51760-23-7Relevant academic research and scientific papers
New fluorescent tetraphenylporphyrin-based dendrimers with alkene-linked fluorenyl antennae designed for oxygen sensitization
Blanchard-Desce, Mireille,Mongin, Olivier,Paul, Frédéric,Paul-Roth, Christine O.,Shi, Limiao,Sun, Zhipeng,Yao, Dandan
, (2021/08/23)
The design of porphyrin-based dendrimers featuring conjugated fluorenyl dendrons via alkene spacers allows evaluating the importance of the role of these spacers on the optical properties of interest. In the continuation of previous studies, a second-gene
Structure-Activity Studies with Bis-Amidines That Potentiate Gram-Positive Specific Antibiotics against Gram-Negative Pathogens
Wesseling, Charlotte M. J.,Slingerland, Cornelis J.,Veraar, Shanice,Lok, Samantha,Martin, Nathaniel I.
, p. 3314 - 3335 (2021/11/24)
Pentamidine, an FDA-approved antiparasitic drug, was recently identified as an outer membrane disrupting synergist that potentiates erythromycin, rifampicin, and novobiocin against Gram-negative bacteria. The same study also described a preliminary structure-activity relationship using commercially available pentamidine analogues. We here report the design, synthesis, and evaluation of a broader panel of bis-amidines inspired by pentamidine. The present study both validates the previously observed synergistic activity reported for pentamidine, while further assessing the capacity for structurally similar bis-amidines to also potentiate Gram-positive specific antibiotics against Gram-negative pathogens. Among the bis-amidines prepared, a number of them were found to exhibit synergistic activity greater than pentamidine. These synergists were shown to effectively potentiate the activity of Gram-positive specific antibiotics against multiple Gram-negative pathogens such as Acinetobacter baumannii, Klebsiella pneumoniae, Pseudomonas aeruginosa, and Escherichia coli, including polymyxin- and carbapenem-resistant strains.
ENDOSOMOLYTIC AGENTS FOR GENE THERAPY
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, (2018/04/17)
Compounds of formula (I), wherein Ar is an aryl group optionally further substituted with one or more groups R3; A is a lipophilic, hydrophobic moiety; R1 is a phosphodiester, phosphotriester, thioether or amide group; X is an unsubs
Structure-guided design of selective inhibitors of neuronal nitric oxide synthase
Huang, He,Li, Huiying,Martásek, Pavel,Roman, Linda J.,Poulos, Thomas L.,Silverman, Richard B.
, p. 3024 - 3032 (2013/06/04)
Nitric oxide synthases (NOSs) comprise three closely related isoforms that catalyze the oxidation of l-arginine to l-citrulline and the important second messenger nitric oxide (NO). Pharmacological selective inhibition of neuronal NOS (nNOS) has the potential to be therapeutically beneficial in various neurodegenerative diseases. Here, we present a structure-guided, selective nNOS inhibitor design based on the crystal structure of lead compound 1 in nNOS. The best inhibitor, 7, exhibited low nanomolar inhibitory potency and good isoform selectivities (nNOS over eNOS and iNOS are 472-fold and 239-fold, respectively). Consistent with the good selectivity, 7 binds to nNOS and eNOS with different binding modes. The distinctly different binding modes of 7, driven by the critical residue Asp597 in nNOS, offers compelling insight to explain its isozyme selectivity, which should guide future drug design programs.
Synthesis of S-acetyl oligo-p-aryleneethynylene tetrathiols
Hassan Omar, Omar,Babudri, Francesco,Farinola, Gianluca M.,Naso, Francesco,Operamolla, Alessandra
supporting information; experimental part, p. 529 - 537 (2011/03/22)
A novel class of tetrathiolated aryleneethynylene oligomers was obtained by the Cassar-Heck-Sonogashira coupling between S,S-(5-ethynyl-1,3-phenylene) bis(methylene)diethanethioate (1) and aryl diiodides or dibromides. Although standard coupling condition
