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1.
Eur J Med Chem ; 75: 195-202, 2014 Mar 21.
Article in English | MEDLINE | ID: mdl-24531232

ABSTRACT

A series of 1,2,4-(triazolo[3,4-b][1,3,4]thiadiazol-6-yl)selenopheno[2,3-d]pyrimidines (10a-j) were synthesized with various substituted anilines and benzoic acids. Structures of newly synthesized compounds were established by IR, (1)H &(13)C NMR and LC-MS spectral data. The antioxidant activity of the synthesized compounds was evaluated by DPPH, NO and H2O2 radical scavenging methods. The newly synthesized compounds were evaluated for their antimicrobial activity against Gram +ve and Gram -ve bacteria and antifungal activity by well diffusion method. Compounds 10d, 10h and 10i showed promising antioxidant, antibacterial as well as antifungal activity and these were found to be the most potent activity molecules when compared with that of standard drugs. Molecules docking studies have been performed on Staphylococcus aureus (SA) of Gram +ve bacteria.


Subject(s)
Anti-Infective Agents/chemistry , Antioxidants/chemistry , Benzene Derivatives/chemistry , Organoselenium Compounds/chemistry , Pyrimidines/chemistry , Thiadiazoles/chemistry , Anti-Infective Agents/chemical synthesis , Anti-Infective Agents/pharmacology , Antioxidants/chemical synthesis , Antioxidants/pharmacology , Bacteria/drug effects , Bacterial Infections/drug therapy , Benzene Derivatives/chemical synthesis , Benzene Derivatives/pharmacology , Fungi/drug effects , Humans , Microbial Sensitivity Tests , Molecular Docking Simulation , Mycoses/drug therapy , Organoselenium Compounds/chemical synthesis , Organoselenium Compounds/pharmacology , Pyrimidines/chemical synthesis , Pyrimidines/pharmacology , Thiadiazoles/chemical synthesis , Thiadiazoles/pharmacology
2.
Eur J Med Chem ; 58: 340-5, 2012 Dec.
Article in English | MEDLINE | ID: mdl-23149297

ABSTRACT

This study represents the synthesis of a new series of N-substituted phenyl-5-methyl-6-(5-(4-substituted phenyl)-1,3,4-oxadiazol-2-yl)thieno[2,3-d]pyrimidin-4-amine derivatives (4a-l) and substituted phenylamino-5-methylthieno[2,3-d]pyrimidine-6-carboxylic acid derivatives (3a-d). The newly synthesized compounds were characterized by (1)H NMR, (13)C NMR, LC-MS and IR analyses. All these novel compounds were screened for their in vitro antioxidant activity by employing DPPH, hydrogen peroxide, and nitric oxide radical scavenging assays. Compounds 4k, 4j, 4d, and 4e showed significant radical scavenging due to the presence of electron donating substituent on both sides of the thienopyrimidine ring enhances the activity and electron withdrawing groups like nitro decrease.


Subject(s)
Antioxidants/chemistry , Free Radical Scavengers/chemistry , Oxadiazoles/chemistry , Pyrimidines/chemistry , Biphenyl Compounds/chemistry , Hydrogen Peroxide/chemistry , Nitric Oxide/chemistry , Picrates/chemistry
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