Next Article in Journal
A Facile One-Pot Process for the Formation of Hindered Tertiary Amines
Previous Article in Journal
Comparison of the Simple Cyclic Voltammetry (CV) and DPPH Assays for the Determination of Antioxidant Capacity of Active Principles
Open AccessArticle

Synthesis and Bioactivity of Pyrazole Acyl Thiourea Derivatives

State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agriculture Bioengineering, Ministry of Education, Guizhou University, Guiyang 550025, China
Author to whom correspondence should be addressed.
These authors contributed equally to this work.
Molecules 2012, 17(5), 5139-5150;
Received: 11 April 2012 / Revised: 19 April 2012 / Accepted: 19 April 2012 / Published: 3 May 2012
Sixteen novel pyrazole acyl thiourea derivatives 6 were synthesized from monomethylhydrazine (phenylhydrazine) and ethyl acetoacetate. The key 5-chloro-3-methyl-1-substituted-1H-pyrazole-4-carbonyl chloride intermediates 4 were first generated in four steps through cyclization, formylation, oxidation and acylation. Thess were then reacted with ammonium thiocyanate in the presence of PEG-400 to afford 5-chloro-3-methyl-1-substituted-1H-pyrazole-4-carbonyl isothiocyanates 5. Subsequent reaction with fluorinated aromatic amines resulted in the formation of the title compounds. The synthesized compound were unequivocally characterized by IR, 1H-NMR, 13C-NMR and elemental analysis and some of the synthesized compounds displayed good antifungal activities against Gibberella zeae, Fusarium oxysporum, Cytospora mandshurica and anti-TMV activity in preliminary antifungal activity tests. View Full-Text
Keywords: pyrazole acyl thiourea derivatives; synthesis; antifungal activity; antiviral activity pyrazole acyl thiourea derivatives; synthesis; antifungal activity; antiviral activity
Show Figures

Figure 1

MDPI and ACS Style

Wu, J.; Shi, Q.; Chen, Z.; He, M.; Jin, L.; Hu, D. Synthesis and Bioactivity of Pyrazole Acyl Thiourea Derivatives. Molecules 2012, 17, 5139-5150.

Show more citation formats Show less citations formats

Article Access Map by Country/Region

Only visits after 24 November 2015 are recorded.
Back to TopTop