الفهرس 
INTRODUCTIONOnly 14 pages are availabe for public view
 |  | from | 150 |  |  |
| | | from | 150 | | |
Abstract
A mixture of p-hydroxy acetophenone, benzaldehyde, ethyl cyano acetate, ammonium acetate and absolute ethanol was refluxed for 12 h, filtered, dried afforded 1 in 72% yield.
A mixture of 1, ethyl chloro acetate, dry acetone, anhydrous K2CO3 and dry DMF was refluxed together for 12 h, filtered, dried afforded 2 in 69% yield.
Reagent conditions:
(i)- ethyl chloro acetate/ dry DMF/ anhydrous K2CO3, refluxed for 12 h.
A mixture of 2 with hydrazine hydrate and absolute ethanol was refluxed for 12 h, filtered, dried afforded 3 in 65% yield.
Reagent conditions:
(i) Hydrazine hydrate/ abs. ethanol, refluxed for 12 h.
Reaction of the azide derivative 5 with appropriate amino acid methyl ester hydrochloride, ethyl acetate, triethyl amine was stirred at 0oC for 20 min, filtered, dried, afforded 6 in 52% yields, according to Reagent conditions:
(i) AcOH/ 1NHCl/ NaNO2/ stirring at -5oC.
(ii) –HCl.
(iii) Amino acid methyl ester hydrochloride/ ethyl acetate/ Et3N/ stirring at 0oC.
A mixture of 6 with hydrazine hydrate and absolute ethanol was refluxed for 12 h, filtered, dried afforded 7 in 51% yields, according to Reagent conditions:
(i) hydrazine hydrate/ abs.ethanol/ refluxed for 12 h.
A solution of appropriate amino acid methyl ester hydrochloride, ethyl
acetate, tri ethyl amine, was stirred together at 0oC for 20 min, the filtrate was added to the azide 8 the mixture was kept at -5oC for 12 h, filtered, dried, afforded 9 in 51% yields, according to Reagent conditions:
(i) AcOH/ 1NHCl/ NaNO2/ stirring at -5oC.
(ii) –HCl.
(iii) Amino acid methyl ester / ethyl acetate/ Et3N/ stirring at 0oC.
The results of the viral screening against HBV of the newly synthesized
compounds indicated that some compounds showed moderate viral replication inhibition and mild cytotoxicity.
Also, the results indicated generally that tested compounds did not show high activity against bacteria under test (Escherichia coli and Bacillus subtilis) while some compounds revealed high activity against fungi. All new compounds were active against the microorganisms.