Studies of antimicrobial activities of some 4-thiazolidinone fused pyrimidines, [1,5]-benzodiazepines and their oxygen substituted hydroxylamine derivatives

Abstract

Thiazolidin-4-one fused pyrimidines, [1,5]-benzodiazepines and their oxygen substituted hydroxylamine derivatives have been screened for antibacterial, antifungal and antimalarial activity. Bacillus subtilis, Escherichia coli, Proteus mirabilis and Salmonella typhi were used for antibacterial screening. Aspergillus fumigatus and Candida albicans were used for antifungal screening and Plasmodium species were used for antimalarial screening. The antibacterial and antifungal activities are expressed in terms of zone of inhibition and antimalarial activity is expressed in IC50 value. Fifteen compounds 2Xa, 2Xb, 2Xc, 2Xs, 3IV, 3Va, 3Vc, 3VIIIa, 3VIIIh, 3IXa, 3IXb, 3IXc, 3Xa, 4IXa and 4Xa were tested for antibacterial as well as antifungal activity and seven compounds 2IXb, 2Xb, 3VIIIc, 3Xc, 4IXa, 4Xa and 4IXw were tested for antimalarial activity. Streptomycin, griseofulvin and chloroquine were taken as standard drugs in antibacterial, antifungal and antimalarial activity, respectively. The compound 2Xs was found significant antimicrobial against Bacillus subtilis, E. coli, Aspergillus fumigatus and Candida albicans as well as compound 3Xa was significant antimicrobial against Bacillus subtilis, E. coli, Salmonella typhi, Aspergillus fumigatus and Candida albicans. The compound 2Xb showed significant antimalarial activity.

Pyrimidine-fused heterocycle derivatives as a novel class of inhibitors for α-glucosidase

“…The needs for diverse inhibitors of α-Gls promote the search for novel classes of these molecules. As reported recently, pyrimidine-fused heterocyclic (PFH) compounds display various biological activities including anticancer activity, 11 antiviral activity, 12 antimicrobial activity, 13 antiinflammatory properties, antioxidant effects, and tyrosine kinase inhibitory activity.…”

“…This strategy offers a powerful tool for preparing a new pyrimidine scaffold which has high potential for application in medicinal chemistry. The synthetic compounds were also characterized using different spectroscopic techniques such as 1 H-NMR, 13 C NMR, infrared (IR) and mass spectroscopies. The data clearly revealed that these molecules were produced successfully.…”

Synthesis and Antibacterial Activity of Thienopyrimidine Amide Derivatives

“…This scaffold shows a broad spectrum of biological activities. The thienopyrimidines were assessed as antitumour [6][7][8][9], medicine [10], enzyme [11][12][13][14], phosphodiesterase inhibitors [15], antioxidative [16,17], antimalarial drug [18,19], antibacterial drug [20], antiviral [21], antifungal [22,23], medication [24], antiplatelet [25] and medicament [26]. In view of these observations, the varied biological property of thienopyrimidine pharmacophore impelled to synthesize the title compounds.…”

Syntheses, spectroscopic and magnetic properties of polystyrene-anchored coordination compounds of thiazolidinone

“…They show broad spectrum of biological activities due to their ready accessibility and diverse chemical reactivity [12,13]. They are involved in variety of applications such as antimicrobial, antibacterial, anticonvulsant, antifungal, anti-HIV, antiproliferative, anti-inflammatory, cystic fibrosis and antithyroid [14], etc.…”