A5058383338- Catalytic C–H Functionalization Methods
- Catalytic Alkyne Reactions
- Synthesis and Biological Evaluation
- Cyclopropane Reaction Mechanisms
- Synthesis and Catalytic Reactions
- Antifungal resistance and susceptibility
- Asymmetric Hydrogenation and Catalysis
- Catalytic Cross-Coupling Reactions
- Synthesis and biological activity
- Cancer therapeutics and mechanisms
- Asymmetric Synthesis and Catalysis
- Histone Deacetylase Inhibitors Research
- Protein Degradation and Inhibitors
- Ubiquitin and proteasome pathways
- Garlic and Onion Studies
- Nail Diseases and Treatments
- Research on Leishmaniasis Studies
- Click Chemistry and Applications
- Chemical synthesis and alkaloids
- Fungal Infections and Studies
- Organic Chemistry Cycloaddition Reactions
- Phenothiazines and Benzothiazines Synthesis and Activities
- Synthesis and Characterization of Heterocyclic Compounds
- Axial and Atropisomeric Chirality Synthesis
- Ovarian cancer diagnosis and treatment
University of Sussex
2025
University of Sheffield
2013-2014
University of Liverpool
2009-2013
Nantes Université
2008-2011
Cibles et Médicaments des Infections et de l'Immunité
2009
Enlarge! CH bond activation and β-carbon elimination are combined in a net intramolecular hydroacylation of alkylidenecyclobutanes alkylideneazetidines the presence rhodium catalysts, affording eight-membered-ring compounds high yield (see scheme). This study demonstrates possibility exploiting strain energy azetidines through new transition-metal-catalyzed reactions.
The profile of PC945, a novel triazole antifungal designed for administration via inhalation, was assessed in range vitro and vivo studies. PC945 characterized as potent, tightly binding inhibitor Aspergillus fumigatus sterol 14α-demethylase (CYP51A CYP51B) activity (50% inhibitory concentrations [IC50s], 0.23 μM 0.22 μM, respectively) with characteristic type II azole spectra. Against 96 clinically isolated A. strains, the MIC values ranged from 0.032 to >8 μg/ml, while those voriconazole...
Copper catalyzed aldehyde–alkyne–amine (A3) couplings lead to multifunctional, racemic, propargylic amines, many on a multigram scale. As part of an industrial collaboration, selection linkers was purified by chiral HPLC afford single enantiomers, the absolute configuration which determined vibrational circular dichroism (vCD). To show medicinal chemistry applications, selected were further derivatized into potential cellular probes and (+)-JQ1 containing PROTACs (proteolysis targeting...
Significant rate enhancements in the Diels–Alder reaction of alkynes and 2-pyrones bearing a Lewis basic group are observed when combination alkynyltrifluoroborates BF3·OEt2 is used. This process generates functionalized aromatic compounds with complete regiocontrol. The enhancement was studied by density functional theory methods appears to originate from coordination diene substrate mixture alkynylborane intermediates, followed acid-mediated product equilibration step. Evidence for this...
Von kleinen zu großen Ringen: C-H-Aktivierung und β-Kohlenstoffeliminierung wurden in einer intramolekularen Hydroacylierung von Alkylidencyclobutanen -azetidinen kombiniert, die Gegenwart Rhodiumkatalysatoren abläuft Produkte mit achtgliedrigen Ringen hohen Ausbeuten liefert (siehe Schema). Dabei konnte Spannungsenergie Azetidinen übergangsmetallkatalysierten Reaktion unter genutzt werden.
Mild intramolecular hydroacylation of α,α-disubstituted 4-alkylidenecyclopropanals has been developed, avoiding decarbonylation and affording cycloheptenones in good yields. The reaction is chemoselective favour the alkylidenecyclopropane moiety when potential alkene or alkyne acceptors are tethered to substrate.
The Rh(I)-catalyzed intramolecular hydroacylation of cis and trans asymmetrically substituted alkylidenecyclobutanes proceeds according to three mechanistic pathways. As shown by deuterium-labeling experiments, the mechanism accounting for rearrangement isomers includes cleavage carbon-carbon bonds a remarkable transannular 3-exo-trig carbometalation.
ABSTRACT The antifungal effects of the novel triazole PC1244, designed for topical or inhaled administration, against Aspergillus fumigatus were tested in a range vitro and vivo studies. PC1244 demonstrated potent activities clinical A. isolates ( n = 96) with MIC 0.016 to 0.25 μg/ml, whereas voriconazole was 0.5 μg/ml. strong tight-binding inhibitor recombinant CYP51A CYP51B (sterol 14α-demethylase) enzymes strongly inhibited ergosterol synthesis 50% inhibitory concentration 8 nM. effective...
Abstract As part of our studies focused on the design 1‐[((hetero)aryl‐ and piperidinylmethyl)amino]‐2‐phenyl‐3‐(1 H ‐1,2,4‐triazol‐1‐yl)propan‐2‐ols as antifungal agents, we report development new extended benzylamine derivatives substituted at para position by sulfonamide or retrosulfonamide groups linked to alkyl aryl chains. These molecules have broad‐spectrum activities not only against Candida spp., including fluconazole‐resistant strains, but also a filamentous species ( A. fumigatus...
A new series of 1-benzyl-3-(imidazol-1-ylmethyl)indoles were synthesized according to a previous 3D-QSAR predictive model and assayed for their antiparasitic activity upon Leishmania mexicana promastigotes. The biological results obtained these twelve molecules showed an IC50 ranging from 2.3 32 μM mainly illustrated the importance hydrophobic parameter para-position benzyl group. In order improve activities compounds check potential influence electronic on this particular position, Craig...
In situ generated alkynylaluminum reagents have been utilized in a [4 + 2] cycloaddition with 2-pyrones bearing Lewis basic donor. The reactions proceed at or below room temperature and complete regiocontrol. This one-pot method affords diversely substituted aromatic compounds under very mild conditions.
Atropisomeric drug substances are known to have different biological properties. Compounds containing the N-benzoylbenzazepine motif been shown exhibit energetically restricted rotation around Ar(CO)N axis. Herein we report, for first time, synthesis, physical characterisation and anti-viral profiles of a series C-4 C-5 methylated thieno-benzazepines. NMR analysis reveals that incorporation single additional substituent at either these loci influences conformational dynamics azepine ring...
Abstract CDK12 and CDK13 regulate gene expression through translation splicing of mRNA. Impaired activity has been shown to reduce the a range genes involved in DNA homologous repair leading induction ‘BRCAness’ phenotype cells. inhibitors have potential many different indications, including overcoming emergent resistance PARP inhibition, enhancing efficacy inhibition patients with BRCA1/2 wt status [1] extending immune checkpoint immunogenic cell death [2]. Recently, certain classes also...
Abstract In situ prepared alkynylaluminum derivatives are used as novel 2π compounds in [4 + 2] cycloadditions with 2‐pyrans bearing amides or N‐heteroarenes directing groups.
Abstract Mild intramolecular hydroacylation of α,α‐disubstituted 4‐alkylidenecyclopropanals, such (I), (VII), and (IX) is described avoiding decarbonylation affording cycloheptenones (II), (VIII), (X) in good yields.
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