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Journal articles on the topic 'Thiazoles. Heterocyclic compounds'

Author: Grafiati

Published: 4 June 2021

Last updated: 2 February 2022

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1

Luna, Isadora Silva, Rayssa Marques Duarte da Cruz, Ryldene Marques Duarte da Cruz, Rodrigo Santos Aquino de Araújo, and Francisco Jaime Bezerra Mendonça-Junior. "1,4-Dithiane-2,5-diol: A Versatile Synthon for the Synthesis of Sulfur-containing Heterocycles." Current Organic Synthesis 15, no. 8 (2018): 1026–42. http://dx.doi.org/10.2174/1570179415666180821154551.

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Background: 1,4-Dithiane-2,5-diol (1,4-DTD) is the stable dimer of α-mercapto acetaldehyde. This commercially available ambidentade compound is characterized as having in its chemical structure one group that acts as an electrophile and another that acts as a nucleophile, this permits its use as versatile and efficient synthon in synthetic heterocycle procedures. Objective: The aim of this review is to present synthetic applications of 1,4-DTD in heterocyclic chemistry and their applicability to the synthesis of bioactive compounds. Conclusion: Gewald reactions to obtain C-4 and C-5 unsubstitu

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2

Gümüş, Mehmet, Mehmet Yakan, and İrfan Koca. "Recent advances of thiazole hybrids in biological applications." Future Medicinal Chemistry 11, no. 15 (2019): 1979–98. http://dx.doi.org/10.4155/fmc-2018-0196.

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Thiazoles have attracted much synthetic interest due to their wide variety of biological properties and are important members of heterocyclic compounds. In recent years, studies on the synthesis of thiazole compounds have been increasing because of the properties of this core. In particular, the hybrid structures in which the thiazole ring and the other nuclei are linked have gained popularity. Hybrid structures are formed by the combination of different groups of chemical reactivity and biological activity characteristics. In this review, we highlight recent developments related to hybrid str

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3

Abu-Melha, Sraa. "Synthesis, Modeling Study and Antioxidants Activity of New Heterocycles Derived from 4-Antipyrinyl-2-Chloroacetamidothiazoles." Applied Sciences 8, no. 11 (2018): 2128. http://dx.doi.org/10.3390/app8112128.

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The present work reports the preparation of twelve new heterocyclic scaffolds containing an antipyrinyl-thiazole hybrid through the reaction of 4-antipyrinyl-2-chloroacetamido-thiazoles 1 and 6 with various types of nucleophiles, namely; ethyl thioglycolate, 2-mercaptobenzothiazole, 2-mercaptobenzoxazole, ammonium thiocyanate, malononitrile, and salicylaldehyde. The constructed compounds were characterized by conventional spectroscopic techniques (IR, 1H NMR, 13C NMR, and mass analysis). A DFT method (material studio package) was used to predict the geometry, bond lengths, bond angles, and dip

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4

Mohareb, Rafat M., Amr S. Abouzied, and Nermeen S. Abbas. "Synthesis and Biological Evaluation of Novel 4,5,6,7-Tetrahydrobenzo[D]-Thiazol-2- Yl Derivatives Derived from Dimedone with Anti-Tumor, C-Met, Tyrosine Kinase and Pim-1 Inhibitions." Anti-Cancer Agents in Medicinal Chemistry 19, no. 12 (2019): 1438–53. http://dx.doi.org/10.2174/1871520619666190416102144.

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Background: Dimedone and thiazole moieties are privileged scaffolds (acting as primary pharmacophores) in many compounds that are useful to treat several diseases, mainly tropical infectious diseases. Thiazole derivatives are a very important class of compounds due to their wide range of pharmaceutical and therapeutic activities. On the other hand, dimedone is used to synthesize many therapeutically active compounds. Therefore, the combination of both moieties through a single molecule to produce heterocyclic compounds will produce excellent anticancer agents. Objective: The present work repor

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Eldin, Sanaa M. "Reactions of Cyanothioacetamide Derivatives with 2-Hydrazinothiazol-4(5H)-one: Synthesis, Cyclization and Biological Evaluation of Several New Annelated Pyran, Thiazole, 1,2,4-Triazole and 1,2,4-Triazine Derivatives." Zeitschrift für Naturforschung B 54, no. 12 (1999): 1589–97. http://dx.doi.org/10.1515/znb-1999-1218.

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The thiocarboxamidocinnamonitriles (2) reacted with 2-hydrazinothiazol-4(5H)-one (3) to afford the corresponding pyrano[2,3-d]thiazoles (6). Compounds 6 were used for the synthesis of several new annelated pyran, thiazole, 1,2,4-triazole and 1,2,4-triazine derivatives via their reactions with chloroacetic acid, ethyl chloroformate, diethyl oxalate and acetylacetone. Structures were established based on elemental and spectral data studies. Some of the newly synthesized heterocyclic derivatives were tested for their antimicrobial activity.

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6

Evren, Asaf Evrim, Leyla Yurttaş, Busra Eksellı, and Gulsen Akalın-Cıftcı. "Novel Tri-substituted Thiazoles Bearing Piperazine Ring: Synthesis and Evaluation of their Anticancer Activity." Letters in Drug Design & Discovery 16, no. 5 (2019): 547–55. http://dx.doi.org/10.2174/1570180815666180731122118.

