Academic literature on the topic '2-Aminothiazole'
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Journal articles on the topic "2-Aminothiazole"
Zhang, Xiao Lin, Hong Xia Ouyang, and Yong Hong Ding. "The Synthesis and Characterization of Potential Novel Active Compounds - 2-aminothiazole Derives Schiff Bases." Advanced Materials Research 396-398 (November 2011): 2489–93. http://dx.doi.org/10.4028/www.scientific.net/amr.396-398.2489.
Full textFarouk Elsadek, Mohamed, Badreldin Mohamed Ahmed, and Mohamed Fawzi Farahat. "An Overview on Synthetic 2-Aminothiazole-Based Compounds Associated with Four Biological Activities." Molecules 26, no. 5 (March 7, 2021): 1449. http://dx.doi.org/10.3390/molecules26051449.
Full textKatritzky, Alan R., Kathleen S. Laurenzo, and Douglas I. Relyea. "The preparation and fungicidal activity of a series of thiazolyl- and isothiazoiyl-diarylcarbinols." Canadian Journal of Chemistry 66, no. 7 (July 1, 1988): 1617–24. http://dx.doi.org/10.1139/v88-262.
Full textSamadhiya, Pushkal, Ritu Sharma, Santosh Srivastava, and Savitri Srivastava. "Synthesis of 2-oxo-azetidine derivatives of 2-amino thiazole and their biological activity." Journal of the Serbian Chemical Society 77, no. 5 (2012): 599–605. http://dx.doi.org/10.2298/jsc110616002s.
Full textToplak, Renata, Nina Lah, Julija Volmajer, Ivan Leban, and Alenka Majcen Le Maréchal. "2-Aminothiazole and 2-aminothiazolinone derivatives." Acta Crystallographica Section C Crystal Structure Communications 59, no. 9 (August 9, 2003): o502—o505. http://dx.doi.org/10.1107/s0108270103015580.
Full textYeşilel, Okan Zafer, Kamber Akdağb, Hümeyra Paşaoğlu, and Orhan Büyükgüngör. "Synthesis And Spectral, Thermal And Structural Characterization Of A Vitamin B13 Complex Of Nickel(II) With 2-Aminothiazole, Mer-[Ni(HOr)(H2o)2(Ata)2]." Zeitschrift für Naturforschung B 62, no. 6 (June 1, 2007): 818–22. http://dx.doi.org/10.1515/znb-2007-0610.
Full textZav'yalov, S. I., N. E. Kravchenko, G. I. Ezhova, L. B. Kulikova, A. G. Zavozin, and O. V. Dorofeeva. "Synthesis of 2-aminothiazole derivatives." Pharmaceutical Chemistry Journal 41, no. 2 (February 2007): 105–8. http://dx.doi.org/10.1007/s11094-007-0023-4.
Full textÇiftçi, Hakan, Hasan Nur Testereci, and Zeki Öktem. "Electrochemical polymerization of 2-aminothiazole." Polymer Bulletin 66, no. 6 (June 4, 2010): 747–60. http://dx.doi.org/10.1007/s00289-010-0307-9.
Full textChohan, Zahid H., and Samina Kausar. "Synthesis, Characterization and Biological Properties of Tridentate NNO, NNS and NNN Donor Thiazole-Derived Furanyl, Thiophenyl and Pyrrolyl Schiff Bases and Their Co(II), Cu(II), Ni(II) and Zn(II) Metal Chelates." Metal-Based Drugs 7, no. 1 (January 1, 2000): 17–22. http://dx.doi.org/10.1155/mbd.2000.17.
Full textArenas, Juan F., Jesús Perez-Peña, and Melchor Gonzalez-Davila. "Vibrational spectra and thermodynamic properties of thiazole, 2-aminothiazole, 2-amino-[2H]-thiazole and 2-amino-[2H2]-thiazole." Collection of Czechoslovak Chemical Communications 54, no. 1 (1989): 28–41. http://dx.doi.org/10.1135/cccc19890028.
Full textDissertations / Theses on the topic "2-Aminothiazole"
Millet, Antoine. "Synthèse et optimisation de nouveaux dérivés anti-mélanome 4-phényl-2-aminothiazole ciblant GRP78 pour contourner les mécanismes de résistances." Thesis, Université Côte d'Azur (ComUE), 2016. http://www.theses.fr/2016AZUR4084.
