI) that occurred during the injury were detected and imaged from a TBI mouse brain. The loading values from principal component analysis (PCA) were shown to be useful for identification of features of interest from the large LEMS imaging dataset.
Temple University--Theses
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Jaramillo, Forcada Tatiana. "Synthesis and biological evaluation of natural and synthetic ganoderic acids." Thesis, University of Nottingham, 2017. http://eprints.nottingham.ac.uk/43313/.

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Ganoderma lucidum also known as lingzhi or mushroom of immortality in East Asia countries, has been known for over 2000 years. Ganoderic acids (GA), which are important secondary metabolites of this mushroom, are highly oxygenated lanostane-type entities with extraordinary pharmacological properties. GA are biosynthesised from lanosterol by a still unknown mechanism. The synthesis of thirteen GA analogues and the biological evaluation of ten of them against prostate cell-lines is described in this thesis. Analogues with different functionalities at C-3, C-7, C-8, C-9, C-11, C-23, C-24, C-25 and C-26 of the lanostane frame have been synthesised. As functional groups, alcohols, acetates, ketones, carboxylic acids and single and conjugated double bonds have been introduced. For their preparation, aldehyde 89 was formed from commercial lanosterol in up to 47% overall yield over a 3 or 4 step sequence. Wittig olefination, Reformatsky reaction and direct oxidation of aldehyde 89 provided the precursors from which the analogues were achieved. Analogues were prepared after a total of six to eight steps in 7-44% overall yield. GA and their analogues inhibited the cell viability of prostate cell-lines. However, they were less effective in the inhibition than Taxotere® (docetaxel). Besides, by comparing their IC50 values and thus, building a structure activity relationship (SAR) analysis, the most important positions for activity were determined. Interestingly, some of the ganoderic acids, GA-H (24), and analogues 3-ketone 108 and 7,11-diketone 146, were less toxic for the normal prostate cells than for the pre-malignant ones, conferring on them prophylactic activity. It is believed that ketones at C-3, C-7 and C-11 could be responsible for this behaviour. Ganoderma lucidum is rare in nature. However, due to its great demand, it is now being farmed. For their cultivation sawdust, logs or cork is used. New substrates, otherwise disposed as waste, are being investigated to produce high quality mushrooms, among them oil palm fibres such as mesocarp or empty fruit bunch fibres. Therefore, to unveil new cultivation methods, the triterpene composition of the mushroom grown at different stages, with different substrates or conditions has been assessed and their biological activity evaluated against prostate cancer cell-lines. Cultivating the mushroom in mesocarp or empty fruit bunch fibres produced similar results to those of sawdust. However, poor ventilated conditions reduced their biological activity against prostate cancer cell-lines. Likewise, it was established that triterpene composition varied during different stages and for different target body parts, their biological activity also varied with age, increasing as the mushroom aged during the 2- to 8-week period studied.
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Petersson, Nina. "Optimisation of capillary gel electrophoresis method for enhanced separation of mRNA shortmers." Thesis, Uppsala universitet, Institutionen för kemi - BMC, 2018. http://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-351119.

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Advancements in the field of modified messenger RNA (mRNA) has led to new ventures in the pharmaceutical industry. However, new drug products demand new analytical methods to ensure the efficacy and purity of the drug. Capillary gel electrophoresis (CGE) with UV detection shows great potential for separation of mRNA samples due to the equal mass-to-charge ratio of mRNA and the flexible parameters of the CGE methods. This thesis investigates the optimal parameters of the capillary electrophoresis method, sample treatment procedure and sieving medium composition for enhanced shortmers separation of mRNA by CGE analysis. An RNA ladder with 100-1000 nucleotides and EPO mRNA with 900 nucleotides were used as model compounds. The effect of capillary dimensions and separation temperature on the resolution of the RNA peaks was established through comparative experiments. Sample treatment processes were evaluated to achieve an optimal conformation of the mRNA for CGE analysis. By heating the mRNA sample for 15 min at 80°C all multimers were seemingly eradicated. Moreover, it was found that addition of 4 M of urea to mRNA sample before heating resulted in improved peak shape. A sieving medium consisting of a mix of the two polymers polyvinylpyrrolidine (PVP) and hydroxyethyl cellulose (HEC) proved to have beneficial qualities for separation. The addition of sucrose as viscosity modifier in the sieving medium surprisingly further enhanced the resolution. Moreover, during the project a heavy wash was established which drastically improved repeatability of the analyses through more efficient regeneration of the capillary. ISSN:
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Verma, Abha. "Design, Synthesis and Biological Evaluation of Novel Cannabinoid Antagonist." ScholarWorks@UNO, 2012. http://scholarworks.uno.edu/td/1527.

