Synthesis and antifungal activity of novel sulfoxide derivatives containing trimethoxyphenyl substituted 1,3,4-thiadiazole and 1,3,4-oxadiazole moiety

Liu, Fang; Luo, X.J.; Song, Baoan; Bhadury, Pinaki S.; Yang, Song; Jin, Linhong; Xue, Wei; Hu, Deyu

doi:10.1016/j.bmc.2008.02.006

Cited by 153 publications

(69 citation statements)

References 18 publications

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“…The structures of the synthesized compounds were assigned from studying their spectral data, such as IR, 1 H NMR, Mass spectra, as well as elemental analysis [1,2,8].…”

Section: Chemistrymentioning

confidence: 99%

“…The synthesis of novel quinazolin derivatives and investigation of their chemical and antimicrobial behavior has gained more importance in recent decades for biological, medicinal and agricultural reasons [5][6][7][8][9]. Quinazolinone nucleus has been gaining prominence due to the fact that its derivatives have been found to possess wide spectrum of pharmacological properties.…”

Section: Introductionmentioning

confidence: 99%

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Synthesis and antimicrobial evaluation of some new quinazolin-4(3H)-one derivatives

2012

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“…The structures of the synthesized compounds were assigned from studying their spectral data, such as IR, 1 H NMR, Mass spectra, as well as elemental analysis [1,2,8].…”

Section: Chemistrymentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Synthesis and antimicrobial evaluation of some new quinazolin-4(3H)-one derivatives

2012

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“…1,3,4-Oxadiazoles forms an important class of heterocyclic compounds with broad spectrum of biological activities. Substituted 1,3,4-oxadiazoles have revealed antibacterial 21 , antimycobacterial 22 , antifungal 23 , anti-inflammatory and analgesic [24][25][26] , anticonvulsant 27 , antihyperglycemic 28 , anticancer 29 , anti-HIV-1 30 , and tyrosinase inhibitory activity 31 . 1,2,4-Oxadiazole derivatives have been reported as potent anti-inflammatory agents with selectivity for COX-2 [32][33][34] .…”

Section: Research Articlementioning

confidence: 99%

Synthesis and biological evaluation of 2,5-disubstituted 1,3,4-oxadiazole derivatives with both COX and LOX inhibitory activity

Akhter

Alam

et al. 2011

Journal of Enzyme Inhibition and Medicinal Chemistry

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“…Heterocyclic nucleus 1,3,4-thiadiazole constitutes an important class of compounds for new drug development because of its interesting biological properties such as anticancer [5], antibacterial [6] and antifungal activity [7]. Especially, the structure of ''N-C-S'' in 1,3,4-thiadiazole derivatives can work as the active center, chelate certain metal ions in vivo, and show good tissue permeability..…”

Section: Introductionmentioning

confidence: 99%

<strong>Microwave-assisted Facile Synthesis And Anticancer Evaluation Of N-((5-(substituted Methylene Amino)- 1,3,4-thiadiazol-2-yl)methyl) Benzamide Derivatives</strong>

Nikalje¹,

Tiwari²,

Siddiqui³

et al. 2016

Proceedings of the 20th International Electronic Conference on Synthetic Organic Chemistry

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Microwave induced synthesis has various advantages over conventional synthesis, such as highly accelerated reaction rate , reasonable better yields, simple open systems, no solvent or very less amount of solvents required, eco friendly method, clean heating system and control on reaction parameters .In the present work novel Schiff's bases containing thiadiazole scaffold and benzamide group, through appropriate pharmacophore were designed and synthesized , because of the important biological properties associated with these three moieties/groups. The coupling of these important moieties was achieved under microwave The same compounds were also synthesized using conventional approach. The conventional method required 15-18 hrs, while microwave irradiation method required only 15-20 minutes and gave better yields. Total 12 final compounds were synthesized as per the scheme reported. Structures of synthesized compounds were confirmed by IR, NMR, and Mass spectral study. All the designed hybrids were evaluated for their in vitro anticancer activity against a panel of four human cancer cell lines viz SK-MEL-2(melanoma), HL-60 (leukemia), HeLa (cervical) and MCF-7(breast) using MTT assays method. Most of the synthesized compounds exhibited promising anticancer activity with the some compounds having GI 50 values similar to that of the Adriamycin. The compounds 7k, 7l, 7b, and 7a were found to be the most promising in this study. A computational study of synthesized compounds 7(a-l) was performed for prediction of ADMET. The absorption, distribution, metabolism, excretion and Toxicity (ADMET) properties of all compounds were predicted using Qikprop v3.5 (Schrödinger LLC).

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Synthesis and antifungal activity of novel sulfoxide derivatives containing trimethoxyphenyl substituted 1,3,4-thiadiazole and 1,3,4-oxadiazole moiety

Cited by 153 publications

References 18 publications

Synthesis and antimicrobial evaluation of some new quinazolin-4(3H)-one derivatives

Synthesis and antimicrobial evaluation of some new quinazolin-4(3H)-one derivatives

Synthesis and biological evaluation of 2,5-disubstituted 1,3,4-oxadiazole derivatives with both COX and LOX inhibitory activity

<strong>Microwave-assisted Facile Synthesis And Anticancer Evaluation Of N-((5-(substituted Methylene Amino)- 1,3,4-thiadiazol-2-yl)methyl) Benzamide Derivatives</strong>

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