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Medicinal-Pharmaceutical Chemistry Commons

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Articles 1 - 4 of 4

Full-Text Articles in Medicinal-Pharmaceutical Chemistry

Antifungal Potential Of Copper(Ii), Manganese(Ii) And Silver(I) 1,10-Phenanthroline Chelates Against Multidrug-Resistant Fungal Species Forming The Candida Haemulonii Complex: Impact On The Planktonic And Biofilm Lifestyles, Rafael M. Gandra, Pauraic Mc Carron, Mariana F. Fernandes, Lívia S. Ramos, Thaís P. Mello, Ana Carolina Aor, Marta H. Branquinha, Malachy Mccann, Michael Devereux, André L. S. Santos Jul 2017

Antifungal Potential Of Copper(Ii), Manganese(Ii) And Silver(I) 1,10-Phenanthroline Chelates Against Multidrug-Resistant Fungal Species Forming The Candida Haemulonii Complex: Impact On The Planktonic And Biofilm Lifestyles, Rafael M. Gandra, Pauraic Mc Carron, Mariana F. Fernandes, Lívia S. Ramos, Thaís P. Mello, Ana Carolina Aor, Marta H. Branquinha, Malachy Mccann, Michael Devereux, André L. S. Santos

Articles

Candida haemulonii, Candida haemulonii var. vulnera and Candida duobushaemulonii, which form the C. haemulonii complex, are emerging etiologic agents of fungal infections known to be resistant to the most commonly used antifungals. The well-established anti-Candida potential ofmetal complexes containing 1,10-phenanthroline (phen) ligands encouraged us to evaluate different copper(II), manganese(II), and silver(I) phen chelates for their ability to inhibit planktonic growth and biofilm of C. haemulonii species complex. Two novel coordination complexes, {[Cu(3,6,9-tdda)(phen)2].3H2O.EtOH}n and [Ag2(3,6,9-tdda)(phen)4].EtOH (3,6,9-tddaH2 = 3,6,9-trioxaundecanedioic acid), were ...


The Antibacterial Activity Of Metal Complexes Containing 1, 10-Phenanthroline: Potential As Alternatire Therapeutics In The Era Of Antibiotic Resistance, Livia Viganon, Orla L. Howe, Pauraic Mccarron, Malachy Mccann, Michael Devereux Jan 2017

The Antibacterial Activity Of Metal Complexes Containing 1, 10-Phenanthroline: Potential As Alternatire Therapeutics In The Era Of Antibiotic Resistance, Livia Viganon, Orla L. Howe, Pauraic Mccarron, Malachy Mccann, Michael Devereux

Articles

The “antibiotic era”, characterized by the overuse and misuse of antibiotics, over the last half-century has culminated in the present critical “era of resistance”. The treatment of bacterial infections is challenging because of a decline in the current arsenal of useful antibiotics and the slow rate of new drug development. The discovery of a new gene (mcr-1) in 2015, which enables bacteria to be highly resistant to polymyxins (such as colistin), the last line of antibiotic defence left, heralds a new level of concern as this gene is susceptible to horizontal gene transfer, with alarming potential to be spread between ...


Inhibition Of The Thioesterase Activity Of Human Fatty Acid Synthase By 1,4- And 9,10-Diones, Herman H. Odens Sep 2014

Inhibition Of The Thioesterase Activity Of Human Fatty Acid Synthase By 1,4- And 9,10-Diones, Herman H. Odens

Faculty Works

Fatty acid synthase (FASN) is the enzyme that synthesizes fatty acids de novo in human cells. Although FASN is generally expressed at low levels in most normal tissues, its expression is highly upregulated in many cancers. Consistent with this notion, inhibition of FASN activity has demonstrated potential to halt proliferation and induce cell death in vitro and to block tumor growth in vivo. Consequently, FASN is widely recognized as a valuable therapeutic target. In this report, we describe a variety of 1,4-quinones and 9,10- anthraquinones, including several natural compounds and some newly synthesized compounds, that potently inhibit the ...


Studies On The Synthesis Of Orthogonally Protected Azalanthionines, And Of Routes Towards B-Methyl Azalanthionines, By Ring-Opening Of N-Activated Aziridine-2-Crboxylates, Keith O'Brien, Keith Ó Proinsias, Fintan Kelleher Jun 2014

Studies On The Synthesis Of Orthogonally Protected Azalanthionines, And Of Routes Towards B-Methyl Azalanthionines, By Ring-Opening Of N-Activated Aziridine-2-Crboxylates, Keith O'Brien, Keith Ó Proinsias, Fintan Kelleher

Articles

Orthogonally protected azalanthionines were successfully synthesised by the ring-opening of N-activated aziridine-2-carboxylates with protected diaminopropanoic acids (DAPs). The required DAPs were also prepared by ring-opening of N-activated aziridine-2-carboxylates with para-methoxybenzylamine, but it was found that the choice of aziridine protecting groups dictated both the success of the reaction as well as the regioselectivity of the isolated products. Attempts to extend the methodology to the preparation of the more sterically demanding b-methyl azalanthionines have, so far, been unsuccessful.