Works (6)
Updated: August 12th, 2023 21:14
2017 journal article
Structure of the Francisella response regulator QseB receiver domain, and characterization of QseB inhibition by antibiofilm 2-aminoimidazole-based compounds
MOLECULAR MICROBIOLOGY, 106(2), 223–235.
MeSH headings : Anti-Bacterial Agents / pharmacology; Bacterial Proteins / chemistry; Bacterial Proteins / metabolism; Bacterial Proteins / ultrastructure; Biofilms / drug effects; Francisella tularensis / metabolism; Gene Expression Regulation, Bacterial / genetics; Imidazoles / metabolism; Imidazoles / pharmacology; Protein Binding; Virulence / drug effects; Virulence Factors / genetics; Virulence Factors / metabolism
TL;DR:
It is shown that QseB interacts with 2‐aminoimidazole based compounds that impede its function, and this information will assist in tailoring compounds to act as adjuvants that will enhance the effect of antibiotics.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Source: Web Of Science
Added: August 6, 2018
2016 journal article
Evaluation of ethyl N-(2-phenethyl) carbamate analogues as biofilm inhibitors of methicillin resistant Staphylococcus aureus
ORGANIC & BIOMOLECULAR CHEMISTRY, 14(28), 6853–6856.
MeSH headings : Anti-Bacterial Agents / chemistry; Anti-Bacterial Agents / pharmacology; Biofilms / drug effects; Carbamates / chemistry; Carbamates / pharmacology; Humans; Methicillin-Resistant Staphylococcus aureus / drug effects; Methicillin-Resistant Staphylococcus aureus / physiology; Microbial Sensitivity Tests; Small Molecule Libraries / chemistry; Small Molecule Libraries / pharmacology; Staphylococcal Infections / drug therapy
TL;DR:
A small molecule library consisting of 45 compounds was synthesized based on the bacterial metabolite ethyl N-(2-phenethyl) carbamate which revealed a potent analogue capabale of inhibiting several strains of Methicillin Resistant S. aureus biofilms with low to moderate micromolar IC50 values.
(via Semantic Scholar)
open access via europepmc.org (repository)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Source: Web Of Science
Added: August 6, 2018
2016 journal article
Marine sponge alkaloids as a source of anti-bacterial adjuvants
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 26(24), 5863–5866.
author keywords: Marine sponge; Pyrrole-imidazole alkaloid; Biofilm; Antibiotic; Adjuvant
MeSH headings : Acinetobacter baumannii / drug effects; Alkaloids / chemistry; Alkaloids / metabolism; Alkaloids / pharmacology; Animals; Anti-Bacterial Agents / chemistry; Anti-Bacterial Agents / metabolism; Anti-Bacterial Agents / pharmacology; Dose-Response Relationship, Drug; Imidazoles / chemistry; Imidazoles / pharmacology; Methicillin-Resistant Staphylococcus aureus / drug effects; Microbial Sensitivity Tests; Molecular Structure; Porifera; Pyrroles / chemistry; Pyrroles / pharmacology; Structure-Activity Relationship
TL;DR:
The potential of marine secondary metabolites to serve as a source of non-traditional anti-bacterial agents is demonstrated by showing that pyrrole-imidazole alkaloids inhibit biofilm formation and suppress antibiotic resistance.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
14. Life Below Water
(OpenAlex)
Source: Web Of Science
Added: August 6, 2018
2016 journal article
Potentiation of the fosmidomycin analogue FR 900098 with substituted 2-oxazolines against Francisella novicida
MEDCHEMCOMM, 7(10), 1952–1956.
TL;DR:
A highly potent 2-oxazoline adjuvant was discovered capable of potentiating FR 900098 with a 1000-fold reduction in MIC against the Francisella sub-species F. novicida and F. philomiragia.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Source: Web Of Science
Added: August 6, 2018
2015 journal article
Aryl amide small-molecule inhibitors of microRNA miR-21 function
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 25(21), 4793–4796.
author keywords: miR-21; MicroRNA; Small-molecule inhibitors; Cancer; Gene regulation; Post-transcriptional regulation
MeSH headings : Amides / chemical synthesis; Amides / chemistry; Amides / pharmacology; Cell Line, Tumor; Dose-Response Relationship, Drug; HeLa Cells; Humans; MicroRNAs / antagonists & inhibitors; MicroRNAs / genetics; Molecular Structure; Small Molecule Libraries / chemical synthesis; Small Molecule Libraries / chemistry; Small Molecule Libraries / pharmacology; Structure-Activity Relationship
TL;DR:
Using a luciferase-based reporter assay under the control of miR-21 expression, a high-throughput screen of >300,000 compounds led to the discovery of a new aryl amide class of small-molecule miR -21 inhibitors, thus affording a new chemical probe for future studies.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science; OpenAlex)
Source: Web Of Science
Added: August 6, 2018
2015 journal article
Potentiation of Francisella resistance to conventional antibiotics through small molecule adjuvants
MEDCHEMCOMM, 7(1), 128–131.
TL;DR:
A screen of 20 compounds identified small molecule adjuvants capable of potentiating anitbiotic activty against Francisella philomiragia and led to the discovery of a potentially new class of small molecule aduvants containg an indole core.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Source: Web Of Science
Added: August 6, 2018
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