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Background: Cancer cells are described as an unregulated growth and spread of abnormal cells. Recently, cancer has become the most important major reason for deaths in the world. Methods: For anticancer activity, we have used the MTT method and determine the early/late apoptosis by flow cytometry. Results: The title compounds were procured by reacting 2-chloro-N-[4-(pyridin-4-yl)thiazol-2- yl]acetamide with some substituted piperazine derivatives. The in vitro anticancer activity of synthesized compounds was tested against C6 rat glioma cells and A549 human lung carcinoma cells. As a result, t

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7

da Silva Filho, Antonio João, Lucinêz da Cruz Dantas, and Otávio Luís de Santana. "Diradicalar Character and Ring Stability of Mesoionic Heterocyclic Oxazoles and Thiazoles by Ab Initio Mono and Multi-Reference Methods." Molecules 25, no. 19 (2020): 4524. http://dx.doi.org/10.3390/molecules25194524.

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Mesoionics are neutral compounds that cannot be represented by a fully covalent or purely ionic structure. Among the possible mesomeric structures of these compounds are the diradical electronic configurations. Theoretical and experimental studies indicate that some mesoionic rings are unstable, which may be related to a significant diradical character, that until then is not quantified. In this work, we investigated the diradical character of four heterocycles: 1,3-oxazol-5-one, 1,3-oxazol-5-thione, 1,3-thiazole-5-one, and 1,3-thiazole-5-thione. The oxazoles are known to be significatively le

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8

EL-Hashash, Maher A., A. Essawy, and Ahmed Sobhy Fawzy. "Synthesis and Antimicrobial Activity of Some Novel Heterocyclic Candidates via Michael Addition Involving 4-(4-Acetamidophenyl)-4-oxobut-2-enoic Acid." Advances in Chemistry 2014 (September 10, 2014): 1–10. http://dx.doi.org/10.1155/2014/619749.

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This paper discusses the utility of 4-(4-acetamidophenyl)-4-oxobut-2-enoic acid as a key starting material for the preparation of a novel series of pyridazinones, thiazoles derivatives, and other heterocycles via interaction with nitrogen, sulfur, and carbon nucleophiles under Michael addition conditions and studies the antimicrobial activities of some of these compounds.

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9

Banert, Klaus. "Functionalized Allenes: Generation by Sigmatropic Rearrangement and Application in Heterocyclic Chemistry." Current Organic Chemistry 23, no. 27 (2020): 3040–63. http://dx.doi.org/10.2174/1385272823666191112102523.

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The present review article summarizes the synthesis of allenes, which bear an adjacent functional group, by [3,3]- or [2,3]-sigmatropic rearrangement of appropriate propargyl substrates. Functionalized allenes, such as allenyl isothiocyanates, isoelenocyanates, isocyanates, thiocyanates, azides, azo compounds and others, are easily available by these methods. In several cases, however, the title compounds show high reactivity, which leads to rapid intermolecular or intramolecular successive reactions. Consequently, synthesis of the allenes by sigmatropic rearrangement has to be combined with s

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Fuentes-Gutiérrez, Alfredo, Everardo Curiel-Quesada, José Correa-Basurto, Alberto Martínez-Muñoz, and Alicia Reyes-Arellano. "N-Heterocycles Scaffolds as Quorum Sensing Inhibitors. Design, Synthesis, Biological and Docking Studies." International Journal of Molecular Sciences 21, no. 24 (2020): 9512. http://dx.doi.org/10.3390/ijms21249512.

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Quorum sensing is a communication system among bacteria to sense the proper time to express their virulence factors. Quorum sensing inhibition is a therapeutic strategy to block bacterial mechanisms of virulence. The aim of this study was to synthesize and evaluate new bioisosteres of N-acyl homoserine lactones as Quorum sensing inhibitors in Chromobacterium violaceum CV026 by quantifying the specific production of violacein. Five series of compounds with different heterocyclic scaffolds were synthesized in good yields: thiazoles, 16a–c, thiazolines 17a–c, benzimidazoles 18a–c, pyridines 19a–c

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11

de Souza, Marcus Vinícius Nora. "Synthesis and biological activity of natural thiazoles: An important class of heterocyclic compounds." Journal of Sulfur Chemistry 26, no. 4-5 (2005): 429–49. http://dx.doi.org/10.1080/17415990500322792.

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12

Shivkant Sharma, Manish Devgun, Karan Wadhwa, and Sahil Banwala. "In-silico molecular docking study of some n-substituted thiazoles derivatives as FabH inhibitors." World Journal of Advanced Research and Reviews 8, no. 2 (2020): 043–55. http://dx.doi.org/10.30574/wjarr.2020.8.2.0387.

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Heterocyclic compounds with thiazole moiety are one of the most promising compounds in the medicinal chemistry possessing numerous therapeutic activities. The present was designed to study the high throughput in silico screening of 10 designed 2-phenyl-amino thiazole derivatives as a potent FABH inhibitor in Molegro virtual docker software (Version 6.0) using 3iL9 as PDB. The docking results showed mol dock score of -90.94 with four hydrogen bonding for the standard drugs griseofulvin, while on the other hand, N-substituted thiazole derivatives S2, S5, S6, S7, S8, and S9 exhibited excellent mo

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13

An, Tran Nguyen Minh, Pham Thai Phuong, Nguyen Minh Quang, et al. "Synthesis, Docking Study, Cytotoxicity, Antioxidant, and Anti-microbial Activities of Novel 2,4-Disubstituted Thiazoles Based on Phenothiazine." Current Organic Synthesis 17, no. 2 (2020): 151–59. http://dx.doi.org/10.2174/1570179417666191220100614.

