Academic literature on the topic 'Thiazole analogues'

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Journal articles on the topic "Thiazole analogues"

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Pelageev, Dmitry N., Svetlana M. Kovach, Nadezhda N. Balaneva, et al. "Synthesis and biological activity of thiazole--carbohydrate conjugates based on thiacarpine, an analogue of the cytotoxic alkaloid from the ascidian <em>Polycarpa aurata</em>." Mendeleev Communications 35, no. 1 (2025): 66–68. https://doi.org/10.71267/mencom.7522.

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Based on bis(2-amino-4-phenyl-5-thiazolyl) disulfides, thiazole analogues of polycarpine, a cytotoxic alkaloid from the ascidian &lt;em&gt;Polycarpa aurata&lt;/em&gt;, a wide range of thiazole--carbohydrate conjugates based on D-glucose and D-xylose has been obtained. Antitumor and antimicrobial activity for the synthesized compounds has been studied.
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Sharma, Diksha, Archana Sharma, Rakesh Pahwa, Avtar Chand Rana, and Prabodh Chander Sharma. "Design, synthesis, anti-infective and anti-cancer potential of thiazole based Pyrazoles bearing benzothiazole moiety." Journal of medical pharmaceutical and allied sciences 11, no. 2 (2022): 4622–28. http://dx.doi.org/10.55522/jmpas.v11i2.2470.

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A new series of (E)-6-methyl-N-((3-phenyl-1-(4-phenylthiazol-2-yl)-1H-pyrazol-4-yl)methylene)benzo[d]thiazol-2-amine derivatives was developed. Structural investigation of the synthesized derivatives was carried out by several instrumental method of analysis like IR, and 1H-NMR spectroscopy. The titled analogues were examined for in-vitro anticancer and antiinfective activities. The biological findings specified that analogues 5a, 5b, 5d, 5e, 5f and 5g showed most potent antibacterial activity (MIC 62.5-250μg/mL) and 5a, 5e, 5f and 5g displayed most potent antifungal action (MIC 62.5-500 μg/mL
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Tokárová, Zita, Renáta Gašparová, Natália Kabaňová, Marcela Gašparová, and Róbert Balogh. "Hemetsberger–Knittel and Ketcham Synthesis of Heteropentalenes with Two (1:1), Three (1:2)/(2:1) and Four (2:2) Heteroatoms." Reactions 4, no. 2 (2023): 254–73. http://dx.doi.org/10.3390/reactions4020015.

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The synthetic methods leading to furo[3,2-b]pyrroles and thiazolo [5,4-d]thiazoles are reviewed herein. Furo-, thieno- and seleno [3,2-b]pyrroles are related to heteropentalenes, containing two heteroatoms in the entire structure, one each per core. The synthetic approach follows the Hemetsberger–Knittel protocol covering three reaction steps—the nucleophilic substitution of halogen-containing aliphatic carboxylic acid esters, Knoevenagel condensation and, finally, thermolysis promoting the intramolecular cyclocondensation to O,N-heteropentalene. The Hemetsberger–Knittel reaction sequence is a
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Ram, Sevak Verma*1 Nitin Mittal2 Bhumika Yogi3 Shikha Sharma4 Abhishek Mishra5. "A Review On Chemistry And Antimicrobial Activity Of Thiazole." International Journal in Pharmaceutical Sciences 2, no. 3 (2024): 1184–201. https://doi.org/10.5281/zenodo.10893122.

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The recent study classe of five-membered heterocyclic compounds is thiazoles. Several thiazoles, both synthetic and natural, and their derivatives exhibited strong biological activity. Thiazole derivatives exhibit strong antibacterial action against a variety of bacterial species &amp; diseases because of their special characteristics. As a result, the current study assigns different thiazoles and there derivatives' antimicrobial activity. Through the use of many databases, every pertinent piece of literature has been examined. The important studies on the antibacterial activity of thiazole de
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JishaMol., V* Binsalma K.S Vivek M. Rubeena V. K. "SYNTHESIS, CHARACTERISATION AND INVITRO ANTIBACTERIAL SCREENING OF NOVEL THIAZOLE ANALOGUES." Indo American Journal of Pharmaceutical Sciences 04, no. 07 (2017): 1944–51. https://doi.org/10.5281/zenodo.831662.

