2,4-Disubstituted thiazoles as multitargated bioactive molecules

Arora, Preeti; Narang, Rakesh; Nayak, Satheesha B; Singh, Sachin Kumar; Judge, Vikramjeet

doi:10.1007/s00044-016-1610-2

Cited by 50 publications

(21 citation statements)

References 141 publications

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“…The biological activity of compounds containing thiazole is almost infinite, they are antineoplastic 188, 189, antibiotic 190, anti-inflammatory agents 191,192,antiulcer 192,193,antimicrobial 195, antifungal drugs 196 and many more. [70] Most biologically active thiazole-containing compounds have substitutions at positions 2 and 4 or one of them. It was found that these substitutes give the compounds different biological properties depending on the difference of the substitutes themselves.…”

Section: Biological Activitiesmentioning

confidence: 99%

Review of the synthesis and biological activity of thiazoles

Ali

Sayed

2020

Synthetic Communications

117

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Section: Biological Activitiesmentioning

confidence: 99%

Review of the synthesis and biological activity of thiazoles

Ali

Sayed

2020

Synthetic Communications

117

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“…A large variety of thiazole‐based and pyrazole‐based compounds have been extensively exploited and applied in pharmaceutical products in relation to their large spectrum of biological activities: antibacterial, antifungal, anti‐inflammatory, antitumour, antitubercular, antidiabetic, antiviral or antioxidant.…”

Section: Introductionmentioning

confidence: 99%

Organoselenium compounds containing pyrazole or phenylthiazole groups: Synthesis, structure, tin(IV) complexes and antiproliferative activity

Popa

Licărete

Banciu

et al. 2018

Applied Organom Chemis

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The diorganodiselenides (pzCH 2 CH 2 ) 2 Se 2 (1) and (PhtzCH 2 ) 2 Se 2 (2) were prepared by reacting Na 2 Se 2 with 1-(2-bromoethyl)-1H-pyrazole and 4-(chloromethyl)-2-phenylthiazole, respectively, while the reactions between 1-(2-bromoethyl)-1H-pyrazole or 4-(chloromethyl)-2-phenylthiazole and the lithium organoselenolates [2-(Et 2 NCH 2 )C 6 H 4 ]SeLi and [2-{O(CH 2 CH 2 ) 2 NCH 2 } C 6 H 4 ]SeLi in a 1:1 molar ratio resulted in the heteroleptic diorganoselenium(II) compounds [2-(Et 2 NCH 2 )C 6 H 4 ](R)Se (R = pzCH 2 CH 2 (3) or PhtzCH 2 (5)) and [2-{O(CH 2 CH 2 ) 2 NCH 2 }C 6 H 4 ](R)Se (R = pzCH 2 CH 2 (4) or PhtzCH 2 (6)). The diorganotin(IV) bis(organoselenolato) derivatives of type R 2 Sn(SeCH 2 CH 2 pz) 2 (R = 2-(Me 2 NCH 2 )C 6 H 4 (7) or Me (8)) were obtained by reacting (pzCH 2 CH 2 ) SeNa with the appropriate diorganotin(IV)dichloride in a 2:1 molar ratio. All compounds were investigated using NMR spectroscopy ( 1 H, 13 C, 77 Se, 119 Sn as appropriate) and ESI+ mass spectrometry. The molecular structures of 2 and 6 were determined using single-crystal X-ray diffraction. The formation of a 10-Se-3 hypercoordinated species was evidenced for 6 in the solid state, as a consequence of the C,N coordination behaviour of the 2-{O(CH 2 CH 2 ) 2 NCH 2 } C 6 H 4 group. Compounds 1, 7 and 8 were investigated for their antiproliferative activity towards the mouse colon carcinoma C26 cell line with the preliminary results showing a better activity than 5-fluorouracil.

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“…Thiazole derivatives containing nitrogen and sulphur atoms are among the most important pharmacophore groups in drug research studies 1 and it is known that many drugs [1][2][3] and natural products 4 such as Abafungin, Famotidin, Meloxicam and Ritonavir contain a thiazole ring in their structures. [1][2][3][4] Thiazoles are present in a wide range of pharmacologically active compounds exhibiting antibacterial, [5][6][7][8] antimycobacterial, [9][10][11] antifungal, [5][6][7][8] anticancer [12][13][14] and antiviral 15,16 activity.…”

Section: Introductionmentioning

confidence: 99%

“…[1][2][3][4] Thiazoles are present in a wide range of pharmacologically active compounds exhibiting antibacterial, [5][6][7][8] antimycobacterial, [9][10][11] antifungal, [5][6][7][8] anticancer [12][13][14] and antiviral 15,16 activity. Furthermore, thiazole derivatives are useful as chemosensors 17 and fluorescent sensors.…”

Section: Introductionmentioning

confidence: 99%

Green synthesis of highly functionalized octahydropyrrolo[3,4-c]pyrrole derivatives using subcritical water, and their anti(myco)bacterial and antifungal activity

Nural¹,

Gemili²,

Yabalak³

et al. 2018

Arkivoc

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A series of novel 2-(thiazol-2-yl)-octahydropyrrolo [3,4-c]pyrroles was synthesized by reaction of octahydropyrrolo [3,4-c]pyrrole N-benzoylthiourea derivatives and α-haloketones in subcritical water at 130 °C in 75-91% yield. Both the thiourea intermediates and the end products were synthesized in subcritical water, which proved a suitable green alternative to acetone by delivering the desired compounds in much shorter reaction times and practically the same yields. The antimicrobial activity of the compounds was determined against five bacterial strains and three fungal strains, and MIC values of 15.62-250 g/mL were observed. Moreover, the compounds exhibited antimycobacterial activity against M. tuberculosis H37Rv with MIC values of 7.81-62.5 µg/mL.

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2,4-Disubstituted thiazoles as multitargated bioactive molecules

Cited by 50 publications

References 141 publications

Review of the synthesis and biological activity of thiazoles

Review of the synthesis and biological activity of thiazoles

Organoselenium compounds containing pyrazole or phenylthiazole groups: Synthesis, structure, tin(IV) complexes and antiproliferative activity

Green synthesis of highly functionalized octahydropyrrolo[3,4-c]pyrrole derivatives using subcritical water, and their anti(myco)bacterial and antifungal activity

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