Full textSince 2011, 7 new anti-melanoma therapies have been approved. They are composed of 4 B-Raf or MEK inhibitors and 3 antibodies, and allowed considerable improvements in the patients’ life span. Nevertheless, the treatment of the resistant form of the melanoma is still an unmet challenge. In this context, this manuscript reports the synthesis and the characterization of new 4-phenyl-2-aminothiazole derivatives active against resistant melanoma. We focused our attention on the modification of the position 2 of the thiazole, the positions 3 and 4 of the phenyl ring, and finally the bis-aryl core. Several derivatives were synthetized and assessed against A375 melanoma cells to depict the structure-activity relationship studies of this new series. Thus, we succeeded in a 10-fold improvement in cytotoxic activity against cancer cells compared with the initial hit, reaching a 0.5 μM EC50 against A375 cell line. Strikingly, lead derivative exerted strong in vivo anti-tumoral activity in mice tumor xenograft experiments. This new series of compound inhibits GRP78, a chaperone protein, resulting in the strong activation level of unfolded protein response and leading to cell death by concomitant apoptotic and autophagy mechanisms. This innovative mode of action confers to our compounds a high cytotoxic activity on various cancer cells (melanoma, pancreatic, CML, colon etc.), regardless to their mutational status. Ultimately, we found a potential clinical candidate that could embody a new solution for the treatment of resistant and aggressive forms of cancer
Schumann, Jörg. "Arylsubstituierte Fünfringheteroaromaten als Halbleiter- und Emittermaterialien zur Anwendung in Organischen Elektrolumineszenzdioden." Doctoral thesis, Technische Universitaet Bergakademie Freiberg Universitaetsbibliothek "Georgius Agricola", 2009. http://nbn-resolving.de/urn:nbn:de:swb:105-2623887.
Full textAnnadurai, Sivakumar. "Lead generation using a privileged structure-based approach." Diss., Temple University Libraries, 2011. http://cdm16002.contentdm.oclc.org/cdm/ref/collection/p245801coll10/id/213119.
Full textPh.D.
In drug discovery there are several approaches to lead generation and one traditional approach involves the synthesis and screening of a structurally diverse compound library against a number of biological targets to identify high affinity lead compounds. The use of a `privileged' structure-based compound library represents a viable approach that could lead to drug like lead compounds. Privileged structures are defined as those ligand substructures that may be used to generate high affinity leads for more than one type of receptor. Examples of privileged structures include phenyl substituted monocycles such as biphenyls, diphenyl methane derivatives, 1,4-dihydropyridines, fused ring systems such as chromones, quinoxalines, quinazolines, 2-benzoxazolones, indoles, benzimidazoles and benzofurans. There are several instances in the literature describing the development of compound libraries based on privileged structures with reportedly high hit rates. Privileged structure based approaches has been used with notable success in the identification of high affinity ligands especially for G-protein coupled receptors (GPCRs). The scaffold 2-aminothiazole (fused and non-fused) may be considered a privileged structure because of its occurrence in a wide variety of pharmaceuticals. The scaffold is found in antibacterials, anti-inflammatory agents, glutamate transporter (GLT-1) modulators, serotonin and muscarinic ligands. The present study involves the synthesis of a 2-aminothiazole (fused and non-fused) based compound library (60 compounds) by incorporating bioactive fragments shown to produce hits in the biological targets of interest. Microwave assisted organic synthesis (MAOS) has been employed at key steps of scaffold synthesis as well as in Suzuki coupling to generate the target aminothiazoles. Preliminary biological screening has resulted in the identification of some promising lead compounds. Trifluoromethoxy substituted aminothiazoles were found to be potent antimicrobials with MIC values in the range of 4-16 microgram/ml. Furanone based aminothiazoles showed affinity for muscarinic receptors. Piperidine based aminothiazoles showed greater than 90% of control (8-OH-DPAT) specific agonist response at the 5-HT1A receptor subtype. The Clog P values of the most potent antimicrobials were found to be in the range of 4.5-6.2 indicating the high lipophilicity of the compounds. High lipophilicity is known to cause solubility issues that may hamper future development. Therefore in an effort to make compounds with intermediate lipophilicity, the phenyl core of the potent aminothiazoles will be replaced with pyridine core using literature procedures (Pyridine core containing aminothiazoles showed Clog P < 4). Future plans include expanding the library, improving the yields of compounds and to evaluate the compounds as modulators of glutamate transporter (GLT-1). The work could be extended to include other privileged structures such as 2-aminooxazole, 2-aminobenzoxazole, 2-aminoimidazole and 2-aminobenzimidazole. These mono and bicyclic heterocyles may be considered bioisosteres of 2-aminothiazole.
