Green synthesis and evaluation of the antitumor activity of a novel series of 3-[4-bi-(4-fluorophenyl)methylpiperazinyl]-4-amino-5-thione-1,2,4-triazole Schiff bases

Ding, Yong; Zhang, Zhen; Zhang, Gang; Mo, Song; Li, Qinghan; Zhao, Zhigang

doi:10.1007/s11164-015-2200-5

Cited by 12 publications

(4 citation statements)

References 28 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…However, in case of refluxing of 4 H -1,2,4-triazole-3-thiol ( 268 ) with chloroacetic acid and different aldehydes or isatin derivatives in acidic media, various 5-substituted arylidene-thiazolotriazoles 269a – e in 49–68% yields or ( Z )-5-(1-acetyl-2-oxo-1 H -indol-3(2 H ,3 aH ,7 aH )-ylidene)thiazolo[3,2- b ]-1,2,4-triazol-6(5 H )-ones 270 were efficiently synthesized in 40% yield ( Scheme 78 ) [ 101 ]. Screening of the obtained compounds for anticancer activity revealed that 5-arylidene-[1,3]thiazolo[3,2- b ][1,2,4]triazol-6-ones 269a – e exhibited more potent anticancer activity than respective amides [ 101 ].…”

Section: Reactions Of 124-triazolethionesmentioning

confidence: 99%

Chemistry and Biological Activities of 1,2,4-Triazolethiones—Antiviral and Anti-Infective Drugs

et al. 2020

View full text Add to dashboard Cite

Mercapto-substituted 1,2,4-triazoles are very interesting compounds as they play an important role in chemopreventive and chemotherapeutic effects on cancer. In recent decades, literature has been enriched with sulfur- and nitrogen-containing heterocycles which are used as a basic nucleus of different heterocyclic compounds with various biological applications in medicine and also occupy a huge part of natural products. Therefore, we shed, herein, more light on the synthesis of this interesting class and its application as a biologically active moiety. They might also be suitable as antiviral and anti-infective drugs.

show abstract

Section: Reactions Of 124-triazolethionesmentioning

confidence: 99%

Chemistry and Biological Activities of 1,2,4-Triazolethiones—Antiviral and Anti-Infective Drugs

et al. 2020

View full text Add to dashboard Cite

show abstract

“…A high probability of finding a pharmacologically valuable substances among 1,2,4-triazoles and the broad possibilities for their chemical modifications are a solid foundation for the search for new synthetic drugs among them [5,6]. Compounds containing 1,2,4-triazole moiety have been demonstrated to have antimicrobial, antitumor, analgesic, hypolipidemic, neuroleptic and other kinds of activities [7][8][9][10][11][12]. Hence, the synthesis of new highly effective antimicrobial medicines containing this heterocyclic fragment is a promising branch in pharmaceutical chemistry investigations.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and antimicrobial activity of s-substituted derivatives of 1,2,4-triazol-3-thiol

Karpun

Поліщук

2021

SR: PS

View full text Add to dashboard Cite

The aim of the work. 1,2,4-triazole derivatives possess a wide range of pharmacological activity, so they are used for the development of drugs and active pharmaceutical ingredients. Due to the reactivity of 1,2,4-triazoles there are many options for their further structural modification on different reaction centers. Therefore, the aim of the work was to obtain new S-substituted derivatives of 1,2,4-triazole-3-thiols, study physicochemical parameters of the substances synthesized, evaluate the antimicrobial activity of new S-derivatives of the 4-R1-5-((3-(pyridin-4-yl)-1H-1,2,4-triazol-5-yl)thio)methyl)-4H-1,2,4-triazole-3-thiol series, and study some regularities of the “structure – biological activity” relationship for the synthesized compounds as well. Materials and methods. The subject of the study was new S-substituted 1,2,4-triazoles containing 2-oxopropan-1-yl and 2-aryl-2-oxoethan-1-yl substituents. The antimicrobial activity was studied by double serial dilutions on test cultures of Staphylococcus aureus (ATCC 25923), Escherichia coli (ATCC 25922), Pseudomonas aeruginosa (ATCC 27853), and Candida albicans (ATCC 885-653). The results of the biological screening showed that at a concentration of 125 g/mL, all synthesized substances showed activity (MIC – in the range of 31.25 - 62.5 μg/mL, MBCK - in the range of 62.5–125 μg/mL) against strains of Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa, Candida albicans. Variation of substituents on the sulfur atom did not lead to a significant change in antimicrobial and antifungal activities among derivatives of 4-R1-5-((3-(pyridin-4-yl)-1H-1,2,4-triazole-5-yl) thio)methyl)-4H-1,2,4-triazole-3-thiols. Conclusions. Biological screening data indicate the prospects for the search for new antimicrobial substances among the abovementioned derivatives of 1,2,4-triazoles. The most active compounds were 1-((4-ethyl-5-((3-(pyridin-4-yl)-1H-1,2,4-triazol-5-yl)thio)methyl)-4H-1,2,4-triazol-3-yl)thio)propan-2-one and 1-(4-methoxyphenyl)-2-(4-ethyl-5-(((3-(pyridin-4-yl)-1H)-1,2,4-triazol-5-yl)thio)methyl)-4H-1,2,4-triazol-3-yl)thio)ethanone, which showed the most pronounced antimicrobial activity against the Pseudomonas aeruginosa strain (MIC – 31.25 μg/mL, MBcK - 62.5 μg/mL)

show abstract

“…Протисудомна активність. Дослідниками [32] розглянуто регресійний аналіз, в якому як залежна змінна було виявлено протисудомну активність та обчислено дескриптори. Це дало моделі QSAR, точність та надійність, яка підтвердженна статистичними тестами.…”

unclassified

Biological activity of the derivatives of 1,2,4-triazole

Kravchenko

Панасенко

Knysh

2018

Farm Zh

View full text Add to dashboard Cite

The rapid development of modern medicine and pharmacy leads to an increase in synthetic drugs. Thus, in the professional literature says that one of the perspective directions are searching for new biologically active compounds including heterocyclic systems and the introduction of the latest in medical, pharmaceutical or veterinary practice. It is known that heterocyclic ring system 1,2,4-triazole moiety is promising for the synthesis of new active ingredients with various kinds of pharmacological actions. The aim of the study was the analysis of literature and patent sources over the past 10 years and the generalization of the results for certain types of biological activity of 1,2,4-triazole. Results of literary analysis show a wide range of biological activity of 1,2,4-triazole-3-tion. The data determine the relevance of further research of derivatives of 1,2,4-triazole in the actoprotective, antimicrobial, antifungal, antihypoxic, hypoglycemic, analgesic, antiinflammatory and others activity in order to find new highly effective in terms of biological substances that can form the basis of new medicines.

show abstract

Green synthesis and evaluation of the antitumor activity of a novel series of 3-[4-bi-(4-fluorophenyl)methylpiperazinyl]-4-amino-5-thione-1,2,4-triazole Schiff bases

Cited by 12 publications

References 28 publications

Chemistry and Biological Activities of 1,2,4-Triazolethiones—Antiviral and Anti-Infective Drugs

Chemistry and Biological Activities of 1,2,4-Triazolethiones—Antiviral and Anti-Infective Drugs

Synthesis and antimicrobial activity of s-substituted derivatives of 1,2,4-triazol-3-thiol

Biological activity of the derivatives of 1,2,4-triazole

Contact Info

Product

Resources

About