On the basis of our previous results 22 salicylanilides were synthesized. The compounds were tested for in vitro antimycobacterial activity against Mycobacterium tuberculosis, Mycobacterium kansasii, and Mycobacterium avium. The Free-Wilson method was used to evaluate structure-antimycobacterial activity relationships. 4-Chloro-N-(4-propylphenyl)salicylamide and 5-chloro-N-(4-propylphenyl)salicylamide were selected for preclinical studies.
Based on our previous studies, 21 new halogenated 3-(4-alkylphenyl)-1,3-benzoxazine-2,4-(3H)-diones were synthesized by the reaction of salicylanilides and methyl-chloroformate. All compounds were screened in vitro against three different strains of mycobacterium, and Free-Wilson method was used to establish structure-activity relationships. 6-Bromo-3-(4-butylphenyl)-1,3-benzoxazine-2,4-(3H)-dione 3b proved to be the most active compound of the series.
Antibacterial activity X 0060The Oriented Development of Antituberculotics: Salicylanilides. -Synthesis and evaluation of SAR of title compounds (I) are described. Derivatives (Ia) and (Ib) are selected for preclinical studies. -(WAISSER*, K.; MATYK, J.; DIVISOVA, H.; HUSAKOVA, P.; KUNES, J.; KLIMESOVA, V.; KAUSTOVA, J.; MOELLMANN, U.; DAHSE, H.-M.; MIKO, M.; Arch. Pharm. (Weinheim, Ger.) 339 (2006) 11, 616-620; Fac. Pharm., Charles Univ., CZ-500 05 Hradec Kralove, Czech Republic; Eng.) -H. Haber 11-233
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