dc.contributor.author |
Ibrahim, MA |
|
dc.contributor.author |
Panda, SS |
|
dc.contributor.author |
Oliferenko, AA |
|
dc.contributor.author |
Oliferenko, PV |
|
dc.contributor.author |
Girgis, AS |
|
dc.contributor.author |
Elagawany, M |
|
dc.contributor.author |
Kucukbay, FZ |
|
dc.contributor.author |
Panda, CS |
|
dc.contributor.author |
Pillai, GG |
|
dc.contributor.author |
Samir, A |
|
dc.contributor.author |
Tamm, K |
|
dc.contributor.author |
Hall, CD |
|
dc.contributor.author |
Katritzky, AR |
|
dc.date.accessioned |
2022-10-13T11:46:38Z |
|
dc.date.available |
2022-10-13T11:46:38Z |
|
dc.date.issued |
2015 |
|
dc.identifier.uri |
http://hdl.handle.net/11616/79600 |
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dc.description.abstract |
Novel, 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. |
|
dc.description.abstract |
C1 [Ibrahim, Mohamed A.; Panda, Siva S.; Oliferenko, Alexander A.; Oliferenko, Polina V.; Elagawany, Mohamed; Kucukbay, F. Zehra; Panda, Chandramukhi S.; Pillai, Girinath G.; Hall, C. Dennis; Katritzky, Alan R.] Univ Florida, Dept Chem, Gainesville, FL 32611 USA. |
|
dc.description.abstract |
[Ibrahim, Mohamed A.] Misr Univ Sci & Technol, Coll Pharm, Dept Organ Chem, Soaad Kafafi, Giza Governorat, Egypt. |
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dc.description.abstract |
[Ibrahim, Mohamed A.] Almaarefa Coll Sci & Technol, Dept Pharmaceut Chem, Riyadh 11597, Saudi Arabia. |
|
dc.description.abstract |
[Panda, Siva S.] Georgia Reagents Univ, Dept Chem & Phys, Augusta, GA 30912 USA. |
|
dc.description.abstract |
[Girgis, Adel S.] Natl Res Ctr, Dept Pesticide Chem, Giza 12622, Egypt. |
|
dc.description.abstract |
[Elagawany, Mohamed] Damanhour Univ, Fac Pharm, Dept Pharmaceut Chem, Damanhour, Egypt. |
|
dc.description.abstract |
[Kucukbay, F. Zehra] Inonu Univ, Fac Pharm, Dept Basic Pharmaceut Sci, TR-44280 Malatya, Turkey. |
|
dc.description.abstract |
[Pillai, Girinath G.; Tamm, Kaido] Univ Tartu, Dept Chem, EE-50411 Tartu, Estonia. |
|
dc.description.abstract |
[Samir, Ahmed] Cairo Univ, Fac Vet Med, Dept Microbiol, Cairo, Egypt. |
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dc.source |
ORGANIC & BIOMOLECULAR CHEMISTRY |
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dc.title |
Macrocyclic peptidomimetics with antimicrobial activity: synthesis, |
|
dc.title |
bioassay, and molecular modeling studies |
|