National Repository of Grey Literature 27 records found  1 - 10nextend  jump to record: Search took 0.00 seconds. 
Synthesis and evaluation of potential cholinesterases inhibitors
Houngbedji, Neto-Honorius ; Krátký, Martin (advisor) ; Kučerová, Marta (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of Organic and Bioorganic Chemistry Author: Neto-Honorius Houngbedji Supervisor: PharmDr. Mgr. Martin Krátký, Ph.D. Title of diploma thesis: Synthesis and evaluation of potential inhibitors of cholinesterases During the last years, the number of patients affected by Alzheimer's disease has been constantly increasing. This disease, which burdens the patients as well as their milieu, requires a costly treatment, based on the use of acetylcholinesterase inhibitors currently. The theoretical part summarizes the contemporary knowledge about the pathology, epidemiology and therapy of Alzheimer's disease. This part also presents the results of previous research of salicylanilide-based cholinesterase inhibitors. The use of acetylcholinesterase inhibitors in the treatment of Alzheimer's disease led to the design of eight novel compounds (esters of salicylanilides and phosphorus acids) with inhibitory activity against cholinesterases. Thus, the experimental part of this diploma thesis consists in the synthesis, characterization and biological evaluation of the novel inhibitors. Finally, three new compounds were synthesized and evaluated successfully. Their inhibitory activities (IC50) were within the range of 48.13-66.13 µM against...
Synthesis and evaluation of potential cholinesterases inhibitors
Vu, Quynh Anh ; Krátký, Martin (advisor) ; Palát, Karel (referee)
This bachelor thesis deals with the synthesis of novel acetylcholinesterase and butyrylcholinesterase inhibitors as potential inhibitors of both cholinesterases. All the prepared molecules contain propargylamine structural motif, i.e., a proved scaffold for drugs targeting central nervous system. Some of its derivatives are currently investigated for the treatment of neurodegenerative disorders including Alzheimer's disease. The theoretical part summarizes facts about the Alzheimer's disease and its current treatment focused on cholinergic hypothesis and inhibitors of cholinesterases. The experimental part reports the synthesis and evaluation of potential inhibitors of acetylcholinesterase and butyrylcholinesterase. Seventeen compounds were synthesized in satisfactory yields, predominantly amides and imines of salicylic and cinnamic acid derivatives. All of them were investigated for their activities against both cholinesterases using Ellman's method. 5-Bromo-N-(prop-2-yn-1-yl)salicylamide and N-(prop-2-yn-1- yl)benzamide showed the lowest IC50 values for acetylcholinesterase (8.05 and 23.16 µM, respectively). 2,4-Dibromo-6-[(prop-2-yn-1-yl)carbamoyl]phenyl (N-ethyl-N- methyl)carbamate showed the best inhibition of butyrylcholinesterase (IC50 = 26.09 µM). Several of the prepared compounds were more...
Synthesis and biological evaluation of novel uncharged cholinesterase reactivator against nerve agent intoxication
Vaněk, Mojmír ; Roh, Jaroslav (advisor) ; Krátký, Martin (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Organic and Bioorganic Chemistry Student: Mojmír Vaněk Supervisor: doc. PharmDr. Jaroslav Roh Ph.D. Advisors: PharmDr. Jan Korábečný Ph.D.; PharmDr. Vendula Hepnarová Ph.D. Title of diploma thesis: Synthesis and biological evaluation of novel uncharged cholinesterase reactivator against nerve agent intoxication Nerve agents (NPL) and pesticids are strongly toxic organophosphorus compounds with high affinity to acetylcholinesterase (AChE) enzyme. This enzyme is present in CNS and neuromuscular synapses. The intoxication leads into an acute cholinergic crisis, which can ultimately results into death. The therapy must be quick and includes application of atropine, reactivators of AChE and diazepam. Among the commonly used AChE reactivators, mono- or bis- quarternary aldoximes cen be found. These compounds are permanently charged, so their penetration through the blood-brain barrier (HEB) is very limited (up to 10 %, often only 1-3 %). Within the diploma thesis, a non quarternary AChE reactivator has been developed by multiple-steps synthesis approach. This compound, denoted as K1396, would exert high ability to penetrate through HEB. In vitro assessments of his capability to reactivate AChE has been carried out by method of Ellman....
