Synthesis and Antimycobacterial Activity of some 2-(4-Aminophenyl)-5-Substitutedamino-1,3,4-thiadiazole Derivatives and Their Coupling Products

Year 2016, Volume: 20 Issue: 2, 199 - 206, 02.02.2016

Sevgi Karakuş , Sevim Rollas

Abstract

In the present study, several 2-(4-aminophenyl)-5-substitutedamino-1,3,4-thiadiazoles (2a-l) and their coupling products, 2,3,4-pentanetrione-3-[4-(5-alkyl/arylamino-1,3,4-thiadiazole-2-yl)phenyl]hydrazones (3a-j) were synthesized in good yields and characterized by UV,  IR, ¹H-NMR, mass and elemental analysis. The compounds were evaluated for their in vitro antimycobacterial  activity  against Mycobacterium tuberculosis H37Rv. Antitubercular activity of the synthesized compounds was determined in vitro using the BACTEC 460 Radiometric System against Mycobacterium tuberculosis H37Rv at 6.25 mg/mL. The antimycobacterial data of screened compounds indicated  that 2-(4-aminophenyl)-5-(4-chlorophenyl)amino-1,3,4-thiadiazole demonstra-ted the highest inhibition  (2f ).

 

Keywords

1 , 3 , 4-thiadiazole , coupling products , antimycobacterial activity

Synthesis and antimycobacterial activity of some 2-(4-aminophenyl)- 5-substituted amino-1,3,4-thiadiazole derivatives and their coupling products

Abstract

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