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Studies of Antimicrobial Activities of some 4-Thiazolidinone Fused Pyrimidines, [1,5]-Benzodiazepines and their Oxygen Substituted Hydroxylamine Derivatives.

Singh B, Maheshwari A, Dak G, Sharma K, Talesara GL - Indian J Pharm Sci (2010)

Bottom Line: 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.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.

View Article: PubMed Central - PubMed

Affiliation: Organic Research Laboratory, Department of Chemistry, Banasthali University, Banasthali-304 022, India.

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 IC(50) 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.

No MeSH data available.


Related in: MedlinePlus

General structure of compounds synthesized[19] 4IXa (X=H, Z=H), 4Xa (X=H, Z=H, n=2) and 4Xw (X=Cl, Z=OH, n=4)
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Figure 4: General structure of compounds synthesized[19] 4IXa (X=H, Z=H), 4Xa (X=H, Z=H, n=2) and 4Xw (X=Cl, Z=OH, n=4)

Mentions: Alkoxyphathalimide derivative of thiazolidinop-yrimidines were found to have significant antifungal, antibacterial and antimalarial activity. Activity was increased with introduction of chloro group at the para-position in arylimino moiety and with increasing of length of alkyl chain in alkoxyphthalimide group whereas it is decreased when hydroxyl group was introduced. Structures of compounds 2Xa, 2Xb, 2Xc and 2Xs are shown in fig. 1. The antibacterial and antifungal activities were increased when the arylidene unit was introduced in thiazolidinone nucleus at position-5 but activity was decreased when hydroxyl group was present at para-position in arylidene unit. Structures of the compounds are shown in figs. 2 and 3. Compounds 2Xs, 3Xa and 4Xa were found to exhibit significant antimicrobial activities. These results suggest that antimicrobial activities are strongly affected by the presence or absense of alkoxyphthalimide moiety and hence compound 3Xa and 4Xa showed significant activity than compounds 3IXa and 4IXa (comparison in figs. 3] and 4). Although [1,5]-benzodiazepines have strong antibacterial and antifungal activity but it was found to show slightly lower activity than alkoxyphthalimide derivatives of thiazolidinopyrimidines.


Studies of Antimicrobial Activities of some 4-Thiazolidinone Fused Pyrimidines, [1,5]-Benzodiazepines and their Oxygen Substituted Hydroxylamine Derivatives.

Singh B, Maheshwari A, Dak G, Sharma K, Talesara GL - Indian J Pharm Sci (2010)

General structure of compounds synthesized[19] 4IXa (X=H, Z=H), 4Xa (X=H, Z=H, n=2) and 4Xw (X=Cl, Z=OH, n=4)
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC3116306&req=5

Figure 4: General structure of compounds synthesized[19] 4IXa (X=H, Z=H), 4Xa (X=H, Z=H, n=2) and 4Xw (X=Cl, Z=OH, n=4)
Mentions: Alkoxyphathalimide derivative of thiazolidinop-yrimidines were found to have significant antifungal, antibacterial and antimalarial activity. Activity was increased with introduction of chloro group at the para-position in arylimino moiety and with increasing of length of alkyl chain in alkoxyphthalimide group whereas it is decreased when hydroxyl group was introduced. Structures of compounds 2Xa, 2Xb, 2Xc and 2Xs are shown in fig. 1. The antibacterial and antifungal activities were increased when the arylidene unit was introduced in thiazolidinone nucleus at position-5 but activity was decreased when hydroxyl group was present at para-position in arylidene unit. Structures of the compounds are shown in figs. 2 and 3. Compounds 2Xs, 3Xa and 4Xa were found to exhibit significant antimicrobial activities. These results suggest that antimicrobial activities are strongly affected by the presence or absense of alkoxyphthalimide moiety and hence compound 3Xa and 4Xa showed significant activity than compounds 3IXa and 4IXa (comparison in figs. 3] and 4). Although [1,5]-benzodiazepines have strong antibacterial and antifungal activity but it was found to show slightly lower activity than alkoxyphthalimide derivatives of thiazolidinopyrimidines.

Bottom Line: 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.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.

View Article: PubMed Central - PubMed

Affiliation: Organic Research Laboratory, Department of Chemistry, Banasthali University, Banasthali-304 022, India.

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 IC(50) 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.

No MeSH data available.


Related in: MedlinePlus