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Simple method of preparation and characterization of new antifungal active biginelli type heterocyclic compounds.

Pothiraj C, Velan AS, Joseph J, Raman N - Mycobiology (2008)

Bottom Line: They were prepared from a reaction mixture consisting of substituted benzaldehydes, thiourea and ethylacetoacetate using ammonium dihydrogenphosphate as catalyst.The four new synthesised compounds were tested for their antifungal activity.They have good antifungal activity comparing to the standard (Fluconazole).

View Article: PubMed Central - PubMed

Affiliation: Department of Microbiology, VHNSN College, Virudhunagar-626 001, India.

ABSTRACT
A simple, efficient and cost effective method is described for the synthesis of Biginelli type heterocyclic compounds of dihydropyrimidinones analogous. They were prepared from a reaction mixture consisting of substituted benzaldehydes, thiourea and ethylacetoacetate using ammonium dihydrogenphosphate as catalyst. The procedure for the preparation of the compounds is environmentally benign and safe which is advantageous in terms of experimentation, catalyst reusability, yields of the products, shorter reaction times and preclusion of toxic solvents. The four new synthesised compounds were tested for their antifungal activity. They have good antifungal activity comparing to the standard (Fluconazole).

No MeSH data available.


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The Biginelli dihydropyrimidine synthesis.
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Figure 1: The Biginelli dihydropyrimidine synthesis.

Mentions: The most thoroughly studied ring system amongst the heterocyclic compounds is that of pyrimidine (Kappe, 1993, 2000; Raman et al., 2007). They serve as building units of many valuable chemotherapeutic agents (bleomycine), vitamins (vitamin B1), drugs (hyprotic, antibacterial, antimalarial) and nucleic acids (cytosine and uracil). In 1893, Italian chemist Pietro Biginelli reported on the acid-catalyzed cyclocondensation reaction of ethylacetoacetate (1), benzaldehyde (2) and urea (3). The reaction was carried out simply by heating a mixture of the three components dissolved in ethanol with a catalytic amount of HCl at reflux temperature. The product of this novel onepot, three-component synthesis that precipitated on cooling of the reaction mixture was identified correctly by Biginelli as 3,4-dihydropyrimidin-2(1H)-one (4) (Fig. 1), (Muniz and Juaristi, 2003).


Simple method of preparation and characterization of new antifungal active biginelli type heterocyclic compounds.

Pothiraj C, Velan AS, Joseph J, Raman N - Mycobiology (2008)

The Biginelli dihydropyrimidine synthesis.
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC3755255&req=5

Figure 1: The Biginelli dihydropyrimidine synthesis.
Mentions: The most thoroughly studied ring system amongst the heterocyclic compounds is that of pyrimidine (Kappe, 1993, 2000; Raman et al., 2007). They serve as building units of many valuable chemotherapeutic agents (bleomycine), vitamins (vitamin B1), drugs (hyprotic, antibacterial, antimalarial) and nucleic acids (cytosine and uracil). In 1893, Italian chemist Pietro Biginelli reported on the acid-catalyzed cyclocondensation reaction of ethylacetoacetate (1), benzaldehyde (2) and urea (3). The reaction was carried out simply by heating a mixture of the three components dissolved in ethanol with a catalytic amount of HCl at reflux temperature. The product of this novel onepot, three-component synthesis that precipitated on cooling of the reaction mixture was identified correctly by Biginelli as 3,4-dihydropyrimidin-2(1H)-one (4) (Fig. 1), (Muniz and Juaristi, 2003).

Bottom Line: They were prepared from a reaction mixture consisting of substituted benzaldehydes, thiourea and ethylacetoacetate using ammonium dihydrogenphosphate as catalyst.The four new synthesised compounds were tested for their antifungal activity.They have good antifungal activity comparing to the standard (Fluconazole).

View Article: PubMed Central - PubMed

Affiliation: Department of Microbiology, VHNSN College, Virudhunagar-626 001, India.

ABSTRACT
A simple, efficient and cost effective method is described for the synthesis of Biginelli type heterocyclic compounds of dihydropyrimidinones analogous. They were prepared from a reaction mixture consisting of substituted benzaldehydes, thiourea and ethylacetoacetate using ammonium dihydrogenphosphate as catalyst. The procedure for the preparation of the compounds is environmentally benign and safe which is advantageous in terms of experimentation, catalyst reusability, yields of the products, shorter reaction times and preclusion of toxic solvents. The four new synthesised compounds were tested for their antifungal activity. They have good antifungal activity comparing to the standard (Fluconazole).

No MeSH data available.


Related in: MedlinePlus