Temple University--Theses
Nakamura, Ana Paula Rizzato. "Síntese e caracterização de sílica gel funcionalizada com 2-aminotiazol e 5-amino-1,3,4-tiadiazol-2-tiol para aplicações adsortivas e voltamétricas /." Ilha Solteira, 2018. http://hdl.handle.net/11449/153058.
Full textResumo: No presente trabalho, a 3-cloropropil sílica gel (SG) foi preparada e organofuncionalizada com dois grupos funcionais, 2-aminotiazol (SATZ) e 5-amino-1,3,4-tiadiazol-2-tiol (SATT). Com o objetivo de produzir novos materiais através da modificação química da superfície da sílica gel, com aplicabilidade na remoção de íons metálicos em meio etanólico, tendo a possibilidade de serem aplicados na remoção de metais pesados em combustível etanol e aguardente. Esses novos materiais também podem ser trabalhados como novos eletrodos quimicamente modificados na detecção de nitrito encontrado na urina e em águas naturais. Esses materiais foram caracterizados por técnicas de espectroscopia na Região do Infravermelho (FTIR), ressonância magnética nuclear (RMN) e microscopia eletrônica de varredura (MEV). Posteriormente foram realizados estudos de adsorção de íons metálicos (Cu+2, Cd+2 e Zn+2) para o SATZ e SATT em solvente etanólico (99%). Para testar a capacidade de adsorção de íons metálicos, determinou-se a cinática de adsorção para todos íons Cu+2, Cd+2 e Zn+2 (40 minutos), determinou-se a capacidade de adsorção (Nf) através de isotermas com diferentes concentrações molares dos íons metálicos. Ambos os adsorventes tiveram uma capacidade máxima de adsorção maior para os íons Zn2+ do que para os íons Cd2+ e Cu2+, de acordo com a seguinte ordem: Zn2+>Cd2+>Cu2+. Em uma segunda etapa do trabalho após a adsorção dos íons cúpricos (Cu2+) pelo SATT, reagiu-se o SATT com hexacianoferrato (III) ... (Resumo completo, clicar acesso eletrônico abaixo)
Abstract: In the present work, 3-chloropropyl silica gel (SG) was prepared and organofunctionalized with two functional groups, 2-aminothiazole (SATZ) and 5-amino-1,3,4-thiadiazole-2-thiol (SATT). With the objective of producing new materials through the chemical modification of the silica gel surface, with applicability in the removal of metallic ions in ethanolic medium, having the possibility of being applied in the removal of heavy metals in fuel ethanol and brandy. These new materials can also be worked as new chemically modified electrodes in the detection of nitrite found in urine and in natural waters. These materials were characterized by Infrared Region Spectroscopy (FTIR), Nuclear Magnetic Resonance (NMR) and Scanning Electron Microscopy (SEM) techniques. Subsequently, adsorption studies of metal ions (Cu + 2, Cd + 2 and Zn + 2) were performed for SATZ and SATT in ethanolic solvent (99%). The adsorption kinetics were determined for all metal ions Cu + 2, Cd + 2 and Zn + 2 (40 minutes), the adsorption capacity (Nf) was determined through isotherms with different molar concentrations of the metal ions. Both adsorbents had a maximum adsorption capacity it was higher for Zn2 + ions than for Cd2 + and Cu2 + ions, according to the following order: Zn2 +> Cd2 + > Cu2+ . In a second step of the work after the copper ions (Cu2+) adsorption by SATT, the SATT was reacted with potassium hexacyanoferrate (III), thus forming the CuSATTH complex. The graphite paste electrode chemically mod... (Complete abstract click electronic access below)
Mestre
Ferreira, Renan Barroso 1988. "Síntese e avaliação de 2-aminotiazolinas como potenciais ligantes para receptores imidazolínicos." [s.n.], 2012. http://repositorio.unicamp.br/jspui/handle/REPOSIP/249577.