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: A series of novel 1,3-thiazole derivatives (5a-i) with a modified phenothiazine moiety were synthesized and tested against cancer cell line MCF-7 for their cytotoxicity. Most of them (5a-i) were less cytotoxic or had no activity against MCF-7 cancer cell line. Material and Methods: The IC50 value of compound (4) was 33.84 μM. The compounds (5a-i) were also evaluated for antimicrobial activities, but no significant activity was observed. The antioxidant activity was conducted for target compounds (5a-i). The IC50 value of compound (5b) was 0.151mM. Results: The total amount of energy, ACE (at

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14

Mardaneh, Jalal, Hamid Beyzaei, Seyed Hadi Hashemi, Behzad Ghasemi, and Abbas Rahdar. "Comparative Evaluation of the Inhibitory Potential of Synthetic N-Heterocycles, Cu/Fe3O4@SiO2 Nanocomposites and Some Natural Products against Non-Resistant and Antibiotic-Resistant Acinetobacter baumannii." Pharmaceutical Sciences 26, no. 2 (2020): 184–92. http://dx.doi.org/10.34172/ps.2020.12.

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Background: Acinetobacter baumannii is a common infectious agent in hospitals. New antimicrobial agents are identified and prepared to combat these bacterial pathogens. In this context, the blocking potentials of a series of synthesized N-heterocyclic compounds, Cu/Fe3O4@SiO2 nanocomposites, glycine, poly-L-lysine, nisin and hydroalcoholic extracts of Trachyspermum ammi, Curcuma longa and green tea catechins were evaluated against non-resistant and multidrug-resistant strains of A. baumannii. Methods: Solutions of heterocyclic derivatives and hydroalcoholic extracts of Trachyspermum ammi, Curc

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15

Journal, Baghdad Science. "Synthesis and characterization of some heterocyclic including oxazoles,Thiazoles, Pyridazines, phthalizines and Pyrazoles with evaluating of biological activity." Baghdad Science Journal 10, no. 3 (2013): 818–27. http://dx.doi.org/10.21123/bsj.10.3.818-827.

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A series of new compounds including p-bromo methyl pheno acetate [2]. N-( aminocarbonyl)–p-bromo pheno acetamide [3] , N-( aminothioyl) -p-bromo phenoacetyl amide [4], N-[4-(p-di phenyl)-1,3-oxazol-2-yl]-p-bromopheno acetamide [5],N-[4-p-di phenyl]-1,3-thiazol-2-yl-p-bromo phenoacet amide [6], p-bromopheno acetic acid hydrazide [7] , 1-N-(p-bromo pheno acetyl)-1,2-dihydro-pyridazin-3,6- dione [8], 1-N-(p-bromo pheno acetyl)-1,2-dihydro-phthalazin-3,8- dione[ 9], 1-(p-bromo pheno acetyl)-3-methylpyrazol-5-one [10] and 1-(p-bromo phenol acetyl)- 3,5-dimethyl pyrazole [11] have been synthesized.

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16

Nayak, Swarnagowri, and Santhosh L. Gaonkar. "A Review on Recent Synthetic Strategies and Pharmacological Importance of 1,3-Thiazole Derivatives." Mini-Reviews in Medicinal Chemistry 19, no. 3 (2019): 215–38. http://dx.doi.org/10.2174/1389557518666180816112151.

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Thiazole is the most common heterocyclic compound in heterocyclic chemistry and in drug design. Presence of several reaction sites in the thiazole moiety extends their range of applications and leads to new solutions for challenges in synthetic and medicinal chemistry. Thiazole derivatives are widely used as bioactive agents, liquid crystals, sensors, catalysts, etc. The motivating molecular architecture of 1,3-thiazoles makes them suitable moieties for drug development. In this review, our aim is to corroborate the recent data available on various synthetic strategies and biological propertie

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17

Yurttaş, Leyla, Bahar Demir, and Gülşen A. Çiftçi. "Some Thiazole Derivatives Combined with Different Heterocycles: Cytotoxicity Evaluation and Apoptosis Inducing Studies." Anti-Cancer Agents in Medicinal Chemistry 18, no. 8 (2018): 1115–21. http://dx.doi.org/10.2174/1871520618666180328115314.

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Background: Thiazole ring is an outstanding structure found in many biologically active compounds and clinically available drugs. Because of synthesis simplicity of its derivatives and having a wide range of biological aspects along with high effectiveness, new thiazole derivatives have been studied by medicinal chemists since many years. Objective: Some thiazole compounds combined with different heterocyclic rings were acquired in this study. Novel 5-(4-substituted benzylidene)-2-[(4,5-dimethylthiazol-2-yl)amino]thiazol-4(5H)-one derivatives (4a-g) and 2-(heteroaryl-2/3/5-yl)thio-N-(4,5-dimet

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18

Drapak, І. V. "In silico screening of drug-like molecules for the treatment of cardiovascular diseases on the basis of five-membered privileged heterocycles." Farmatsevtychnyi zhurnal, no. 4 (September 10, 2019): 61–72. http://dx.doi.org/10.32352/0367-3057.4.19.07.

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Among various heterocyclic systems, the derivatives of five-membered heterocycles are of special interest. Most of the above mentioned heterocycles are treatred as so-called privileged structures in modern medicinal chemistry. In silico screening among five-membered heterocycles of molecules for the treatment of cardiovascular diseases is actual. The aim of the work was the search for synthetic drug-like molecules based on functionalized five-membered heterocycles and related heterocyclic systems as an element of the theoretical platform for rational design of compounds acting on the car

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19

Saliyeva, Lesya M., Serhii M. Holota, Alina M. Grozav, et al. "Synthesis, the antiexudative and antimicrobial activity of 6-arylidene substituted imidazo[2,1-b]thiazoles." Journal of Organic and Pharmaceutical Chemistry 19, no. 2(74) (2021): 29–35. http://dx.doi.org/10.24959/ophcj.21.227378.

