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PubMed1991

Pyrazole analogues of the bispyrrolecarboxamide anti-tumour antibiotics: synthesis, DNA binding and anti-tumour properties.

Four bispyrazole compounds have been prepared as potentially more stable analogues of the DNA minor groove binding polypyrrole compounds netropsin and distamycin, which are susceptible to oxidative breakdown. These compounds bind less strongly to DNA, and show much lower specificity for binding to AT-rich DNA sequences in comparison with distamycin. N.m.r. studies show that two of these compounds cause a downfield shift of the DNA imino proton resonances on interaction with the oligonucleotide d(ATATATATAT)2, suggesting that these isomers can adopt low-energy conformations similar to that shown by distamycin in its DNA minor groove binding site. The benzoic acid mustard analogue of one of the minor groove binding bispyrazoles was prepared, and showed in vitro cytotoxicity comparable with that of the previously-reported distamycin mustard, but only a low level of activity in vivo.

Amides↗
PubMed1990

Pyrazole sulfanilamides: nitroderivatives of 1-phenyl-3-sulfanilamidopyrazole. Note XVI.

Synthesis and structural characterization of 3 sulfanilamido-1-phenylpyrazoles bearing on 1-phenyl group nitro substituent o-, m-, p-positioned are reported. All derivatives are analysed through 1H and 13C NMR spectroscopy. The MIC values obtained against Escherichia coli are briefly discussed in terms of structure-activity relationship.

Anti-Bacterial Agents↗
PubMed1986

Pyrrolnitrin analogues. XII. Synthesis and biological activity of some pyrazole carboxylic acids.

Some 1,5-diaryl-, 1-aryl-5-(2-nitrobenzyl)-3-methylpyraloze-4-carboxylic acids and some of their 4-morpholino- and 4-N-methylpiperazino amides are prepared and tested as antibacterial agents. None of the tested compounds shows any noteworthy antimicrobial activity. The results are discussed and compared with the previously published results for other similarly structured compounds.

Anti-Bacterial Agents↗