Quaternary ammonium N,N-dichloroamines as topical, antimicrobial agents

Francavilla, Charles; Low, Eddy; Nair, Satheesh; Kim, Bum; Shiau, Timothy P; Debabov, Dmitri; Celeri, Chris; Alvarez, Nichole; Houchin, Ashley; Xu, Ping; Najafi, Ramin; Jain, Rakesh

doi:10.1016/j.bmcl.2009.03.120

Cited by 23 publications

(17 citation statements)

References 28 publications

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“…It recently completed a phase-II trial for the treatment of bacterial conjunctivitis (NCT01877694). Auriclosene (28) was designed to be a more stable derivative of the naturally occurring oxidant N-dichlorotaurine [172][173][174][175] and also was recently shown to inactivate S. aureus toxins. 176 Lefamulin (29) (BC-3781) is a semi-synthetic pleuromutilin 177,178 derivative originally discovered by Nabriva Therapeutics AG (Vienna, Austria).…”

Section: Compounds Undergoing Clinical Evaluationmentioning

confidence: 99%

Antibiotics in the clinical pipeline at the end of 2015

2016

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There is growing global recognition that the continued emergence of multidrug-resistant bacteria poses a serious threat to human health. Action plans released by the World Health Organization and governments of the UK and USA in particular recognize that discovering new antibiotics, particularly those with new modes of action, is one essential element required to avert future catastrophic pandemics. This review lists the 30 antibiotics and two β-lactamase/β-lactam combinations first launched since 2000, and analyzes in depth seven new antibiotics and two new β-lactam/β-lactamase inhibitor combinations launched since 2013. The development status, mode of action, spectra of activity and genesis (natural product, natural product-derived, synthetic or protein/mammalian peptide) of the 37 compounds and six β-lactamase/β-lactam combinations being evaluated in clinical trials between 2013 and 2015 are discussed. Compounds discontinued from clinical development since 2013 and new antibacterial pharmacophores are also reviewed.

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Section: Compounds Undergoing Clinical Evaluationmentioning

confidence: 99%

Antibiotics in the clinical pipeline at the end of 2015

2016

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“…From the point of view of disinfection, they are bactericidal for a wide range of pathogens such as E. coli [110,111], S. aureus [112,113,114], S. mutans , B. subtilis , P. aeruginosa [114] and the fungal pathogen C. albicans [112,114]. …”

Section: Operational Challenges Cleaning and Disinfectionmentioning

confidence: 99%

Antibacterial Metallic Touch Surfaces

et al. 2016

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Our aim is to present a comprehensive review of the development of modern antibacterial metallic materials as touch surfaces in healthcare settings. Initially we compare Japanese, European and US standards for the assessment of antimicrobial activity. The variations in methodologies defined in these standards are highlighted. Our review will also cover the most relevant factors that define the antimicrobial performance of metals, namely, the effect of humidity, material geometry, chemistry, physical properties and oxidation of the material. The state of the art in contact-killing materials will be described. Finally, the effect of cleaning products, including disinfectants, on the antimicrobial performance, either by direct contact or by altering the touch surface chemistry on which the microbes attach, will be discussed. We offer our outlook, identifying research areas that require further development and an overview of potential future directions of this exciting field.

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“…SHELXS-2013, SHELXL-2013 [2] and X-STEP32 [3] were used for structure solution and refinement. Mercury [4] and Platon [5] were used for structure visualization and analysis.…”

Section: Single-crystal X-ray Diffractionmentioning

confidence: 99%

“…Several possible mechanisms of the antimicrobial activity of QACs have been hypothesized [10][11][12]. The general mechanism of QACs action was summarized by M. Tischer et al [13] and includes adsorption and penetration through the cell wall; binding to components of the cell membrane and their disorganization; cell leakage; intracellular degradation of proteins and nucleic acids; lysis of cell wall components M A N U S C R I P T A C C E P T E D ACCEPTED MANUSCRIPT 3 and, finally, complete loss of structural organization of the cell. Agents that disrupt the cell wall are likely to be bactericidal.…”

Section: Introductionmentioning

confidence: 98%