Synthesis and Biological Activity of Natural Thiazoles: An Important Class of Heterocyclic Compounds

Souza, Michele Souza e

doi:10.1002/chin.200725233

Cited by 10 publications

(12 citation statements)

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“…It is well established that compounds that contain sulfur atoms play a significant role in living organisms [ 18 , 19 ]. 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 ].…”

Section: Introductionmentioning

confidence: 99%

“…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%

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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%

Section: Introductionmentioning

confidence: 99%

Thiazoles and Thiazolidinones as COX/LOX Inhibitors

2018

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“…On the other hand, the nitrogen and sulfur heterocyclic system families are very interesting due to their physicochemical properties, especially in the sense of design of new drugs and new materials. The chemistry and pharmacology of thiazole derivatives has been of great interest to medicinal chemists lately [ 13 ]. The pyrazole ring is a prominent structural moiety found in numerous pharmacologically active compounds.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Antimicrobial Activity of New 4-Heteroarylamino Coumarin Derivatives Containing Nitrogen and Sulfur as Heteroatoms

Dekić¹,

Radulović

Dekić³

et al. 2010

Molecules

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ynthesis, spectral analysis and bioactivity of new coumarin derivatives are described in this paper. Eight new coumarin derivatives were synthesized in moderate to good yields by condensation of 4-chloro-3-nitrocoumarin and the corresponding heteroarylamine. The synthesized compounds were tested for their in vitro antimicrobial activity, in a standard disk diffusion assay, against thirteen strains of bacteria and three fungal strains. They have shown a wide range of activity - from one completely inactive compound to medium active ones.

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“…Thiazole is a five-membered azole heterocyclic organic compound containing a ring of 3 carbon atoms, a nitrogen and a sulphur (Taha et al, 2016). Thiazole and its derivatives have wide industrial application in pharmacy, liquid crystals, and polymers (de Souza, 2005). Thiazoles have several biological activities such as antioxidant, insecticidal, antitumor, anticonvulsant, anti-hyperlipidemic and antiinflammatory (Khan et al, 2016) Computer-aided drug design (CADD) is a unique area in drug discovery arena which apply the concept of molecular modelling to study the interaction between drugs and their target protein (Bibi and Sakata, 2016).…”

Section: Introductionmentioning

confidence: 99%

QSAR modelling and docking analysis of some thiazole analogues as alfa-glucosidase inhibitors

2019

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QSAR modelling and docking studies on 45 thiazole analogues were carried out. The studied compounds in this research were optimized adopting DFT method at B3LYP function with a 6-31G* basis set. The QSAR models were generated in material studio by MLR analysis (GFA method). Based on its statistical fitness, the first model was selected and reported as the best model and assessed with R 2 = 0.906134, R 2 adj = 0.89049, Q 2 cv = 0.86149 and R 2 pred = 0.82581 statistical parameters. The ligand with the highest binding energy of-11.0 kcal/mol among the other ligands was ligand 13 as indicated by the molecular docking. The standard drug (acarbose) was also docked to the binding pocket of ⍺-glucosidase with-9.5kcal/mole docking score. The most active compound was found to be better than standard drug. The outcome of this findings paved way for predicting novel ⍺-glucosidase inhibitors having improved potency toward their target enzyme.

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Synthesis and Biological Activity of Natural Thiazoles: An Important Class of Heterocyclic Compounds

Abstract: ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.

Cited by 10 publications

References 1 publication

Thiazoles and Thiazolidinones as COX/LOX Inhibitors

Thiazoles and Thiazolidinones as COX/LOX Inhibitors

Synthesis and Antimicrobial Activity of New 4-Heteroarylamino Coumarin Derivatives Containing Nitrogen and Sulfur as Heteroatoms

QSAR modelling and docking analysis of some thiazole analogues as alfa-glucosidase inhibitors

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