Antimycobacterial Activity of 3,4-dichlorophenyl-ureas, N,N-diphenyl-ureas and Related Derivatives

Abstract

Substituted urea derivatives were prepared by reacting 3,4-dichlorophenyl isocyanate with amino acids, dipeptides, histamine or dicyandiamide among others, or from N,N-diphenyl-carbamoyl chloride and amino acids, dipeptides, or histamine. Other derivatives were obtained by reaction of PABA or PAS with arylsulfonyl halides. Some of the new compounds showed appreciable activity as antimycobacterial agents against Mycobacterium tuberculosis H37Rv, producing an inhibition of growth in the range of 80–89%, at a concentration of 6.25 μM. Some derivatives of this series might constitute interesting lead molecules for designing novel types of drugs effective against M. tuberculosis, a re-emerging pathogen both in the developed and under-developed countries.

Key Words:

• 3,4-dichlorophenylureas
• N,N-diphenylureas
• Mycobacterium tuberculosis
• Sulfonamides