Full textDissertação (mestrado) - Universidade Estadual de Campinas, Instituto de Química
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Resumo: A clonidina, um agonista a2 central, e um anti-hipertensivo que está em desuso devido a efeitos indesejados, como xerostomia, hipertensão de rebote e síndrome da retirada. Ultimamente acredita-se que a sua atividade e decorrente também do estímulo ao receptor imidazolínico (do subtipo I1), além do receptor a2, que está também associado aos seus efeitos indesejados. Uma vez que a atividade do SNS aumenta com a idade, fármacos I1 seletivos se apresentam como alternativa para contornar estados hipertensivos, decorrentes do aumento de catecolaminas, cuja produção pode ser mediada pelo receptor I1, cuja estrutura ainda não foi definida. No mercado, há dois anti-hipertensivos representativos desta classe, a rilmenidina e a moxonidina, anti-hipertensivos de 2a geração que apresentam uma seletividade I1 muito significativa, mas ainda apresentando efeitos indesejados. Embora estudos teóricos publicados na literatura indiquem similaridade entre as propriedades (geometria, coeficientes de partição e pKa) destes anti-hipertensivos de 2a geração e de uma aminotiazolina, que apresenta uma relação isostérica com a rilmenidina, nenhuma aminotiazolina foi avaliada quanto à sua afinidade por receptores I1. Desta forma, propusemos, neste projeto, a síntese e o estudo da afinidade pelo receptor I1 de uma série de aminotiazolinas, potenciais ligantes destes receptores. Uma serie de nove N-(alquil)-2-aminotiazolinas foi sintetizada e caracterizada, com rendimentos de 6 a 50% para três etapas, utilizando-se a S-ciclização de N-(2-hidroxietil)tiouréias como abordagem sintética. Estudos in vitro evidenciaram interação de uma aminotiazolina com o receptor I1 e ensaios in vivo com ratos normotensos mostraram ausência de efeito hipotensor, mas outros estudos devem ser feitos visto que alguns anti-hipertensivos dessa classe só são ativos em organismos hipertensos
Abstract: Clonidine, a central a2 agonist, is an antihypertensive drug that is in disuse due to undesired effects such as dry mouth, rebound hypertension and withdrawal syndrome. Lately, it is believed that its activity is also due to the stimulation of the imidazolinic receptor (subtype I1) and its undesirable effects are caused by stimulation of the a2-receptor. Since the SNS activity increases with aging, I1 selective drugs is present as an alternative to circumvent hypertensive states due to the increased catecholamine levels, whose production can be mediated by a receptor I1, which structure has no defined yet. In the market, there are two representative 2nd generation antihypertensives of this class, rilmenidine and moxonidine, that have very significant selectivity for I1-receptor, but unwanted effects remain. Although theoretical studies reported in the literature indicate similarity between the properties (geometry, partition coefficients and pKa) of these 2nd generation antihypertensives and a rilmenidine-isoster 2-aminothiazoline, no 2-aminothiazoline was evaluated for its affinity for I1-receptors. Thus, we proposed in this project the synthesis and study of the I1-receptor affinity of 2-aminothiazolines, as potential ligands for these receptors. A series of nine N-alkyl-2-aminothiazolines was synthesized and characterized, in 6 - 50% of yield for three steps, using the S-cyclisation of N-(2-hydroxyethyl)thiourea as synthetic strategy. Studies in vitro showed an interaction between a 2-aminothiazoline and the I1-receptor and in vivo assays with normotensive rats showed no hypotensive effect. Further studies must be done in our laboratory, since some antihypertensive drugs in this class are only active in hypertensive organisms
Mestrado
Quimica Inorganica
Mestre em Química
Wang, Kai-Min, and 王凱民. "Chemistry of Metal Complexes ContainingN-phenyl-N′-cyano-formamidine,2-Aminothiazole or 2-Amino-2 thiazoline." Thesis, 2007. http://ndltd.ncl.edu.tw/handle/10049039733699265406.
