Abstract:
The synthesis of the annelated fused heterocyclic derivatives is divided into two
headings: Such as; annelated substrate and annelating reagent. The annelating substrates
ortho-amino ester such as 2-amino-4,5-diphenylfuran-3-carboxylate (8), ethyl-5-amino-2-
methylpyrozolo-4-carboxylate (2) and ethyl-2-amino-4,5-dimethylthiophene-3_carboxy_
late (14) were prepared from bezoin (7), ethyl(ethoxy methylene)malonitrile (1) and
butanone (13) respectively by using Gewald method and annelating reagents such as 2-
methylthio-2-methyl thiozoline (5) and 2-methylthio-imidazoline (11) were synthesized
from ethanol amine (3) and ethylene diamine (9) respectively by using Jenson and
Hofmann procedure. The annelating substrates were used to synthesize 2,3-diphenylfurano-
6, 7-dihydroimidazo(3 ,4-d]pyrimidin-4-one (12), 2-methyl-6,7 -dihydropyrazoio
(3,4-d]thiozolo(l,2-d] pyrimi-din-4-one (6) and 2,3-dihydro-6,7-dimethyl-5H-thiazolo
(3,2-a]thieno(2,3-d]pyrimidin-5-one (15) by one step reaction in dry acetic acid. in vitro
antimicrobial activity of fused heterocyclic derivatives were evaluated. All these
synthesized products of the fused heterocyclic derivatives have been employed as test
chemicals for determining their antibacterial and antifungal activities against a number of
human and plant pathogens.
All the synthesized compounds dcmonstrated mild growth inhibition against antibiotic
susceptible standard and clinically isolated strains of gram-positive and gram-negative
bacteria as well as fungal pathogens.