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This study was aimed at the development of novel CB1 cannabinoid receptor antago­nists that may have clinical applications for the treatment of cannabinoid and psychostimulant addiction. The rationale for the design for our target was to incorporate a bioisosteric 1,2,3-triazole ring into the vicinal diaryl group revealed in the prototypical antagonist/inverse agonist SR141716 (Rimonabant) that was pre­sumed to interact with a unique region in the CB1 receptors. Based on our prelimi­nary results we identified a novel series of 1,2,3-triazole ester and keto deriva­tives as lead compounds for biological evaluation. Here in the design rationale, syn­thesis and CB1 receptor affinity for a series of 4,5-diaryl-1-substituted-1,2,3-triazoles of ester and ketones is described. These derivatives were synthesized via a one-pot regiospecific click/acylation reaction sequence from 1-azido-2,4-dichlorobenzene and commercially available arylacetylenes. From the structure-activity studies the 5-(4-chlorophenyl) congeners exhibited the most potent CB1 receptor affinities relative to other 5-(substituted-phenyl) moieties. The 1-(2,4-dichlorophenyl)-5-(4-chlorophenyl)-4-propylcarbonyl-1,2,3-triazole (­31a) was found to be the most potent (Ki = 4.6 nM) CB1 receptor ligand of the series and exhibited high CB1 selectivity (CB2/CB1 = 417). The triazole ester 31a was further characterized as a cannabinoid antagonist in locomotor-activity studies by blocking the locomotor-reducing effects of cannabinoid agonist WIN55,212-2. In addition, unlike the prototypical cannabinoid antagonist SR141716A (Rimonabant), the triazole ester 31a did not exhibit increased activity in locomotor activ­ity studies, thus indicating the potential for a neutral antagonist profile.
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Muth, Aaron. "Design, Synthesis, and Biological Evaluation of Novel Polyamine Transport System Probes and their Application to Human Cancers." Doctoral diss., University of Central Florida, 2012. http://digital.library.ucf.edu/cdm/ref/collection/ETD/id/5348.

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The mammalian polyamine transport system (PTS) has been of interest due to its roles in cancer and maintaining cellular homeostasis. Polyamines are essential growth factors which are tightly controlled via a balance of biosynthesis, metabolism, import, and export. This work focused on the development and biological testing of polyamine transport probes to help understand the molecular requirements of the PTS. This was mediated through the use of a CHO (PTS active) and CHO-MG* (PTS deficient) screen, where compounds demonstrating high toxicity in CHO and low toxicity in CHO-MG* were considered PTS selective. The first chapter focused on the development of polyamine-based drugs which are both metabolically stable to polyamine oxidase (PAO) activity and are hyperselective for targeting the PTS. This approach was optimized by combining a di-substituted aryl design with terminal N-methylation of the appended polyamine chains to generate a new class of superior PTS agonists. The metabolic stability of these compounds was demonstrated in CHO and CHO-MG* in the presence and absence of a known PAO inhibitor, aminoguanidine (AG). Highly PTS selective compounds were then tested in the NCI-60 cell line screen to demonstrate the effectiveness of polyamine-based drugs in cancer therapy. During this screen, the MALME-3M (human melanoma) cell line was identified as being very sensitive to these PTS targeting drugs. Further studies using MALME-3M and its normal counterpart, MALME-3, showed excellent targeting of the cancer line over MALME-3. For example, The MeN44Nap44NMe compound showed 59-fold higher toxicity in MALME-3M over MALME-3. The second chapter focused on the development of potential polyamine transport inhibitors (PTIs) for use in combination therapy with ?-difluoromethylornithine (DFMO). This therapy is predicated upon reducing sustained polyamine depletion within cells by inhibiting both polyamine biosynthesis with DFMO and polyamine transport with the PTI ligand. Potential PTIs were identified by blocking the uptake of spermidine in DFMO-treated CHO and L3.6pl cells. Previous work has identified a tri-substituted polyamine-based design as an effective PTI. Low toxicity and a low Ki value in a L1210 screen were good predictors for PTI efficacy. The structural requirements for a potent PTI were explored by modulating the toxicity through the introduction of amide bonds, and also by determining the number and orientation of the polyamine messages (appended to an aryl core) required for efficient inhibition of polyamine uptake. These experiments showed that a tri-substituted design and a triamine message (homospermidine) appended was optimal for PTI potency. The final chapter focused on the development of Dihydromotuporamine C derivatives as non-toxic anti-metastatic agents. Dihydromotuporamine C demonstrated good anti-invasive properties with tumor cells. Derivatives were made in an effort to reduce the cytotoxicity of the parent and improve the anti-migration potency. The motuporamine derivatives all have a polyamine message (norspermidine or homospermidine) appended to make a macrocycle core, making them prime targets to evaluate as potential PTS ligands in the CHO and CHO-MG* screen. Each compound was also tested in the highly metastatic pancreatic cancer cell line L3.6pl to determine both its IC50 value and maximum tolerated dose (MTD). The anti-migration assay was performed at the lowest MTD obtained (0.6 [micro]M) in order to compare the series at the same non-toxic dose. The results suggested that as the N1-amine center was moved further from the macrocyclic ring, an increased ability to inhibit cell migration and reduced toxicity was observed. These collective findings provide new tools for cell biologists to modulate and target polyamine transport in mammalian cells. Future applications of these technologies include new cancer therapies which are cell-selective and inhibit the spread of tumors.
Ph.D.
Doctorate
Chemistry
Sciences
Chemistry
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Books on the topic "Biological and Medical Chemistry"

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Raymond, Kenneth William. General, organic, and biological chemistry: An integrated approach. 2nd ed. Hoboken, NJ: Wiley, 2008.

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Raymond, Kenneth William. General, organic, and biological chemistry: An integrated approach. 3rd ed. Hoboken, N.J: Wiley, 2010.

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General, organic, and biological chemistry: An integrated approach. Hoboken, NJ: J. Wiley, 2006.

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Hostettmann, K. Handbook of chemical and biological plant analytical methods. Chichester, West Sussex: John Wiley & Sons Inc., 2014.

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S, Subramanian K., and Woittiez J. R. W, eds. Element analysis of biological samples: Principles and practice. Boca Raton: CRC Press, 1998.

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D, Loike J., ed. Lignans: Chemical, biological, and clinical properties. Cambridge [England]: Cambridge University Press, 1990.

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Garshin, Anatoliy. General and inorganic chemistry in diagrams, figures, tables, and chemical reactions. ru: INFRA-M Academic Publishing LLC., 2020. http://dx.doi.org/10.12737/1070937.

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The textbook in the form of definitions, drawings, diagrams, tables, formulas and chemical reactions outlines the main provisions of General and inorganic chemistry. It is intended for students of non-chemical specialties of higher education institutions. It can be used by students of secondary vocational schools of chemical and medical-biological profiles, secondary school teachers, applicants, foreign students studying in Russian technical universities and natural science faculties of universities, as well as in the system of pre-University training of foreign students. Each Chapter of the manual contains questions for self-control of the knowledge received by the student and checking the depth of assimilation of the studied material.
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Zhou, Michael. Regulated bioanalytical laboratories: Technical and regulatory aspects from global perspectives. Hoboken, N.J: Wiley, 2011.

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Céspedes, Carlos L. Natural antioxidants and biocides from wild medicinal plants. Cambridge, MA: CAB International, 2013.

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1944-, Hostettmann K., Gupta Mahabir P, Marston A. 1953-, International Organization for Chemical Sciences in Development., and CYTED (Organization), eds. Chemistry, biological, and pharmacological properties of medicinal plants from the Americas: Proceedings of the IOCD/CYTED Symposium, Panama City, Panama, 23-26 February 1997. Amsterdam, The Netherlands: Harwood Academic Publishers, 1999.

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Book chapters on the topic "Biological and Medical Chemistry"

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Gorbik, P. P., L. P. Storozhuk, A. A. Chuiko†, L. Yu. Vergun, and V. F. Chekhun. "Magnetically sensitive nanocomposites for medical and biological applications." In Surface Chemistry in Biomedical and Environmental Science, 299–306. Dordrecht: Springer Netherlands, 2006. http://dx.doi.org/10.1007/1-4020-4741-x_26.

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Boitrel, Bernard. "Bismuth Complexes of Porphyrins and their Potential in Medical Applications." In Biological Chemistry of Arsenic, Antimony and Bismuth, 209–40. Chichester, UK: John Wiley & Sons, Ltd, 2010. http://dx.doi.org/10.1002/9780470975503.ch9.

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Vitali, Francesca, and Rudi Fasan. "Biological and Hybrid Biological/Chemical Strategies in Diversity Generation of Peptidic Macrocycles." In Practical Medicinal Chemistry with Macrocycles, 155–84. Hoboken, NJ, USA: John Wiley & Sons, Inc., 2017. http://dx.doi.org/10.1002/9781119092599.ch7.

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Roda, A., S. Girotti, G. Carrea, P. Simoni, M. A. Angellotti, and R. Rizzoli. "Immobilized Biospecific Proteins in Analytical Clinical Chemistry." In Analytical Uses of Immobilized Biological Compounds for Detection, Medical and Industrial Uses, 249–65. Dordrecht: Springer Netherlands, 1988. http://dx.doi.org/10.1007/978-94-009-2895-4_21.

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Brothers, Penelope J., and Christy E. Ruggiero. "Coordination and Solution Chemistry of the Metals: Biological, Medical and Environmental Relevance." In The Group 13 Metals Aluminium, Gallium, Indium and Thallium: Chemical Patterns and Peculiarities, 519–611. Chichester, UK: John Wiley & Sons, Ltd, 2011. http://dx.doi.org/10.1002/9780470976548.ch9.

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Mishra, Bibhudatta, and Gunjan Joshi. "Serotonin: Chemical, Biological, and Therapeutic Aspects." In Handbook of Research on Medicinal Chemistry, 201–37. Toronto ; New Jersey : Apple Academic Press, 2017.: Apple Academic Press, 2017. http://dx.doi.org/10.1201/9781315207414-6.

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Trisciuoglio, Daniela, and Dante Rotili. "Histone Acetyltransferase Enzymes: From Biological Implications to Most Relevant Inhibitors." In Topics in Medicinal Chemistry, 93–122. Cham: Springer International Publishing, 2019. http://dx.doi.org/10.1007/7355_2019_71.

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Wang, Jianing, Ravindra K. Rawal, and Chung K. Chu. "Recent Advances in Carbocyclic Nucleosides: Synthesis and Biological Activity." In Medicinal Chemistry of Nucleic Acids, 1–100. Hoboken, NJ, USA: John Wiley & Sons, Inc., 2011. http://dx.doi.org/10.1002/9781118092804.ch1.

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He, Shuqing, and Zhen Cheng. "Advancements of Second Near-Infrared Biological Window Fluorophores: Mechanism, Synthesis, and Application In Vivo." In Topics in Medicinal Chemistry, 81–123. Cham: Springer International Publishing, 2019. http://dx.doi.org/10.1007/7355_2019_89.

