Ibrahim, Mohamed A.Panda, Siva S.Oliferenko, Alexander A.Oliferenko, Polina V.Girgis, Adel S.Elagawany, MohamedKucukbay, F. Zehra2024-08-042024-08-0420151477-05201477-0539https://doi.org/10.1039/c5ob01400jhttps://hdl.handle.net/11616/96967Novel, 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.eninfo:eu-repo/semantics/closedAccessAnti-Oncological AlkaloidsRegioselective SynthesisRational DesignAmphotericin-BQsarDerivativesPeptidesEfficacySpectrumArticle1336949295032625683810.1039/c5ob01400j2-s2.0-84940851334Q1WOS:000360656100019Q1