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Aim. To expand the range of 6-arylidene-2-methyl-2,3-dihydroimidazo[2,1-b]thiazolones as potential objects for studying the antiexudative and antimicrobial activities. Results and discussion. It has been shown that the condensation of synthetically affordable 2-methyl-2,3-dihydroimidazo[2,1-b]thiazolone with aromatic aldehydes can be successfully used for obtaining the corresponding 6-ylidene-functionalized derivatives. The biological screening of the compounds synthesized revealed that they possessed a low or moderate anti-inflammatory activity and inhibited the inflammation process in the ra

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20

Abbasi, Muhammad, Muhammad Ramzan, A. Aziz-Ur-Rehman, et al. "Structure-activity relationship and in silico study of unique bi-heterocycles: 5-[(2-amino-1,3-thiazol-4-yl)methyl]-1,3,4-oxadiazole-2-thiol derivatives." Journal of the Serbian Chemical Society 84, no. 7 (2019): 649–61. http://dx.doi.org/10.2298/jsc180203019a.

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This paper presents the synthesis of some unique bi-heterocyclic hybrid molecules with a thiazole and an oxadiazole ring. The synthesis was initiated by the conversion of ethyl 2-(2-amino-1,3-thiazol-4-yl)acetate (1) to the corresponding 2-(2-amino-1,3-thiazol-4-yl)acetohydrazide (2) by the reaction with hydrazine hydrate in methanol. The treatment of the acid hydrazide, 2, with carbon disulfide gave the bi-heterocyclic nucleophile, 5-[(2-amino-1,3- -thiazol-4-yl)methyl]-1,3,4-oxadiazole-2-thiol (3). Finally, the target compounds, 5a?o, were synthesized by stirring the nucleophile 3 with diffe

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21

Rashdan, Huda R. M., Mohamed El-Naggar, and Aboubakr H. Abdelmonsef. "Synthesis, Molecular Docking Studies and In Silico ADMET Screening of New Heterocycles Linked Thiazole Conjugates as Potent Anti-Hepatic Cancer Agents." Molecules 26, no. 6 (2021): 1705. http://dx.doi.org/10.3390/molecules26061705.

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Thiazoles are important scaffolds in organic chemistry. Biosynthesis of thiazoles is considered to be an excellent target for the design of novel classes of therapeutic agents. In this study, a new series of 2-ethylidenehydrazono-5-arylazothiazoles 5a–d and 2-ethylidenehydrazono-5-arylazo- thiazolones 8a–d were synthesized via the cyclocondensation reaction of the appropriate hydrazonyl halides 4a–d and 7a–d with ethylidene thiosemicarbazide 3, respectively. Furthermore, the thiosemicarbazide derivative 3 was reacted with different bromoacetyl compounds 10–12 to afford the respective thiazole

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22

Mohareb, Rafat, and Hanaa Hana. "Synthesis of progesterone heterocyclic derivatives of potential antimicrobial activity." Acta Pharmaceutica 58, no. 1 (2008): 29–42. http://dx.doi.org/10.2478/v10007-007-0043-3.

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Synthesis of progesterone heterocyclic derivatives of potential antimicrobial activityThe aim of this work was to synthesize steroidal heterocycles and to elucidate the potential role of these compounds as antimicrobial agents. The synthesis of steroidal heterocycles containing the pyrazole, isoxazole, thiazole, pyrane, pyridine, pyridazine, or benzopyrane ring attached to the pregnene nucleus is reported. Progesterone (1) reacts with dimethyl formamide dimethyl acetal to form enamine2. Heterocyclization of2with hydrazines, hydroxylamine, glycine, ethyl acetoacetate or cyanomethylene afforded

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23

Moustafa, Moustafa S., Saleh M. Al-Mousawi, Hesham R. El-Seedi, and Mohamed H. Elnagdi. "Tales of the Unexpected in Synthesis of Polyfunctional Heteroaromatics." Current Organic Synthesis 15, no. 5 (2018): 587–602. http://dx.doi.org/10.2174/1570179414666171116152921.

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Background: Our research group has a longstanding interest in the synthesis of novel functionalized heteroaromatic compounds, and the development of new methods for this purpose. During our ongoing investigations, we recently had an instance to check the reproducibility of some published results concerning the chemistry of arylhydrazonals, enamines and other functionally substituted carbonyl compounds. This work has led to the discovery of some new rearrangements, and the revision of the structures originally assigned to several molecules. Objective: This review surveys some correction of seve

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24

Buceta, N. N., E. M. Coyanis, C. O. Della Védova, A. Haas, M. Schettino, and M. Winter. "Synthesis of new heterocyclic compounds: 4-(3,3,3-trifluoro-2-trifluoromethyl-1-propenyl)-1,3-thiazoles: structural and conformational study of 2-phenyl-4-(3,3,3-trifluoro-2-trifluoromethyl-1-propenyl)-1,3-thiazole." Journal of Physical Organic Chemistry 17, no. 4 (2004): 332–42. http://dx.doi.org/10.1002/poc.733.

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25

GUPTA, RAJUL, Neeraj Kumar FULORIA, and Shivkanya FULORIA. "SYNTHESIS AND ANTIMICROBIAL PROFILE OF SOME NEWER HETEROCYCLES BEARING THIAZOLE MOIETY." SOUTHERN BRAZILIAN JOURNAL OF CHEMISTRY 20, no. 20 (2012): 61–67. http://dx.doi.org/10.48141/sbjchem.v20.n20.2012.64_revista_2012a.pdf.

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Various substituted acetophenones on treatment. with iodine and thiourea yielded 2-amino-4-( substituted-phenyl)-thiazole, which on further treatment with acetic anhydride generated N-(4-(substituted phenyl)thiazol-2-ylacetamide(1-5). All the synthesized compounds were characterized by their respective FTIR, 1H NMR, and mass data. Synthesized compounds (l, 2, 3, 4, 5) when subjected to investigation for their antimicrobial activities i.e. antibacterial and antifungal studies against Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Candida albicans, Aspergillus flavus, and Asper

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Kenari, Marziyeh E., Joshua I. Putman, Ravi P. Singh, et al. "Enantiomeric Separation of New Chiral Azole Compounds." Molecules 26, no. 1 (2021): 213. http://dx.doi.org/10.3390/molecules26010213.

