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Öğe Macrocyclic peptidomimetics with antimicrobial activity: synthesis, bioassay, and molecular modeling studies(Royal Soc Chemistry, 2015) Ibrahim, Mohamed A.; Panda, Siva S.; Oliferenko, Alexander A.; Oliferenko, Polina V.; Girgis, Adel S.; Elagawany, Mohamed; Kucukbay, F. ZehraNovel, cyclic peptidomimetics were synthesized by facile acylation reactions using benzotriazole chemistry. Microbiological testing of the synthesized compounds revealed an exceptionally high activity against Candida albicans with a minimum inhibitory concentration (MIC) two orders of magnitude lower than the MIC of the antifungal reference drug amphotericin B. A strikingly high activity was also observed against three Gram-negative bacterial strains (Pseudomonas aeruginosa, Klebsiella pneumoniae and Proteus vulgaris), two of which are known human pathogens. Thus the discovered chemotype is a potential poly-pharmacological agent. The toxicity against mammalian tumor cells was found to be low, as demonstrated in five different human cell lines (HeLa, cervical; PC-3, prostate; MCF-7, breast; HepG2, liver; and HCT-116, colon). The internal consistency of the experimental data was studied using 3D-pharmacophore and 2D-QSAR.