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Carta, Fabrizio, Andrea Angeli, Christian D. T. Nielsen, Claudiu T. Supuran, and Agostino Cilibrizzi. "New Biological Targets for the Treatment of Leishmaniasis." In Medicinal Chemistry of Neglected and Tropical Diseases, 281–309. Boca Raton, FL : CRC Press, Taylor & Francis Group, [2018]: CRC Press, 2019. http://dx.doi.org/10.1201/9781351011655-13.

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Conference papers on the topic "Biological and Medical Chemistry"

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Kaksis, Aris, Agnese Brangule, and Mihails Halitovs. "AN APPROACH TO TEACHING MEDICAL CHEMISTRY THAT HIGHLIGHTS INTERDISCIPLINARY NATURE OF SCIENCE." In 1st International Baltic Symposium on Science and Technology Education. Scientia Socialis Ltd., 2015. http://dx.doi.org/10.33225/balticste/2015.54.

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Thermodynamics is a branch of physics that deals with questions concerning energies and work of a system. It is one of the key topics for understanding processes in the universe as well as any separate system like a gas mixture or a single cell in a biological system. Thermodynamics is included in the university curriculum for engineering, chemistry and physics students as well as medical student curriculum. This paper outlines the problems faced by first year medical students learning thermodynamics at Riga Stradinš University. We describe a medically relevant context based approach to teaching that demonstrates the interdisciplinary nature of medical chemistry, molecular biology and biochemistry. Our method provides a model in which disciplinary barriers are diminished and increased effectiveness of teaching is achieved. Key words: interdisciplinary teaching, medical chemistry, thermodynamics, teaching and learning thermodynamics.
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González-Burgos, Elena, Noelia Fraga Matías, Isabel Maria Ureña Vacas, and M. Pilar Gómez-Serranillos. "Biological evaluation of Cetrarioid clade as cholinesterase inhibitors." In 5th International Electronic Conference on Medicinal Chemistry. Basel, Switzerland: MDPI, 2019. http://dx.doi.org/10.3390/ecmc2019-06316.

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Ratemi, Elaref, and Denis Gravel. "Design, Synthesis and Biological Activity of Selective PHEX Inhibitors." In 1st International Electronic Conference on Medicinal Chemistry. Basel, Switzerland: MDPI, 2015. http://dx.doi.org/10.3390/ecmc-1-a044.

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Kim, Jong H., Kathleen Chan, and Luisa Cheng. "Augmenting the efficacy of antifungal intervention via chemo-biological approaches." In 1st International Electronic Conference on Medicinal Chemistry. Basel, Switzerland: MDPI, 2015. http://dx.doi.org/10.3390/ecmc-1-a011.

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Salvador Gil, Daniel, and Mª Concepción Gimeno. "New Thiourea-thiazolidine Complexes and Study of their Biological Activity." In 3rd International Electronic Conference on Medicinal Chemistry. Basel, Switzerland: MDPI, 2017. http://dx.doi.org/10.3390/ecmc-3-04665.

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Auria-Luna, Fernando, M. Eugenia Marqués-López, M. Concepción Gimeno, and Raquel P. Herrera. "Organocatalytic Synthesis of Chiral 1,4-Dihydropyridines with Potential Biological Properties." In 3rd International Electronic Conference on Medicinal Chemistry. Basel, Switzerland: MDPI, 2017. http://dx.doi.org/10.3390/ecmc-3-04671.

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Fantacuzzi, Marialuigia. "Synthesis, biological evaluation, and docking study of indole aryl sulfonamides as aromatase inhibitors." In 5th International Electronic Conference on Medicinal Chemistry. Basel, Switzerland: MDPI, 2019. http://dx.doi.org/10.3390/ecmc2019-06361.

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Silva-Júnior, Edeildo, Gabriel Passos, Matheus Gomes, Thiago Aquino, Stephannie Souza, João Cavalcante, Elane Santos, Ênio Bassi, and João Araújo-Júnior. "Design, synthesis and in vitro biological evaluation of acrylamide derivatives against Chikungunya virus." In 5th International Electronic Conference on Medicinal Chemistry. Basel, Switzerland: MDPI, 2019. http://dx.doi.org/10.3390/ecmc2019-06379.

