Chemical scaffolds with structural similarities to siderophores of nonribosomal peptide-polyketide origin as novel antimicrobials against Mycobacterium tuberculosis and Yersinia pestis
Mycobacterium tuberculosis (Mtb) and Yersinia pestis (Yp) produce siderophores with scaffolds of nonribosomal peptide-polyketide origin. Compounds with structural similarities to these siderophores were synthesized and evaluated as antimicrobials against Mtb and Yp under iron-limiting conditions mimicking the iron scarcity these pathogens encounter in the host and under standard iron-rich conditions. Several new antimicrobials were identified, including some with increased potency in the iron-limiting condition. Our study illustrates the possibility of screening compound libraries in both iron-rich and iron-limiting conditions to identify antimicrobials that may selectively target iron scarcity-adapted bacteria and highlights the usefulness of building combinatorial libraries of compounds having scaffolds with structural similarities to siderophores to feed into antimicrobial screening programs.
N-Hydroxythiosemicarbazones: Synthesis and in vitro antitubercular activity
N-Hydroxythiosemicarbazide was prepared by two methods starting from 2,4-dimethoxy benzyl amine and hydroxylamine hydrochloride, which in turn was reacted with various aldehydes and ketones to obtain the titled compounds. Eighteen compounds were tested fo
Synthesis, biological evaluation, and quantitative structure -activity relationship analysis of new Schiff bases of hydroxysemicarbazide as potential antitumor agents
Thirty Schiff bases of hydroxysemicarbazide (Ar-CH=NNHCONHOH) have been synthesized and tested against L1210 murine leukemia cells. The IC50 values were found to be in a range from 2.7 × 10-6 to 9.4 × 10-4 M. A total of 17
Ren, Shijun,Wang, Rubin,Komatsu, Kenichi,Bonaz-Krause, Patricia,Zyrianov, Yegor,McKenna, Charles E.,Csipke, Csaba,Tokes, Zoltan A.,Lien, Eric J.
p. 410 - 419
(2007/10/03)
4 hydroxysemicarbazide and derivatives
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Grobner,Muller
p. 341 - 343
(2007/10/08)
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