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Thiazole containing N=C-S moiety exhibit broad spectrum of biological activities like fungicidal, antimicrobial, antitubercular activities and thiazole possess biological activities like bactericidal, antifungal, analgesic, antiinflammatory, diuretic, CNS depressant and anticancer activity. Recent literature reports explore the biological importance of thiazole analogues as antibacterial agent. The aim and objective of the present investigation is to develop novel thiazole analogues. In this study 3 novel thiazole analogues were synthesised by Schiff’s reaction of 2-amino-4-phenylthiazole with
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Stankova, Ivanka, Stoyan Schichkov, Kalina Kostova, and Angel Galabov. "New Analogues of Acyclovir – Synthesis and Biological Activity." Zeitschrift für Naturforschung C 65, no. 1-2 (2010): 29–33. http://dx.doi.org/10.1515/znc-2010-1-205.

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New acyclovir esters with peptidomimetics were synthesized and evaluated in vitro for their antiviral activity against the replication of Herpes simplex virus type 1 (HSV-1) and type 2 (HSV-2). The infl uence of peptidomimetics containing oxazole and thiazolyl-thiazole moieties on the antiviral activity is also reported. The esters were synthesized using the coupling reagents N-ethyl-N’-(3-dimethylaminopropyl)carbodiimide hydrochloride (EDC) and N,N-dimethyl-4-aminopyridine (DMAP) as a catalyst.
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Diness, Frederik, Daniel S. Nielsen, and David P. Fairlie. "Synthesis of the Thiazole–Thiazoline Fragment of Largazole Analogues." Journal of Organic Chemistry 76, no. 23 (2011): 9845–51. http://dx.doi.org/10.1021/jo201675r.

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Gargala, Gilles, Laetitia Le Goff, Jean-Jacques Ballet, Loic Favennec, Andrew V. Stachulski, and Jean-François Rossignol. "Evaluation of New Thiazolide/Thiadiazolide Derivatives Reveals Nitro Group-Independent Efficacy against In Vitro Development of Cryptosporidium parvum." Antimicrobial Agents and Chemotherapy 54, no. 3 (2010): 1315–18. http://dx.doi.org/10.1128/aac.00614-09.

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ABSTRACT Thirty-nine new thiazolide/thiadiazolide compounds were compared with the nitrothiazole nitazoxanide for activity against Cryptosporidium parvum development in HCT-8 cells. Twenty-seven agents exerted ≥90% inhibition. Agents with a lower 50% inhibitory concentration (IC50) than nitazoxanide were either NO2 or halogen 5 substituted on the thiazole moiety. Other 5 substitutions such as methyl, C3H7, C6H11, H, SO2CH3, and SCH3 negatively impacted activity. Five-substituted deacetylated analogues exhibited higher IC50s than their acetylated counterparts. Halogeno-thiazolide/thiadiazolides
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Lamberth, Clemens, Sarah Sulzer-Mosse, and Peter Kubizna. "Synthesis of Ring-Opened Analogues of Oxysterol-Binding Protein-Inhibiting Piperidinyl-thiazole Fungicides." Synlett 28, no. 17 (2017): 2277–80. http://dx.doi.org/10.1055/s-0036-1588473.

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Novel aminoethyl-, aminopropyl-, and aminobutyl-substituted thiazole-4-carboxamides have been prepared which are ring-opened analogues of piperidinyl-thiazole fungicides. Depending of the chain length, completely different synthetic approaches had to be chosen which vary from a Sonogashira coupling with a 2-bromothiazole derivative to a thiazole ring construction from different β- and δ-amino acids.
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Goldstein, BM, JF Leary, BA Farley, VE Marquez, PC Levy, and PT Rowley. "Induction of HL60 cell differentiation by tiazofurin and its analogues: characterization and efficacy." Blood 78, no. 3 (1991): 593–98. http://dx.doi.org/10.1182/blood.v78.3.593.bloodjournal783593.