Full text中原大學
化學研究所
95
This thesis includes two parts discussing the synthesis, structure andintermolecular interactions of metal complexes containing polydentate ligands. Part I. The reactions of the unsymmetrical N-Phenyl-N′-cyano-formamidine (HPhCNF) ligand with Cd(NO3)2 · 4H2O and Co(NO3)2 · 6H2O affordedtwo complexes of the type M(HPhCNF)2(NO3)2(THF), (M = Cd, 1 ; M =Co), 2 which were characterized by single-crystal X-ray diffraction method and elemental analyses.Both the metal center of complexes 1 and 2 adopt pentagonal bipyramidal geometry. The metal atoms were bonded to two nitrogen atoms of cyano group, four chealting nitrate oxygen atoms, and one oxygen atom of THF solvent group. In these two complexes, C-H---O and N-H---O hydrogen bonds were found to link the molecules. Part II. The reactions of 2-aminotkiazole (2-AT) with AgClO4, AgNO3,Ag2SO4, and Zn(OAc)2 · 2H2O afforded four new complexes of the types of [Ag(2AT)2ClO4], 3 [Ag(2AT)2NO3], 4 [Ag2(2AT)2(SO4)][Ag2(2AT)2](SO4)] · 2(CH3OH), 5 and Zn(OAc)2(2AT)2, 6. Their crystal structures were characterized by single-crystal X-ray diffraction method and elementalanalyses. In complexes 3 and 4, the silver metal centers adopt linear geometry that were bonded to two nitrogen atoms of 2-AT. The molecules adopting linear geometry were interlinked through N-H---O hydrogen bonds. Molecules in complexes 5 were linked through extensive Ag---S, Ag---O, Ag---Ag, S---S, S---O, O---O, hydrogen bondings, and π – π staking interactions. In complex 6, the zinc metal centers were bonded to two nitrogen atoms of two different 2-AT groups, one monodentate acetate and one chealting acetate anion, to form a distorted square pyramidal geometry. The molecules were linked through N-H---O hydrogen bonds and S---S interaction. In compounds 7 and 8, the protonated 2-Amino-2-thiazoline cations, [H(2A2T)]+ were interacted with nitrate and perchlorate anions through hydrogen bonds, forming 1-D hydrogen-bonded tapes. The eight complexes were characterized by single-crystal X-ray diffraction method and elemental analyses.
Phillips, John Hudson. "Design, synthesis and screening of a 2-aminothiazole library for inhibition of nucleotide-diphospho-sugar utilizing enzymes." 2005. http://catalog.hathitrust.org/api/volumes/oclc/70807470.html.
Full textSchumann, Jörg. "Arylsubstituierte Fünfringheteroaromaten als Halbleiter- und Emittermaterialien zur Anwendung in Organischen Elektrolumineszenzdioden." Doctoral thesis, 2001. https://tubaf.qucosa.de/id/qucosa%3A22388.
Full textLin, Pei-Ying, and 林佩穎. "Hypervalent Iodine(III) Reagent Mediated Synthesis of 2-Aminothiazoles and Quinoxalines in Liquid PEG-400." Thesis, 2009. http://ndltd.ncl.edu.tw/handle/48886708600677037141.
Full text高雄醫學大學
藥學研究所
97
Hypervalent iodine(III) compounds have been extensively used in organic syntheses due to their low toxicity, ready availability and easy handling. [Hydroxyl(tosyloxy)iodo]benzene (HTIB), phenyliodine(III) diacetate (PIDA) and phenyliodine(III) bis(trifluoroacetate) (PIFA) are the most frequently used and easily available reagents in the family of iodine compounds. Polyethylene glycols (PEG) are well-known to be inexpensive, recoverable, non-toxic, thermally stable, and biological compatible polymers. Polyethylene glycols are most commonly employed as a support or a phase-transfer catalyst in various organic transformations. Compared with classical molecular solvents, the polyethylene glycols are environmentally benign reaction media. In this work, hypervalent iodine(III) reagents and PEG-400 will be applied to prepare 2-aminothiazoles and quinoxaline derivatives.
Book chapters on the topic "2-Aminothiazole"
Wilkes, Marty C., Paul B. Lavrik, and John Greenplate. "N-Benzoyl-N-alkyl-2-aminothiazole Proinsecticides." In Synthesis and Chemistry of Agrochemicals III, 327–35. Washington, DC: American Chemical Society, 1992. http://dx.doi.org/10.1021/bk-1992-0504.ch029.
