Synthesis, crystal structure, anti-HIV, and antiproliferative activity of new pyrazolylthiazole derivatives

Madni, Murtaza; Hameed, Shahid; Ahmed, Muhammad Naeem; Tahir, Muhammad Nawaz; Al‐Masoudi, Najim A.; Pannecouque, Christophe

doi:10.1007/s00044-017-1963-1

Cited by 35 publications

(13 citation statements)

References 38 publications

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“…Great concern has been recently focused on the development of heterocyclic compound bearing 1,3-thiazole ring system, which has been identified as a central structural element of several biologically active natural products such as thiamine vitamin B, and pharmacologically active substances in a large number of drugs as antibacterial, 1,2 antifungal, 3,4 antiviral, [5][6][7] anti-inflammatory, 8,9 anticancer, [10][11][12][13][14] anti-HIV, [15][16][17] anti-oxidant 18,19 and analgesic drugs. 20,21 Both classical and non-classical synthetic methods approaches were used to synthesize thiazole derivatives.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Anticancer Evaluations of Novel Thiazole Derivatives Derived from 4-Phenylthiazol-2-amine

Abdallah

Mohareb

Helal

et al. 2021

ACSi

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Many novel thiazole derivatives were designed and synthesized using 4-phenylthiazol-2-amine. The reactivity of the latter compound toward different chemical reagents was studied. The structure of the newly synthesized compounds was established based on elemental analysis and spectral data. Furthermore, twenty compounds of the synthesized systems were selected and evaluated in (μM) as significant anticancer agents towards three human cancer cell lines [MCF-7 (breast adenocarcinoma), NCI-H460 (non-small cell lung cancer), and SF-268 (CNS cancer)] and normal fibroblasts human cell line (WI-38). The results showed that compounds 9 and 14a displayed higher effeciency than the reference doxorubicin.

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Section: Introductionmentioning

confidence: 99%

Synthesis and Anticancer Evaluations of Novel Thiazole Derivatives Derived from 4-Phenylthiazol-2-amine

Abdallah

Mohareb

Helal

et al. 2021

ACSi

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“…Owing to numerous pharmacological and biological applications thiazole derivatives have gained tremendous attention in the scientific community. Thiazole is reported in literature as antibacterial, 1 antiviral, 2 anti-inflammatory, 3 antifungal, 4 antitubercular, 5 antitumoral, 6 anti-HIV 7 and antioxidant agent. 8 Moreover, numerous marketed drugs possess thiazole scaffold as an active group.…”

Section: Introductionmentioning

confidence: 99%

Recurrent π–π stacking motifs in three new 4,5-dihydropyrazolyl–thiazole–coumarin hybrids: X-ray characterization, Hirshfeld surface analysis and DFT calculations

et al. 2020

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The synthesis and X-ray characterization of three new 4,5-dihydropyrazolylthiazole-coumarin hybrids (1-3) are reported herein, namely 3-(2-(3,5-bis(4-chlorophenyl)-4,5-dihydropyrazol-1-yl)thiazol-4-yl)-2H-chromen-2-one (1), 3-(2-(5-(4-chlorophenyl)-4,5-dihydro-3-phenylpyrazol-1-yl)thiazol-4-yl)-2H-chromen-2-one (2) and 3-(2-(3-(4-Chlorophenyl)-4,5-dihydro-5-p-tolylpyrazol-1-yl)thiazol-4-yl)-2H-chromen-2-one (3). A detailed structural analysis of the noncovalent interactions...

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“…[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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Synthesis, crystal structure, anti-HIV, and antiproliferative activity of new pyrazolylthiazole derivatives

Cited by 35 publications

References 38 publications

Synthesis and Anticancer Evaluations of Novel Thiazole Derivatives Derived from 4-Phenylthiazol-2-amine

Synthesis and Anticancer Evaluations of Novel Thiazole Derivatives Derived from 4-Phenylthiazol-2-amine

Recurrent π–π stacking motifs in three new 4,5-dihydropyrazolyl–thiazole–coumarin hybrids: X-ray characterization, Hirshfeld surface analysis and DFT calculations

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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