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Twelve new azole compounds were synthesized through an ene reaction involving methylidene heterocycles and phenylmaleimide, producing four oxazoles, five thiazoles, and one pyridine derivative, and ethyl glyoxylate for an oxazole and a thiazole compound. The twelve azoles have a stereogenic center in their structure. Hence, a method to separate the enantiomeric pairs, must be provided if any further study of chemical and pharmacological importance of these compounds is to be accomplished. Six chiral stationary phases were assayed: four were based on macrocyclic glycopeptide selectors and two o

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Liu, Xiang, Yu Huang, Xu Meng, et al. "Recent Developments in the Synthesis of Nitrogen-Containing Heterocycles through C–H/N–H Bond Functionalizations and Oxidative Cyclization." Synlett 30, no. 09 (2019): 1026–36. http://dx.doi.org/10.1055/s-0037-1611476.

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The synthesis and structure of nitrogen-containing heterocycles are fascinating because these compounds have a great richness of structural, physicochemical, and biological properties. Therefore, the development of improved ways for the synthesis of polyfunctional nitrogen-containing heterocycles continues to be a challenging goal. This account describes developments in the discovery of C–H/N–H bond functionalization and oxidative cyclization procedures for the synthesis of nitrogen-containing heterocycles (aziridines, indoles, indolizines, triazoles, imidazoles, oxazoles, thiazoles, quinoxali

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Walmik, Prabhakar, Basavaraj S. Naraboli, Swathi B, and Somashekhar Ghanti. "DESIGN, SYNTHESIS OF BIOLOGICALLY ACTIVE HETEROCYCLES CONTAINING INDOL- THIAZOLYL- THIAZOLIDINONE DERIVATIVES." Asian Journal of Pharmaceutical and Clinical Research 11, no. 3 (2018): 113. http://dx.doi.org/10.22159/ajpcr.2018.v11i3.22199.

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Objective: The present study envisage a novel series of thiazole, indole and thiazolidine derivatives, namely, N-((5-Substituted-2-phenyl-1 H-indol-3-yl)methylene)-4,5,6,7-tetrahydro-5,7,-dimethylbenzo [d]thiazole-2-amine (4a-c), 2-(5-substituted-2-phenyl-1H-indol-3-yl)-3-(4,5,6,7- trimethylbenzo[d]thiazol-2-yl)-thiazolidin-4-one (5a-c) and 5-benzylidine-2-(5-substituted-2phenyl-1H-indol-3yl)-3-(4,5,6,7-tetrahydro-5,5,7- trimethylbenzo[d]thiazol-2-yl) thiazolidin-4-one (6a-c).Methods: All the newly synthesized compounds were characterized by infrared, 1H, 13C nuclear magnetic resonance and mas

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Arshadi, S., E. Vessally, L. Edjlali, R. Hosseinzadeh-Khanmiri, and E. Ghorbani-Kalhor. "N-Propargylamines: versatile building blocks in the construction of thiazole cores." Beilstein Journal of Organic Chemistry 13 (March 30, 2017): 625–38. http://dx.doi.org/10.3762/bjoc.13.61.

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Thiazoles and their hydrogenated analogues are not only key structural units in a wide variety of natural products but they also constitute important building blocks in medicinal chemistry. Therefore, the synthesis of these compounds using new protocols is always interesting. It is well known that N-propargylamines can undergo a number of cyclization reactions to produce various nitrogen-containing heterocycles. In this review, we highlight the most important developments on the synthesis of thiazole and its derivatives starting from N-propargylamines. This review will be helpful in the develo

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Journal, Baghdad Science. "Synthesis of some Heterocyclic Compounds Derived from." Baghdad Science Journal 10, no. 3 (2013): 525–36. http://dx.doi.org/10.21123/bsj.10.3.525-536.

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The 4-(?-bromo acetyl)-4?-toluene sulfonanilide (2) was used as key intermediate to synthesize new heterocyclic compounds. This bromo compound was synthesized via sulfonation of amino group of p-amino acetophenone using Hinsburg method with 4-toluene sulfonyl chloride to form 4-acetyl-4?-toluene sulfonanilide (1) which is used as a starting material in this work. This compound was brominated to yield compound (2) which is used as a precursor to synthesize new five and seven membered heterocyclic compounds such as substituted 1,3-oxazoles (3,4), 1,3-thiazole derivatives (5-7), thiourea compound

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Akishina, E. A., and Е. А. Dikusar. "Chemical modification of different compounds with nitrogen-containing heterocycles." Proceedings of the National Academy of Sciences of Belarus, Chemical Series 57, no. 3 (2021): 356–84. http://dx.doi.org/10.29235/1561-8331-2021-57-3-356-384.

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Heterocyclic compounds have an extremely important practical application, since many heterocycles are the basis of the most valuable medicinal substances, both natural (vitamins, enzymes, alkaloids, etc.) and synthetic biologically active compounds. The work mainly considers the most relevant directions for various purposes drugs search by modifying known bioactive natural, organoelement and framework compounds with 1,2-azole, oxazole, oxadiazole, thiazole, triazole, pyridine, pyrimidine heterocycles over the past 10 years. Chemical modification makes it possible to increase the water solubili

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Al-Mutabagani, Laila A., Fathy M. Abdelrazek, Sobhi M. Gomha, et al. "Synthesis and Biological Evaluation of Thiazolyl-Ethylidene Hydrazino-Thiazole Derivatives: A Novel Heterocyclic System." Applied Sciences 11, no. 19 (2021): 8908. http://dx.doi.org/10.3390/app11198908.