Full textFilipowska, Anna, Wojciech Filipowski, and Ewaryst Tkacz. "Study of Structure-Cytotoxicity Relationships of Thiourea Derivatives Containing the 2-Aminothiazole Moiety." In Innovations in Biomedical Engineering, 276–85. Cham: Springer International Publishing, 2016. http://dx.doi.org/10.1007/978-3-319-47154-9_32.
Full textKearney, Patrick C., Monica Fernandez, Mengmeng Fu, and John A. Flygare. "2-Aminothiazoles." In Solid-Phase Organic Syntheses, 1–8. New York, USA: John Wiley & Sons, Inc., 2001. http://dx.doi.org/10.1002/0471220434.ch1.
Full textGarcia-Egido, E., S. Y. F. Wong, and B. H. Warrington. "A Hantzsch Synthesis of 2-Aminothiazoles Performed in a Microreactor System." In Micro Total Analysis Systems 2001, 517–18. Dordrecht: Springer Netherlands, 2001. http://dx.doi.org/10.1007/978-94-010-1015-3_221.
Full textSano, K. "Enzymatic Production of L-Cysteine from DL-2-Aminothiazoline- 4-Carboxylic Acid." In Biochemistry of Vitamin B6, 453–56. Basel: Birkhäuser Basel, 1987. http://dx.doi.org/10.1007/978-3-0348-9308-4_82.
Full text"2-Aminothiazoles." In Privileged Structures in Drug Discovery, 284–320. Hoboken, NJ, USA: John Wiley & Sons, Inc., 2018. http://dx.doi.org/10.1002/9781118686263.ch8.
Full textCailler, Lucie P., Alexander G. Martynov, Yulia G. Gorbunova, Aslan Yu Tsivadze, and Alexander B. Sorokin. "Carbene insertion to N–H bonds of 2-aminothiazole and 2-amino-1,3,4-thiadiazole derivatives catalyzed by iron phthalocyanine." In Porphyrin Science by Women, 1198–207. WORLD SCIENTIFIC, 2021. http://dx.doi.org/10.1142/9789811223556_0106.
Full textConference papers on the topic "2-Aminothiazole"
Touati, Yousseuf, Mohammed Benabdallah, Julio A. Seijas, Noureddine Choukchou-Braham, and M. Pilar Vázquez-Tato. "Reactivity of 2-aminothiazole with benzaldehyde and malononitrile." In The 23rd International Electronic Conference on Synthetic Organic Chemistry. Basel, Switzerland: MDPI, 2019. http://dx.doi.org/10.3390/ecsoc-23-06699.
Full textWang, Xia, Lu Wang, Hua Zou, Wei Qian, and Yaozu Liao. "Synthesis of Poly (2-aminothiazole) Using Chemical Oxidation Method." In 2015 International Conference on Materials, Environmental and Biological Engineering. Paris, France: Atlantis Press, 2015. http://dx.doi.org/10.2991/mebe-15.2015.134.
Full textNaz, Shagufta, Humaira Nadeem, sadia sarwar, Rehan Z. Paracha, Jun Q. Yu, and Fazlul Huq. "Abstract 1967: Synthesis, in vitro evaluation in ovarian cancer cells and molecular modeling analysis of novel 2-aminothiazole and 2-aminopyridine derivatives." In Proceedings: AACR Annual Meeting 2018; April 14-18, 2018; Chicago, IL. American Association for Cancer Research, 2018. http://dx.doi.org/10.1158/1538-7445.am2018-1967.
Full textCaravatti, Giorgio, Vito Guagnano, Robin Fairhurst, Patricia Imbach, Ian Bruce, Mark Knapp, Pascal Furet, et al. "Abstract 1922: 2-Aminothiazoles as potent and selective PI3Kalpha inhibitors: Discovery of NVP-BYL719 and structural basis for the isoform selectivity." In Proceedings: AACR 103rd Annual Meeting 2012‐‐ Mar 31‐Apr 4, 2012; Chicago, IL. American Association for Cancer Research, 2012. http://dx.doi.org/10.1158/1538-7445.am2012-1922.
Full text