- Facile synthesis of novel bis-derivatives of 2,5-diamino-thiadiazole/N,N′-thiocarbohydrazide and their biological perspective
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A series of new bis derivatives of 2,5-thiadiazole and N,N′-thiocarbohydrazide along with their transition metal complexes were synthesized by green methods (sonochemical and microwave), i.e., energy and time efficient and operationally more simple than existing conventional methods. All the synthesized compounds were fully characterized by routine analytical techniques and subjected to a preliminary biological screening. These novel characterized compounds were screened for antimicrobial activities and showed promising results. A few potent compounds were also tested for antitumor activities against MDA-MB231 (human breast carcinoma cell line) and compound 5 has emerged as a potential antitumor compound followed by compound 2, 10 and 9, with IC50 values of 29.48, 32.25, 32.34 and 34.34?μg/ml, respectively. To understand the binding interactions of these compounds, in silico studies were performed using the AUTODOCK 4.2 suite and found to be supportive of the experimental results.
- Bhatt, Priyanka,Sreekanth,Jha, Anjali
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- Synthesis and antimicrobical evaluation of a novel class of 1,3,4-thiadiazole: Derivatives bearing 1,2,4-triazolo[1,5-a]pyrimidine moiety
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A series of novel 1,3,4-thiadiazole derivatives bearing 1,2,4-triazolo[1,5-a]pyrimidine moiety were synthesized by the method of splicing active substructures. Among these derivatives, compounds 12, 13, 15-22 and 24-31 were firstly reported. All the compounds were assayed for antimicrobial activities against five fungi strains and four bacteria strains. The preliminary results indicated that compounds 25 and 28-31 showed good antifungal activities against Physaclospora piricola and Rhizoctonia solani. Compound 26 exhibited good antifungal activities against Cercospora beticola and R. solani. Most of the compounds showed better antibacterial activities against Gram-negative bacteria strains than Gram-positive bacteria strains. Compounds 25 and 28 showed the best activities against Pseudomonas fluorescence while compounds 30-31 showed good activities against Escherichia coli.
- Luo, Yin,Zhang, Shuai,Liu, Zhi-Jun,Chen, Wu,Fu, Jie,Zeng, Qing-Fu,Zhu, Hai-Liang
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- Synthesis and antifungal evaluation of 1,2,4-triazolo[1,5-α] pyrimidine bearing 1,2,4-triazole heterocycle derivatives
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In order to search novel fungicides with higher activity, 28 new 1,2,4-triazolo[1,5-α]pyrimidine derivatives bearing 1,2,4-triazole heterocycle were synthesized. Their structures were characterized by 1H NMR spectroscopy, mass spectrometry and elemental analyses. With triadimefon, validamycin and carbendazim as positive controls, the antifungal activities of 28 compounds against Fusarium oxysporum f. sp. vasinfectum, Gibberella sanbinetti, Cercospora beticola Sacc., Physaclospora piricola and Rhizoctonia solani were evaluated. Compound 2-[(5-(2,6- difluorobenzylthio)-4- phenyl-4H-1,2,4-triazol-3-yl)methylthio]-5,7-dimethyl[1,2,4]triazolo[1, 5-α]pyrimidine (19) showed potent antifungal activities against G. sanbinetti, C. beticola, P. piricola and R. solani. On the basis of the biological results, structure-activity relationships of these compounds were also discussed.
- Chen,Xiang,Fu,Zeng,Zhu
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scheme or table
p. 602 - 608
(2012/01/02)
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- [5,5] sigmatropic shift of N-phenyl-N'-(2-thiazolyl)hydrazines and N,N'- bis(2-thiazolyl)hydrazines into 2-amino-5-(p-aminophenyl)thiazoles and 5,5'- bis(2-aminothiazole) derivatives
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[5,5] Sigmatropic shift of N-phenyl-N'-(2-thiazolyl)hydrazines and N,N'- bis(2-thiazolyl)hydrazines in acid-catalyzed benzidine-type rearrangement into 2-amino-5-(p-aminophenyl)thiazoles and 5,5'-bis(2-aminothiazole) derivatives is described, respectively. (C) 2000 Elsevier Science Ltd.
- Lee, Boong Won,Lee, Seung Dal
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p. 3883 - 3886
(2007/10/03)
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- PRODUCTS FROM REACTION OF BENZALDEHYDE THIOSEMICARBAZONE WITH POTASSIUM ETHOXIDE
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When heated with potassium ethoxide, benzaldehyde thiosemicarbazone gives a mixture of 2,4,5-triphenylimidazole, hydrazodithioformamide, benzoic acid, and benzaldehyde oxime.It was shown that these compounds are formed through the intermediate benzaldehyde azine and benzonitrile.
- Marshalkin, M. F.,Yakhontov, L. N.
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p. 2273 - 2276
(2007/10/02)
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