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The reaction of 2-(1-(2-(2-(4-methoxybenzylidene)hydrazinyl)-4-methylthiazol-5-yl)ethylidene)hydrazinecarbothioamide with a range of hydrazonoyl chlorides and α-halo-compounds yielded three new series of thiazole derivatives. Chemical and physical techniques were used to analyze all newly prepared derivatives (1H-NMR, 13C-NMR, FT-IR and mass spectrometry). The potential antimicrobial and anticancer properties of the synthesized derivatives were investigated using various in vitro biological experiments. Most of the thiazole compounds tested were effective against Gram-positive and Gram-negativ

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Sapijanskaitė-Banevič, Birutė, Božena Šovkovaja, Rita Vaickelionienė, Jūratė Šiugždaitė, and Eglė Mickevičiūtė. "Synthesis, Characterization and Bioassay of Novel Substituted 1-(3-(1,3-Thiazol-2-yl)phenyl)-5-oxopyrrolidines." Molecules 25, no. 10 (2020): 2433. http://dx.doi.org/10.3390/molecules25102433.

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Thiazole derivatives attract the attention of scientists both in the field of organic synthesis and bioactivity research due to their high biological activity. In the present study, thiazole ring was obtained by the interaction of 1-(4-(bromoacetyl)phenyl)-5-oxopyrrolidine-3-carboxylic acid with thiocarbamide or benzenecarbothioamide, as well as tioureido acid. A series of substituted 1-(3-(1,3-thiazol-2-yl)phenyl)-5-oxopyrrolidines with pyrrolidinone, thiazole, pyrrole, 1,2,4-triazole, oxadiazole and benzimidazole heterocyclic fragments were synthesized and their antibacterial properties were

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Omar, Rebaz, Pelin Koparir, and Metin Koparir. "SYNTHESIS OF 1,3-THIAZOLE DERIVATIVES." INDIAN DRUGS 58, no. 01 (2021): 7–19. http://dx.doi.org/10.53879/id.58.01.12427.

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Many heterocyclic compounds containing nitrogen atom are used in drug development. Thiazole is one of the most important heterocyclic compounds in drug design, which contains sulfur and nitrogen atom. Different site reactions in thiazole compounds extend to new drug synthesis and plays an important role in medicinal chemistry. Thiazole and derivatives are found to possess widely biological activities such as anti-inflammatory, anti-diabetic, anti-microbial, anti-cancer, anti-consulsant, anti-HIV, anti-hypertensive, anti-Alzheimer, anti-oxidant and anthelmintic. The aim of this review is to cor

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Zakirova, Gladis G., Dmitrii Yu Mladentsev, and Nataliya N. Borisova. "An Approach to Nonsymmetric Bis(tertiary phosphine oxides) Comprising Heterocyclic Fragments via the Pd-Catalyzed Phosphorylation." Synlett 31, no. 18 (2020): 1833–37. http://dx.doi.org/10.1055/s-0040-1706419.

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Nonsymmetric tertiary phosphine oxides with different five- and six-membered heterocyclic fragments such as pyridine, 2,2′-bipyridine, 1,10-phenantroline, quinoline, imidazole, and thiazole were synthesized in good yields via the successive introduction of phosphine oxide groups into the initial dihalogenated heterocycles by means of Pd-catalyzed phosphorylation reaction. The synthesis of pyridine-type compounds is hindered by competing double coupling, while for five-membered heterocycles the principal difficulty is the dehalogenation. Both side processes were successfully suppressed by the u

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Ballazhi, Lulzime, Emil Popovski, Ahmed Jashari, et al. "Potential antiproliferative effect of isoxazolo- and thiazolo coumarin derivatives on breast cancer mediated bone and lung metastases." Acta Pharmaceutica 65, no. 1 (2015): 53–63. http://dx.doi.org/10.1515/acph-2015-0002.

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Abstract The study highlights the current progress in the development of coumarin scaffolds for drug discovery as novel anticancer agents in metastatic breast cancer. Eight compounds, combining the coumarin core and five membered heterocycles (isoxazoles and thiazoles) in hydrazinyldiene- -chroman-2,4-diones, were characterized in terms of a potential antiproliferative effect on bone (SCP1833) and lung (SCP4175) metastatic breast cancer cell lines using the 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide assay. Cell viability was evaluated after 48 and 72 h of treatment and the 50

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Xia, Liang, Yan Zhang, Jingbo Zhang, et al. "Identification of Novel Thiazolo[5,4-b]Pyridine Derivatives as Potent Phosphoinositide 3-Kinase Inhibitors." Molecules 25, no. 20 (2020): 4630. http://dx.doi.org/10.3390/molecules25204630.

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A series of novel 2-pyridyl, 4-morpholinyl substituted thiazolo[5,4-b]pyridine analogues have been designed and synthesized in this paper. These thiazolo[5,4-b]pyridines were efficiently prepared in seven steps from commercially available substances in moderate to good yields. All of these N-heterocyclic compounds were characterized by nuclear magnetic resonance (NMR) and high-resolution mass spectrometry (HRMS) analysis and tested for phosphoinositide 3-kinase (PI3K) enzymatic assay. The results indicated that these N-heterocyclic compounds showed potent PI3K inhibitory activity, and the IC50

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Sharad K. Awate, Suresh V. Patil, Ravindra S. Dhivare, and Renukacharya G. Khanapure. "Microwave-Assisted Synthesis, Characterization and Antimicrobial Potencies of N-Substituted Iminothiazodin-4-One Derivatives." International Journal of Research in Pharmaceutical Sciences 11, no. 1 (2020): 589–95. http://dx.doi.org/10.26452/ijrps.v11i1.1861.