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Maccallini, Cristina. "Synthesis and biological evaluation of inducible nitric oxide synthase inhibitors as anticancer agents." In 6th International Electronic Conference on Medicinal Chemistry. Basel, Switzerland: MDPI, 2020. http://dx.doi.org/10.3390/ecmc2020-07370.

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Baitiche, Milad, Marc Le Borgne, Dounia Sid, Zineb Elbahri, Ferhat Djerboua, and Mokhtar Boutahala. "Development of water-soluble ternary system for enhancing biological activities of mefenamic acid." In 6th International Electronic Conference on Medicinal Chemistry. Basel, Switzerland: MDPI, 2020. http://dx.doi.org/10.3390/ecmc2020-07461.

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Reports on the topic "Biological and Medical Chemistry"

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Price, Barbara B. Chemical Biological Medical Treatment Symposia-III. Fort Belvoir, VA: Defense Technical Information Center, April 2001. http://dx.doi.org/10.21236/ada394695.

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Sidell, Frederick R., Ernest T. Takafuji, and David R. Franz. Medical Aspects of Chemical and Biological Warfare. Fort Belvoir, VA: Defense Technical Information Center, January 1997. http://dx.doi.org/10.21236/ada398241.

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Barr, S. H., ed. Division of Biological and Medical Research research summary 1984-1985. Office of Scientific and Technical Information (OSTI), August 1985. http://dx.doi.org/10.2172/6039516.

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Baker, J., D. Bernard, S. Christensen, M. Sale, J. Freda, K. Heltcher, L. Rowe, et al. Biological effects of changes in surface water acid-base chemistry. Office of Scientific and Technical Information (OSTI), January 1990. http://dx.doi.org/10.2172/7255574.

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Beebe, Steven J. Second International Symposium on Nonthermal Medical/Biological Treatments using Electromagnetic Fields and Ionized Gases. Fort Belvoir, VA: Defense Technical Information Center, May 2001. http://dx.doi.org/10.21236/ada388316.

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Schoenbach, Karl H. First International Symposium on Nonthermal Medical/Biological Treatments using Electromagnetic Fields and Ionized Gases. Fort Belvoir, VA: Defense Technical Information Center, November 1999. http://dx.doi.org/10.21236/ada376636.

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Curling, Carl A., and Julia K. Burr. NATO Allied Joint Medical Publication 7: Allied Joint Medical Doctrine for Support to Chemical, Biological, Radiological, and Nuclear (CBRN) Defensive Operations, Final Draft. Fort Belvoir, VA: Defense Technical Information Center, July 2014. http://dx.doi.org/10.21236/ada614619.

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Sutton, M., B. Andresen, S. Burastero, M. Chiarappa-Zucca, S. Chinn, P. Coronado, A. Gash, J. Perkins, A. Sawvel, and S. Szechenyi. Modern Chemistry Techniques Applied to Metal Behavior and Chelation in Medical and Environmental Systems ? Final Report. Office of Scientific and Technical Information (OSTI), February 2005. http://dx.doi.org/10.2172/15015925.

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Chung, Myung, Li Dong, Rong Fu, Lance Liotta, Aarthi Narayanan, Emanuel Petricoin, Mark Ross, et al. Rapid Detection of Biological and Chemical Threat Agents Using Physical Chemistry, Active Detection, and Computational Analysis. Office of Scientific and Technical Information (OSTI), January 2007. http://dx.doi.org/10.2172/1049503.

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Burr, Julia K., Carl A. Curling, and Lucas A. LaViolet. Exercise "Dread Night": Using Allied Medical Publication-8(C) to Estimate Chemical, Biological, Radiological, and Nuclear (CBRN) Casualties. Fort Belvoir, VA: Defense Technical Information Center, August 2010. http://dx.doi.org/10.21236/ada531193.

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