Synthesis and antiviral activity of some new bis-1,3-thiazole derivatives

Dawood, Kamal M.; Eldebss, Taha M. A.; Elzahabi, Heba S. A.; Yousef, Mahmoud H Ayesh Haj

doi:10.1016/j.ejmech.2015.08.005

Cited by 101 publications

(31 citation statements)

References 33 publications

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“…In particular, thiazole is a well-known heterocyclic aromatic compound that contains sulfur and nitrogen atoms at positions 1 and 3 of its five-member ring, respectively [ 20 ]. Τhiazole moiety can be found in numerous biologically active compounds of natural origin (e.g., thiamine [ 19 , 20 ], mycothiazole [ 21 ], cystothiazole C [ 22 ], as well as synthetic molecules possessing a wide range of pharmacological activities such as antimicrobial [ 23 , 24 , 25 , 26 , 27 , 28 ], antiviral [ 29 , 30 ], antitubercular [ 23 , 31 ], anti-inflammatory [ 32 , 33 , 34 ], anxiolytic [ 35 ], anaesthetic [ 36 ], anticonvulsant [ 37 , 38 , 39 , 40 ], etc.). There is a large number of known marketed drugs containing thiazole rings, such as the anthelmintic tiabendazole, the antibacterial sulfathiazole, the anticonvulsant riluzole, the anti-ulcer alizatidine, the antiparkinsonian talipexole, the antischistosomal niridazole, the antiviral ritonavir and the anti-inflammatory meloxicam.…”

Section: Introductionmentioning

confidence: 99%

Thiazoles and Thiazolidinones as COX/LOX Inhibitors

2018

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Inflammation is a natural process that is connected to various conditions and disorders such as arthritis, psoriasis, cancer, infections, asthma, etc. Based on the fact that cyclooxygenase isoenzymes (COX-1, COX-2) are responsible for the production of prostaglandins that play an important role in inflammation, traditional treatment approaches include administration of non-steroidal anti-inflammatory drugs (NSAIDs), which act as selective or non-selective COX inhibitors. Almost all of them present a number of unwanted, often serious, side effects as a consequence of interference with the arachidonic acid cascade. In search for new drugs to avoid side effects, while maintaining high potency over inflammation, scientists turned their interest to the synthesis of dual COX/LOX inhibitors, which could provide numerous therapeutic advantages in terms of anti-inflammatory activity, improved gastric protection and safer cardiovascular profile compared to conventional NSAIDs. Τhiazole and thiazolidinone moieties can be found in numerous biologically active compounds of natural origin, as well as synthetic molecules that possess a wide range of pharmacological activities. This review focuses on the biological activity of several thiazole and thiazolidinone derivatives as COX-1/COX-2 and LOX inhibitors.

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Section: Introductionmentioning

confidence: 99%

Thiazoles and Thiazolidinones as COX/LOX Inhibitors

2018

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“…Thiazole and its derivatives are among the most active classes of compounds that are known for their broad spectrum of activity, e.g., antibacterial [53], antifungal [54], antimalarial [55], antitubercular [56], antiviral [57], anti-inflammatory [58], antidiabetic [59], anthelmintic [60], anticonvulsant [61], antioxidant [62], anticancer [63], and cardiovascular activities [64], and known as new inhibitors of bacterial DNA gyrase B [65]. Some drugs that already are on the market including the recent entry dasatinib possess thiazoles nucleus [66].…”

Section: Biological Importance Of Thiazolesmentioning

confidence: 99%

Synthesis and Biological Evaluation of Thiazole Derivatives

Ibrahim¹,

Rizk²

2021

Azoles - Synthesis, Properties, Applications and Perspectives

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Thiazoles belong to the group of azole heterocycles. They are aromatic five-membered heterocycles containing one sulfur and one nitrogen atom. In recent years thiazoles, their derivatives, and isomers have gained considerable attention because of their broad applications in different fields, such as agrochemicals, industrial, and photographic sensitizers. Also, they have pharmaceutical and biological activities that include antimicrobial (sulfazole), antiretroviral (ritonavir), antifungal (abafungin), anticancer (tiazofurin), antidiabetic, anti-inflammatory, anti-Alzheimer, antihypertensive, antioxidant, and hepatoprotective activities. The compounds containing thiazole moieties are a prominent structural feature in a variety of natural products, such as vitamin B and penicillin. Thus, in this chapter several types of thiazole-based heterocyclic scaffolds such as monocyclic or bicyclic systems synthesis and their biological activities studies are presented. Furthermore modification of thiazole-based compounds at different positions to generate new molecules with potent antitumor, antioxidant, and antimicrobial activities is described.

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“…The nitrogen-containing five-membered heterocycles-pyrrole, diazole, triazole, thiazole, thiadiazole, oxadiazole, benzimidazole demonstrate a wide diversity of biological properties. Thiazoles are commonly reported as active antimicrobial [1][2][3][4][5][6][7][8], anti-tuberculous [9][10][11][12], anti-HIV [13], antiviral [14,15], antihistamine [16,17], antipyretic [18], antitumor [3,19], antidepressant [20], fungicidal [21,22] property bearing compounds. 2-Aminothiazoles has found application in agriculture as herbicides and fungicides [23,24].…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Characterization and Bioassay of Novel Substituted 1-(3-(1,3-Thiazol-2-yl)phenyl)-5-oxopyrrolidines

Sapijanskaitė-Banevič

Šovkovaja

Vaickelionienė

et al. 2020

Molecules

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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 evaluated against Gram-positive strains of Staphylococcus aureus, Bacillus cereus, Listeria monocytogenes and Gram-negative Pseudomonas aeruginosa, Escherichia coli and Salmonella enterica enteritidis. The vast majority of compounds exhibited between twofold and 16-fold increased antibacterial effect against the test-cultures when compared with Oxytetracycline.

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Synthesis and antiviral activity of some new bis-1,3-thiazole derivatives

Cited by 101 publications

References 33 publications

Thiazoles and Thiazolidinones as COX/LOX Inhibitors

Thiazoles and Thiazolidinones as COX/LOX Inhibitors

Synthesis and Biological Evaluation of Thiazole Derivatives

Synthesis, Characterization and Bioassay of Novel Substituted 1-(3-(1,3-Thiazol-2-yl)phenyl)-5-oxopyrrolidines

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