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Among inducers of myeloid differentiation for leukemic cells, tiazofurin is of special interest because its mechanism of action is known; it inhibits inosine monophosphate dehydrogenase and thus decreases the guanine nucleotide pool. Reported here are three aspects of tiazofurin induction of myeloid differentiation in HL60 human acute promyelocytic leukemia cells. First, inductive efficacy was evaluated for analogues ara-tiazofurin, xylo-tiazofurin, and selenazofurin, for dinucleotide anabolites thiazole-4-carboxamide adenine dinucleotide (TAD) and selenazole-4-carboxamide adenine dinucleotide
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Dissertations / Theses on the topic "Thiazole analogues"

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Johnston, Heather Jennifer. "Development of novel analogues of the anti-proliferative marine natural product bisebromoamide : synthesis and structure activity relationship studies." Thesis, University of Edinburgh, 2014. http://hdl.handle.net/1842/17617.

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The linear peptide bisebromoamide was isolated by the Suenaga group in 2009 from the marine cyanobacterium Lyngbya sp. It exhibits antiproliferative activity at nanomolar levels against a wide range of cell lines. Current SAR data indicates that there is some flexibility in the structure with respect to stereochemistry, but the range of modifications that have been biologically tested is limited, as reviewed in Chapter 1. Bisebromoamide contains a number of non-commercial amino acids and an oxopropyl pyrrolidine moiety which had not been found in a natural product previously. Several new synth
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Amarouch, Hamid. "Synthèse, étude biochimique et parasitologique de nouveaux analogues du Lévamisole et du Pyrantel." Toulouse 3, 1989. http://www.theses.fr/1989TOU30171.

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Le travail presente est relatif a la pharmacomodulation d'imidazothiazoles et de tetrahydropyrimidines a potentialite anthelmintique, analogues de medicaments comme le pyrantel, le tetramisole et l'oxantel. La premiere partie est consacree aux imidazo (2,1-b) thiazoles, thiazolines et benzothiazoles substitues par des heterocycles oxygenes derivant des benzopyrones, decrits par ailleurs comme antiparasitaires. L'heterocyclisation, selon chichibabin, conduit, d'une part, a des bicycles entierement insatures et, d'autre part, apres modification des intermediaires reactionnels, a des dihydro-5,6
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Bzeih, Tourin. "Methodologies involving N-tosylhydrazones for the synthesis of new isocombretastatin A-4 analogs, and the synthesis of thiazole derivatives for antitumor application." Thesis, Université Paris-Saclay (ComUE), 2018. http://www.theses.fr/2018SACLS488.

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Ce document de thèse est divisé en deux parties indépendantes, la première partie décrit la synthèse et l'évaluation biologique de nouveaux analogues du composé anti-vasculaire, l'isocombretastatine A-4. Ce travail se situe à l'interface entre la chimie et la biologie.Des réactions séquentielles monotopes mettant en œuvre des réactions de couplage pallado-catalysées entre des N-tosylhydrazones et divers bromure de nitro-aryles et bromure de nitro-biaryles suivies d'une cyclisation réductrice ont conduit à la synthèse d’une chimiothèque d'indoles C2-, C3-, N-aryles et des carbazoles de vinyle a
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Boulègue, Cyril. "Synthèse d'analogues peptidiques de la chimiokine RANTES : une nouvelle approche dans le traitement des infections par VIH. Etude méthodologique des synthèses stéréosélectives de thiazolines." Montpellier 2, 2000. http://www.theses.fr/2000MON20161.

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Ce travail est scinde en deux parties distinctes l'une portant sur la synthese d'analogues de la chimiokine rantes et l'autre sur une etude methodologique de syntheses stereoselectives de thiazolines. Pour infecter les cellules cibles, le vih a besoin de se lier conjointement en plus du marqueur de surface cd4 a un corecepteur appele recepteur aux chimiokines (ccr et cxcr). Le recepteur ccr5, recepteur des chimiokines mip-1, mip-1 et rantes est connu comme etant le corecepteur principal du vih presentant un tropisme pour les macrophages. Ainsi, la conception de nouveaux antagonistes du recepte
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Dai, Hsiu-Ling, and 戴秀玲. "Study on the Synthesis and Bioactivity of Sulfanilamide and Thiazole analogues." Thesis, 2003. http://ndltd.ncl.edu.tw/handle/96552379495948489828.

