Synthesis of azole and pyrimidine derivatves and it's effect on some dermatophytes. +CD

number: 
1704
English
department: 
Degree: 
Imprint: 
Chemistry
Author: 
Firas Abdulla Hassan
Supervisor: 
Dr.Salman Ali Ahmed
year: 
2007

Abstract:

Chemotherapy is the science of selective toxicity. The goal of chemotherapeutic treatement is to selectively attenuate or destrory pathogenic microorganisms or cells with minimal side effects to the host . These target cells or organisms may be bacteria , viruses , fungi , or tumor cells . In this work new derivatives of azole and pyrimidine compounds have been synthesized , which contain imidazole compound with a five membered ring containing two nitrogen which is pharmacologically active against dermatophyte diseases . 1-acetyl -4- [4-[[2,4-dicholorphenyl] -2-(1H -imidazole -1-yl -methyl)-1,3-dioxolan -4-yl]methoxy ]phenyl] piperazine (1G) was synthesized by treating of [2-(2,4-dicholorphenyl] -2-(1H -imidazole -1-yl -methyl)-1,3-dioxolan -4-yl]methoxy methanesulfonate with piperazine dervatives. Ethyl -4- aminobenzoate (2a) was synthesized by condensation reaction of -4- amino benzoic acid with HCl saturated ethanol . 2- thioacetic -5- (4-amino phenyl)1,3,4-oxadiazole (2E) was synthesized by treating compound 2-mercapto-5-(4-aminophenyl) 1,3,4-oxadiazole with chloroacetic acid . 1- methyl -4- oxo-1,2,3,4,-tetrahydro-2- thiopyrimidine (4G) was synthesized by reacting of (0.1mole) thiouria with (0.1mole) of ethylacetoacetate . 2- hydrazine -6- methyl pyrimidine -4- (3H) one (5G) was synthesized by reacting the hydrazine hydrate with compound (4G). The purity of the compounds were characterized by using fourier transform infrared spectroscopy (FTIR) . The effects of New compounds (1G,2E,6G,4G and 5G) one the activity of growth the fungal colonies were studied the effect of these compounds by using the tissue culture of fungi in the treatment of dermatophyte that found depend on the incubation time 48 hrs ., 72hrs ., and 96hrs . The invitro study was used the Trichophyton rubrum and geotrichum candidum ,and used sabouraud agar and potato dextrose as culture . Mixture of Ketoconazole compound with caffeine (6G) showed the highest inhibitory effect on the growth of fungi compared with ketoconazle (1G) alone , the least effective compound was (5G) after 72 hrs . of incubation and compound (4G) didnt inhibit the growth of fungal colonies at different concentration . Compound (2E) was highly active against fungal colonies after 48hrs ., 72hrs.,and 96hrs .of incubations .