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The biggest and most multifaceted class of organic compounds includes heterocyclic compounds. Currently, several heterocyclic compounds are identified, and persistently gratefulness to tremendous synthetic work and synthetic usefulness, the number is increasing exponentially. In most fields of science, including medicinal, pharmaceutical, and agro-chemistry, heterocyclic compounds have a function, and biochemistry is also another area. In this research article, the green approach is administered for achieving the nitrogen, oxygen and sulphur centered five-membered heterocyclic derivatives. By

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Sbei, Najoua, Anna V. Listratova, Alexander A. Titov, and Leonid G. Voskressensky. "Recent Advances in Electrochemistry for the Synthesis of N-Heterocycles." Synthesis 51, no. 12 (2019): 2455–73. http://dx.doi.org/10.1055/s-0037-1611797.

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The construction of N-heterocyclic rings represents a very important and fast-developing area of organic synthesis. In this context, electrochemistry has emerged as a mild solution for generating in situ the required electrophilic substrates, bases and nucleophiles derived from low-level and extremely stable reagents, the further application of which makes some heterocycles more accessible. In this review, we have covered the recent advances in the electrochemical synthesis of five- and six-membered N-heterocyclic compounds published from 2017 to October 2018.1 Introduction2 Electrochemical Sy

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Ануфрик, С. С., С. Н. Анучин та В. В. Тарковский. "Структура, генерационные характеристики и фотостабильность новых гетерил-кумаринов". Журнал технической физики 128, № 12 (2020): 1889. http://dx.doi.org/10.21883/os.2020.12.50326.127-20.

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The effect of the structure of a number of new laser media based on heteryl-coumarins on their spectral and lasing characteristics is studied under conditions of coherent nanosecond and microsecond lamp pumping. The effect of triazole, oxadiazole, and thiazole heterocycles in the structure of coumarin molecules on the spectral, lasing, and photochemical properties of their ethanol solutions has been studied. The analysis of the influence of heteroatoms, heterocyclic radicals, and an aryl fragment in the conjugation chain on the electron density distribution in the structure of coumarin molecul

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Abu-Melha, Saraa, Sobhi M. Gomha, Amr S. Abouzied, Mastoura M. Edrees, Ahmed S. Abo Dena, and Zeinab A. Muhammad. "Microwave-Assisted One Pot Three-Component Synthesis of Novel Bioactive Thiazolyl-Pyridazinediones as Potential Antimicrobial Agents against Antibiotic-Resistant Bacteria." Molecules 26, no. 14 (2021): 4260. http://dx.doi.org/10.3390/molecules26144260.

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Pyridazine and thiazole derivatives have various biological activities such as antimicrobial, analgesic, anticancer, anticonvulsant, antitubercular and other anticipated biological properties. Chitosan can be used as heterogeneous phase transfer basic biocatalyst in heterocyclic syntheses. Novel 1-thiazolyl-pyridazinedione derivatives were prepared via multicomponent synthesis under microwave irradiation as ecofriendly energy source and using the eco-friendly naturally occurring chitosan basic catalyst with high/efficient yields and short reaction time. All the prepared compounds were fully ch

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Naqvi, Arshi. "Synthesis, Characterization and Drug-Likeness Predictions of 1,3-Thiazole and Benzothiazole Derivatives." Oriental Journal of Chemistry 34, no. 6 (2018): 3134–39. http://dx.doi.org/10.13005/ojc/340660.

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Heterocyclic compounds bearing nitrogen and sulphur in the main skeleton are reported to be a bioactive group. Thiazole and benzothiazole moieties are biologically significant class of this group. This research focus on the synthesis and characterization of 1,3-thiazole and benzothiazole derivatives. Drug likeness predictions were also undertaken for these newly synthesized compounds.

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Journal, Baghdad Science. "Synthesis and Characterization of New Fused Heterocyclic Compounds Consisting of Benzodiazepine, Quinoxaline, Benzimidazole and Thiazole Rings." Baghdad Science Journal 5, no. 3 (2008): 440–45. http://dx.doi.org/10.21123/bsj.5.3.440-445.

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In this study, new heterocyclic compounds were synthesized through the cyclization reactions of o-phenylenediamine (1) with various organic reagents. Benzodiazepine derivatives (2-4) were obtained by reaction of (1) with ethylacetoacetate, malonic acid and acetyl acetone.Treatment of compound (1) with chloroacetamide, chloroacetic acid, p-bromophenacyl bromide and oxalic acid dihydrate afforded quinoxaline derivatives (5-8), respectively. Reaction of compound (1) with benzoic acid, piperonal, cyclohexanone and carbon disulfide resulted in the formation of compounds (9-12), respectively. Finall

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Kaur Bhatia, Richa. "Anti-Protozoal Potential of Heterocyclic Compounds Against Giardiasis." Current Bioactive Compounds 15, no. 3 (2019): 280–88. http://dx.doi.org/10.2174/1573407214666180201154009.

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The aim of this literature review is to compile data of heterocyclic antigiardial agents. The importance is to analyze the structural requirements for improved antigiardial activity, to overcome resistance and enhance the bioavailability of the compounds under study. Though, nitroimidazoles/ imidazoles and benzimidazoles are major classes, other heterocyclic scaffolds viz. oxoindolinylidene, dioxodihydroisobenzofuran-5-carboxamide, fluoroquinolone, thieno[2,3-b]pyridine- 5-carbonitrile, &#945;-amino-phosphonate analogs of polyoxins, nitazoxanide benzologue, thiazole and triazolyl- quinolon

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Saleh, Ebraheem Abdu Musad, Abdullah Mohammed AL Dawsari, Kakul Husain, Ismail Hassan Kutty, and K. M. Lokanatha Rai. "Synthesis, Antibacterial, and Antioxidant Evaluation of Novel Series of Condensed Thiazoloquinazoline with Pyrido, Pyrano, and Benzol Moieties as Five- and Six-Membered Heterocycle Derivatives." Molecules 26, no. 2 (2021): 357. http://dx.doi.org/10.3390/molecules26020357.

