Design and synthesis of short amphiphilic cationic peptidomimetics based on biphenyl backbone as antibacterial agents
Antimicrobial peptides (AMPs) and their synthetic mimics have received recent interest as new alternatives to traditional antibiotics in attempts to overcome the rise of antibiotic resistance in many microbes. AMPs are part of the natural defenses of most living organisms and they also have a unique mechanism of action against bacteria. Herein, a new series of short amphiphilic cationic peptidomimetics were synthesized by incorporating the 3′-amino-[1,1′-biphenyl]-3-carboxylic acid backbone to mimic the essential properties of natural AMPs. By altering hydrophobicity and charge, we identified the most potent analogue 25g that was active against both Gram-positive Staphylococcus aureus (MIC = 15.6 μM) and Gram-negative Escherichia coli (MIC = 7.8 μM) bacteria. Cytoplasmic permeability assay results revealed that 25g acts primarily by depolarization of lipids in cytoplasmic membranes. The active compounds were also investigated for their cytotoxicity to human cells, lysis of lipid bilayers using tethered bilayer lipid membranes (tBLMs) and their activity against established biofilms of S. aureus and E. coli.
Kuppusamy, Rajesh,Yasir, Muhammad,Berry, Thomas,Cranfield, Charles G.,Nizalapur, Shashidhar,Yee, Eugene,Kimyon, Onder,Taunk, Aditi,Ho, Kitty K.K.,Cornell, Bruce,Manefield, Mike,Willcox, Mark,Black, David StC,Kumar, Naresh
p. 1702 - 1722
(2017/11/17)
SOLABEGRON ZWITTERION AND USES THEREOF
This application relates to solabegron zwitterion useful for the treatment of lower urinary tract symptoms such as, for example, overactive bladder and prostate disorders. Additionally, this application relates to pharmaceutical compositions and methods o
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Paragraph 0075;0089
(2017/05/19)
HEPATITIS B CORE PROTEIN ALLOSTERIC MODULATORS
ABSTRACT The present disclosure provides, in part, compounds having allosteric effector properties against Hepatitis B virus Cp. Also provided herein are methods of treating viral infections, such as hepatitis B, comprising administering to a patient in need thereof a disclosed compound.
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Paragraph 000408
(2015/10/05)
Synthesis of the β3-adrenergic receptor agonist Solabegron and Analogous N-(2-Ethylamino)-β-amino alcohols from O-acylated cyanohydrins - expanding the scope of minor enantiomer recycling
A novel methodology to produce highly enantioenriched N-(2-ethylamino)-β-amino alcohols was developed. These compounds were obtained from O-(α-bromoacyl) cyanohydrins, which were synthesized by the minor enantiomer methodology employing a Lewis acid and a
Hertzberg, Robin,Monreal Santiago, Guillermo,Moberg, Christina
p. 2937 - 2941
(2015/03/18)
Biarylaniline phenethanolamines as potent and selective β3 adrenergic receptor agonists
The synthesis of a series of phenethanolamine aniline agonists that contain an aniline ring on the right-hand side of the molecule substituted at the meta position with a benzoic acid or a pyridyl carboxylate is described. Several of the analogues (e.g.,
Uehling, David E.,Shearer, Barry G.,Donaldson, Kelly H.,Chao, Esther Y.,Deaton, David N.,Adkison, Kim K.,Brown, Kathleen K.,Cariello, Neal F.,Faison, Walter L.,Lancaster, Mary E.,Lin, Jasmine,Hart, Robert,Milliken, Tula O.,Paulik, Mark A.,Sherman, Bryan W.,Sugg, Elizabeth E.,Cowan, Conrad
p. 2758 - 2771
(2007/10/03)
Cyclic imino derivatives and pharmaceutical compositions containing them
The invention relates to cyclic imino compounds which have, inter alia, valuable pharmacological properties, especially inhibitory effects on cell aggregation, pharmaceutical compositions which contain these compounds and processes for preparing them.
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(2008/06/13)
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