3D model
Krátký, Martin ; Klečka, Jan (referee) ; Richter, Miloslav (advisor)
The aim of this bachelor thesis is to create a spatial model from images capturing an object illuminated by a laser pattern. The thesis presents possible solutions to the problem using methods of active triangulation and stereoscopy. Methods are designed for laboratory and outdoor measurements. The requirements for the measuring workplace are defined and then the implemented workplace is presented. Each of the designed methods is tested by scanning a series of objects.
Oxadiazoles as potential drugs III.
Lukáčová, Michaela ; Kučerová, Marta (advisor) ; Krátký, Martin (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Chemistry and Pharmaceutical Analysis Title of diploma thesis: Oxadiazoles as potential drugs III. Student: Michaela Lukáčová Supervisor: PharmDr. Marta Kučerová, Ph.D. Theoretical part of this diploma thesis summarises biological activity of 1,2,4-oxadiazoles, while focusing primarily on their antimycobacterial, antibacterial and antifungal effects. 1,2,4-Oxadiazoles are compounds with versatile biological applications, therefore their antioxidant, antiinflammatory, analgesic and cytostatic activity is also mentioned. Based on the facts in the theoretical part, it is perceptible, that 1,2,4-oxadiazoles are substances with great therapeutical potential not only for the treatment of tuberculosis, but also many other diseases. Thus, the experimental part of this work is focused on the synthesis of 5-substituted 3-pyrazinyl-1,2,4-oxadiazoles followed by evaluation of their antibacterial, antifungal and most importantly antimycobacterial activity. Synthesic procedure for each compound is also included. Nine compounds were successfully synthesized, six of them were prepared by reaction of N'-hydroxypyrazine-2-carboximidamide with different carboxylic acid anhydrides and three of them by reaction of...
Synthesis of substituted arylguanidines as potential drugs XIII.
Straka, Ondřej ; Palát, Karel (advisor) ; Krátký, Martin (referee)
Charles university Faculty of Pharmacy in Hradec Králové Department of Organic and Bioorganic Chemistry Author: Ondřej Straka Supervisor: PharmDr. Karel Palát, CSc Title of diploma thesis: Synthesis of substituted arylguanidines as potential drugs XIII. The ever increasing number of bacterial strains resistant to the currently used antibiotics intensifies the demand for new structures with antibacterial activity. Similarly, the high mortality of immunocompromised individuals caused by pathogenic fungi requires the synthesis of new drugs with antifungal activity. At the Department of Organic and Bioorganic Chemistry, the Faculty of Pharmacy, Charles University has been studying for many years with the potential antifungal and antibacterial activity of arylguanidins, which has been linked to this work. Two series of derivatives of arylguanidines, totaling seven substances in four-step synthesis were synthesized in the thesis. In the first step, a sulfide was formed by the reaction of substituted chloronitrobenzene and thiol. The nitro group was reduced to the amino group in the next step. The aniline formed was converted to anilinium chloride using gaseous hydrogen chloride. At the last step of the synthesis, anilinium chloride reacted with cyanamide to form arylguanidine. Antifungal and...
Derivative of Aminobenzoic Acids as Potential Antimicrobial Agents
Brokešová, Kateřina ; Krátký, Martin (advisor) ; Janďourek, Ondřej (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of Organic and Bioorganic Chemistry Candidate: Mgr. Kateřina Brokešová Consultant: PharmDr. Mgr. Martin Krátký, Ph.D. Title of Thesis: Derivatives of Aminobenzoic Acids as Potential Antimicrobial Agents The increasing resistance to previously unnecessarily used antimicrobial drugs has led to the need for search and synthesis of new drugs including Schiff bases. The rigorous thesis deals with the synthesis and subsequent characterization and evaluation of biological properties of new Schiff bases synthesized from substituted salicylaldehydes and aromatic amino acids and their derivatives (3-aminobenzoic, 3,5-diaminobenzoic acids and esters of 4-aminobenzoic acid). The prepared derivatives were evaluated for their antibacterial, antifungal and antimycobacterial activities; cytotoxicity was also investigated for the most active ones. Most of the Schiff bases exhibit antibacterial activity with minimum inhibitory concentration (MIC) from 7.81 µM, which is comparable with a standard drug bacitracin for some strains. Schiff bases appear to be more effective against Gram-positive bacteria including methicillin- resistant Staphylococcus aureus. The newly synthesized compounds are also effective against yeasts and filamentous fungi. The...