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A novel synthesis of thiazolo[2,3-b]quinazolines 4(a–e), pyrido[2′,3′:4,5]thiazolo[2,3-b]quinazolines {5(a–e), 6(a–e), and 7(a–e)}, pyrano[2′,3′:4,5]thiazolo[2,3-b]quinazolines 8(a–e), and benzo[4,5]thiazolo[2,3-b]quinazoloine9(a–e) derivatives starting from 2-(Bis-methylsulfanyl-methylene)-5,5-dimethyl-cyclohexane-1,3-dione 2 as efficient α,α dioxoketen dithioacetal is reported and the synthetic approaches of these types of compounds will provide an innovative molecular framework to the designing of new active heterocyclic compounds. In our study, we also present optimization of the synthetic

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Rawat, Bhupender Singh, and S. C. Mehra. "SYNTHESIS OF SOME NEW 1, 3-DI METHYL SUBSTITUTED GUANIDINE WITH POSSIBLE ANTIBACTERIAL AND ANTIFUNGAL ACTIVITY." Green Chemistry & Technology Letters 2, no. 3 (2016): 138–40. http://dx.doi.org/10.18510/gctl.2016.233.

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The compounds containing thiazole, thiadiazole, oxazole, oxadiazole, imidazole, pyrimidine, pyridine & benzothiazole rings have been found to exhibit broad spectrum of biological activities.Derivatives of 1, 2, 4-thiadiazole and 1, 2, 4-thiadiazolidines exhibit antibacterial and antifungal activity1. Thiazolyl guanidines2 and various substituted aryl guanidine’s have been found to exhibit antibacterial & antifungal activities3.Keeping all these views in mind attempts were made to synthesized some new 1,3-di methyl Substituted Guanidine.In the present work 2,4 Dimethyl -3,5-(di Aryl imi

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Journal, Baghdad Science. "Synthesis, Characterization and Biological Activates Studies of some New Derivatives From 2-aminoo-5-mercapto-1, 3, 4-thiadiazole." Baghdad Science Journal 15, no. 1 (2018): 48–56. http://dx.doi.org/10.21123/bsj.15.1.48-56.

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In this work, thiadiazole derivatives were prepared by taking advantage of active sites in (2-amino-5-mercapto-1, 3, 4-thiadiazole) as a starting material base. The main heterocyclic compounds (1, 3, 4-thiadiazole, oxazole) etc, 2-amino-5-mercapto-1,3,4-thiadiazole compound (1) was prepared by cyclic closure of thiosemicarbazide compound with anhydrous sodium carbonate and carbon disulfide. Oxidation of (1) via hydrogen peroxide, to have (2) which was treated with chloro acetyl chloride to get (3). Preparation of thiazole ring (4) was from reacting of (3) with thiourea. Synthesis of diazonium

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Nagaraju, Pallava, Pedavenkatagari Narayana Reddy, Pannala Padmaja, and Vinod G. Ugale. "Synthesis, Antiproliferative Activity and Molecular Docking of New Thiazole/Benzothiazole Fused Pyranopyrimidine Derivatives." Letters in Organic Chemistry 17, no. 12 (2020): 951–58. http://dx.doi.org/10.2174/1570178617666200319114611.

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A new class of 4H,5H-benzo[4,5]thiazolo[3,2-a]pyrano[2,3-d]pyrimidin-5-one and 5H,6Hpyrano[ 2,3-d]thiazolo[3,2-a]pyrimidin-5-one derivatives were synthesized via the one-pot threecomponent reaction of 2-hydroxy-4H-benzo[4,5]thiazolo[3,2-a]pyrimidin-4-one and 7-hydroxy-5Hthiazolo[ 3,2-a]pyrimidin-5-one to various aromatic aldehydes and malononitrile. This domino transformation involves the formation of pyranopyrimidine ring by the formation of three C–C bonds and one C– O bond a single synthetic operation. As the products precipitate out of the reaction, simple filtration is enough to gather th

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Kovtun, Yu P., and N. N. Romanov. "Condensed heterocycles with the thiazole nucleus. 17. Thiazolo[4,3-a]-isoquinolinium compounds." Chemistry of Heterocyclic Compounds 25, no. 4 (1989): 463–66. http://dx.doi.org/10.1007/bf00480767.

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Journal, Baghdad Science. "Synthesis and Evaluation Antibacterial Activity of Some New Substituted 5-Bromoisatin Containing Five, Six Heterocyclic Ring." Baghdad Science Journal 13, no. 2 (2016): 345–59. http://dx.doi.org/10.21123/bsj.13.2.345-359.

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This research includes the synthesis of some new different heterocyclic derivatives of 5-Bromoisatin. New sulfonylamide, diazine, oxazole, thiazole and 1,2,3-triazole derivatives of 5-Bromoisatin have been synthesized. The synthesis process started by the reaction of 5-Bromoisatin with different reagents to obtain schiff bases of 5-Bromoisatin intermediate compounds(1, 8, 19) by using glacial acetic acid as a catalyst in three routes. The first route, 5-Bromoisatin reacted with p-aminosulfonylchloride to product compound(1), then converted to sulfonyl amide derivatives(2-7) by the reaction of

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