Some 3-thioxo/alkylthio-1,2,4-triazoles with a substituted thiourea moiety as possible antimycobacterials


Kucukguzel İ. , Kucukguzel Ş. G. , Rollas S., Kiraz M.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, cilt.11, ss.1703-1707, 2001 (SCI İndekslerine Giren Dergi) identifier identifier identifier

  • Cilt numarası: 11 Konu: 13
  • Basım Tarihi: 2001
  • Doi Numarası: 10.1016/s0960-894x(01)00283-9
  • Dergi Adı: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
  • Sayfa Sayıları: ss.1703-1707

Özet

A series of novel N-alkyl/aryl-N-1-[4-(4-alkyl/aryl-2,4-dihydro-3H-1,2,4-triazole-3-thione-5-yl)phenyl]thioureas 1-19 and three S-alkylated representatives of the former, N-alkyl/aryl-N-1-[4-(3-aralkylthio-4-alkyl/aryl -4H-1,2,4-triazole-5-yl)phenyl]thioureas 20-22, were synthesized and tested for antimycobacterial activity against Mycobacterium tuberculosis H37 Rv as well as Mycobacterium fortuitum ATCC 6841 which is a rapid growing opportunistic pathogen. Compounds 4 and 9-11 were found to possess the same MIC value with that of Tobramycin against M. fortuitum ATCC 6541 whereas 1-3 and 21 had positive response against;M. tuberculosis H37Rv at varying degrees. Compound 21 was identified as the most potent derivative of the 1-22 series by an MIC value of 6.25 mug/mL and selectivity index of 1.6. (C) 2001 Elsevier Science Ltd. All rights reserved.