Novel ketolide antibiotics with a fused five-membered lactone ring – synthesis, physicochemical and antimicrobial properties was written by Hunziker, Daniel;Wyss, Pierre-C.;Angehrn, Peter;Mueller, Aranka;Marty, Hans-Peter;Halm, Remy;Kellenberger, Laurenz;Bitsch, Veronique;Biringer, Gerard;Arnold, Wolf;Stampfli, Andreas;Schmitt-Hoffmann, Anne;Cousot, Denis. And the article was included in Bioorganic & Medicinal Chemistry in 2004.Related Products of 45887-08-9 This article mentions the following:
In an effort to find novel semisynthetic macrolides with extended antibacterial spectrum and improved activity we prepared a series of compounds based on com. available clarithromycin, a potent and safe antimicrobial agent of outstanding clin. and com. interest. According to the literature, improvement of antibacterial activity of erythromycin type antibiotics can be achieved by introduction of fused heterocycles such as cyclic carbonates or carbamates at positions 11 and 12 (such as in telithromycin). In the course of the work presented here, a similar, hitherto unprecedented set of compounds bearing a five-membered lactone ring fused to positions 11 and 12 was prepared based on carbon-carbon bond formation via intramol. Michael addition of a [(hetero)arylalkylthio]acetic acid ester enolate to an α,β-unsaturated ketone as the key step. Some of the ketolide compounds described in this paper were highly active against a representative set of erythromycin sensitive and erythromycin resistant test strains. The best compound showed a similar antimicrobial spectrum and comparable activity in vitro as well as in vivo as telithromycin. Furthermore, some physicochem. properties of these compounds were determined and are presented here. On the basis of these results, the novel ketolide lactones presented in this paper emerged as valuable lead compounds with comparable properties as the com. ketolide antibacterial telithromycin (KetekTM). In the experiment, the researchers used many compounds, for example, 3-(1H-Pyrazol-3-yl)pyridine (cas: 45887-08-9Related Products of 45887-08-9).
3-(1H-Pyrazol-3-yl)pyridine (cas: 45887-08-9) belongs to pyrazole derivatives. An alternative way to synthesize multisubstituted pyrazoles is the Csingle bondH arylation of simple pyrazoles. Pyrazole the presence of this nucleus in pharmacological agents of diverse therapeutic categories such as celecoxib, a potent anti-inflammatory, the antidepressant agent fezolamide have proved the pharmacological potential of the pyrazole moiety. Related Products of 45887-08-9
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics