Design, Synthesis, and Study of a Novel RXPA380-Proline Hybrid (RXPA380-P) as an Antihypertensive Agent

In drug discovery, molecular modification over the lead molecule is often crucial for the development of a drug. Herein, we report the molecular hybridization design of a novel RXPA380-proline hybrid via linking the parent compound, phosphinic peptide RXPA380, with a proline analogue. The presented synthetic route is straightforward and produces the desired product RXPA380-P in moderate yield. The C- and N-domain constructs of the angiotensin-converting enzyme of RXPA380-P appeared to be poor inhibitors of ACE as compared to the parent compound RXPA380

SERS of trititanate nanotubes : selective enhancement of catechol compounds

Funding: Xi'an Jiaotong Liverpool University. Grant Number: RDF- RDF-16-01-06.The surface enhanced Raman scattering of trititanate nanotubes (TiNT) modified with enediol ligands was investigated and it was found that the functional group dramatically affects the enhancement observed. For TiNT‐4‐nitrocatechol, a SERS enhancement is seen; however, when dopamine is attached, no signal is seen. The relative band gap positions upon 785 nm laser excitation are proposed to explain the observed phenomenon. This attachment is investigated by solid state NMR and UV/Vis spectroscopy and supported by DFT calculations to offers further insights into catechol coatings of nanomaterials and SERS by the chemical method. We expect this non noble metal containing composite material to have applications in bioimaging and bio and chemical detection.PostprintPeer reviewe

Glycosyl-Nucleolipids as New Bioinspired Amphiphiles

Four new Glycosyl-NucleoLipid (GNL) analogs featuring either a single fluorocarbon or double hydrocarbon chains were synthesized in good yields from azido thymidine as starting material. Physicochemical studies (surface tension measurements, differential scanning calorimetry) indicate that hydroxybutanamide-based GNLs feature endothermic phase transition temperatures like the previously reported double chain glycerol-based GNLs. The second generation of GNFs featuring a free nucleobase reported here presents a better surface activity (lower glim) compared to the first generation of GNFs

Structure-based bioisosteric design, synthesis and biological evaluation of novel pyrimidines as antiplasmodial antifolate agents

The efficacy of most marketed antimalarial drugs has been compromised by the development of parasite resistance, underscoring an urgent need to find new drugs with new mechanisms of action. This article describes the synthesis and the in vitro antimalarial profiling of antifolate P218 analogues, by exploring a bioisosteric replacement of the carboxylic group by a phosphinic moiety as well as structural isomerization of P218. The detailed synthetic route employed to access the title compounds is described. The listed compounds exhibited low antimalarial activity against drug-resistant strains of P. falciparum including chloroquine-resistant W2

Unprecedented Convergent Synthesis of Sugar-Functionalization of Phosphinic Acids under Metal-Free Conditions

[Image: see text] A novel TEA-catalyzed sugar-esterification of phosphinic acids was used as a general and efficient approach for the synthesis of a variety of phosphinates without any transition metal. The high efficiency of the current methodology and a convenient experimental procedure compensate for the moderate yields obtained. Another advantage is that the reaction tolerates different substituents attached to the phosphinic acids and the sugar moieties alongside the ease of isolation of the product

Parentage testing of day 10 equine embryos by amplified PCR analysis of microsatellites

International audienc

Parentage testing of day 10 equine embryos by amplified PCR analysis of microsatellites

National audienc