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碩士<br>臺北醫學大學<br>藥學系<br>91<br>Study on the Synthesis and Bioactivity of Sulfanilamide and Thiazole analogues Abstract The sulfanilamides were the first effective antibacterial drug which is folic acid antagonist. The sulfanilamide lead molecule constituted the basis for the development of all these types of pharmacological agents which such a varied spectrum of biological actions, as exemplified below for antibacterial agent, carbonic anhydrase inhibitor, diuretic agent, hypoglycemic agent, HIV protease inhibitor, metalloprotease inhibitor. A
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Chen, Liang-I., and 陳俍伊. "Syntheses of Thiazoles Analogues as Anticancer Agents." Thesis, 2018. http://ndltd.ncl.edu.tw/handle/gz69xs.

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Trinh, Nguyen Trieu. "Small molecule inhibitors of the hedgehog signalling pathway as cancer suppressing agents." Thesis, 2016. http://hdl.handle.net/1959.13/1337980.

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Research Doctorate - Doctor of Philosophy (PhD)<br>The HSP plays a pivotal role in the spatial and temporal regulation of cell proliferation and differentiation. Conversely aberrant Hh signalling is involved in Gorlin syndrome, basal cell carcinoma (the most common cancer in the world), and more than one third of all human medulloblastoma cases. In all of these cases, it is believed that deregulated Hh signalling leads to increased cell proliferation and tumour formation. Inhibition of the Hedgehog Signalling Pathway, is a recently validated anti-cancer drug target, with vismodegib (GDC-0449,
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Book chapters on the topic "Thiazole analogues"

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Balasubramanian, Palaniappan, and Garland R. Marshall. "Angiotensin II. Synthesis and biological activity of 8-(R and S)-tetrahydroisoquinoline and 7-(R and S)-(proline)thiazole analogs." In Peptides. Springer Netherlands, 1988. http://dx.doi.org/10.1007/978-94-010-9595-2_133.

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Lange J.H.M. "Conceptual Design of Cannabinoid CB." In Solvay Pharmaceuticals Conferences. IOS Press, 2008. https://doi.org/10.3233/978-1-58603-949-3-111.

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Cannabinoids constitute an area of intensive research, both in industry and in academic institutions. Approximately 15 years ago, tremendous progress has been made in the molecular characterization of endogenous cannabinoids and their receptors. Cannabinoid CB1receptor antagonists showed clinical efficacy in the treatment of obesity and improved cardiovascular and metabolic risk factors. They have good prospects in other therapeutic areas, including smoking and alcohol addiction. Solvay's research achievements in the fast-moving field of CB1receptor antagonists are highlighted in relation with
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Conference papers on the topic "Thiazole analogues"

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Arnout, J., A. Van Hecken, I. Delepeleire, et al. "EFFECTIVENESS AND TOLERABILITY OF CV-3988, A SELECTIVE PAF ANTAGONIST, AFTER INTRAVENOUS ADMINISTRATION TO MAN." In XIth International Congress on Thrombosis and Haemostasis. Schattauer GmbH, 1987. http://dx.doi.org/10.1055/s-0038-1642878.

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Platelet activating factor (PAF) is a naturally occurring phospholipid with a wide spectrum of biological activities. Although PAF has been ascribed a potential role in various conditions including inflammation, asthma, glomerulonephritis and thrombosis, its precise function in physiologic/pathophysiologic processes remains unclear. The introduction of selective PAF receptor antagonists could represent a useful tool to extend our knowledge of the role of this mediator in health and disease.We have investigated the efficacy and tolerability of (RS)-2-methoxy-3-(octadecylcarbomoyloxy)propy1 2-(3
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