Synthesis and in vitro evaluation of novel iron chelators based on salicylaldehyde isonicotinoyl hydrazone
Kubeš, Jan ; Roh, Jaroslav (advisor) ; Krátký, Martin (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Organic and Bioorganic Chemistry Author: Jan Kubeš Supervisors: doc. PharmDr. Jaroslav Roh, PhD. PharmDr. Hana Jansová, PhD. Title of Diploma Thesis: Synthesis and in vitro evaluation of novel iron chelators based on salicylaldehyde isonicotinoyl hydrazone Iron ions (Fe) are required in many vital processes. However, this transition metal may also catalyze reactions which results in the formation of toxic reactive oxygen species (ROS), e.g. Haber- Weiss reaction producing highly toxic hydroxyl radicals. Salicylaldehyde isonicotinoyl hydrazone (SIH) is a tridental chelator selectively forming complexes with Fe ions. As a result of its low molecular weight and good lipophilicity, SIH can be administered orally. It readily enters the cells, effectively chelates the intracellular Fe ions, and is therefore able to very efficiently inhibit the Fe dependent processes, such as production of ROS, but also the synthesis of some proteins and enzymes and the processes they regulate (e.g., cellular growth and proliferation). In this work we focused on the design, synthesis and in vitro evaluation of novel SIH analogues, in particular the thio analogue of SIH (thioSIH, A), analogues derived from (di)hydroxybenzophenone (B) and...
Synthesis of substituted arylguanidines as potential drugs XIII.
Straka, Ondřej ; Palát, Karel (advisor) ; Krátký, Martin (referee)
Charles university Faculty of Pharmacy in Hradec Králové Department of Organic and Bioorganic Chemistry Author: Ondřej Straka Supervisor: PharmDr. Karel Palát, CSc Title of diploma thesis: Synthesis of substituted arylguanidines as potential drugs XIII. The ever increasing number of bacterial strains resistant to the currently used antibiotics intensifies the demand for new structures with antibacterial activity. Similarly, the high mortality of immunocompromised individuals caused by pathogenic fungi requires the synthesis of new drugs with antifungal activity. At the Department of Organic and Bioorganic Chemistry, the Faculty of Pharmacy, Charles University has been studying for many years with the potential antifungal and antibacterial activity of arylguanidins, which has been linked to this work. Two series of derivatives of arylguanidines, totaling seven substances in four-step synthesis were synthesized in the thesis. In the first step, a sulfide was formed by the reaction of substituted chloronitrobenzene and thiol. The nitro group was reduced to the amino group in the next step. The aniline formed was converted to anilinium chloride using gaseous hydrogen chloride. At the last step of the synthesis, anilinium chloride reacted with cyanamide to form arylguanidine. Antifungal and...
Design of the Tractor's front axle drive
Podhora, David ; Krátký, Martin (referee) ; Prokop, Aleš (advisor)
This master’s thesis is deal with the design of the tractor’s front axle drive to enlarge its braking efficiency of the standing tractor fixed by the parking brake. In the first two chapters, the basic information related to the above stated issue is being summarized. Next, procedure of creating the design including the fundamental calculation proposal is being described. In the last chapter, the strain-stress analysis of the selected partial sections of the design is being presented. The final design is supported with the drawing documentation that is being part of this master’s thesis, too.

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See also: similar author names
9 Kratký, Michal
2 Krátký, Matouš
9 Krátký, Michal
1 Krátký, Milan
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