Quinolones are a very important family of antibacterial agents that are widely prescribed for the treatment of infections in humans. Since their discovery in the early 1960s, the quinolone group of antibacterials has generated considerable clinical and scientific interest. Two major groups of compounds have been developed from the basic molecule: quinolones and naphthyridones. The 4-pyridone-3-...

Abstract The synthesis of polycyclic compounds is high interest due to the prevalence these motifs in drugs and natural products. Herein, we report on stereoselective construction 3D bicyclic scaffolds azetidine derivatives by modulation N ‐sulfonylimines achieve either [4+2]‐ or [2+2]‐cycloaddition reactions. utility method was established further product. Mechanistic studies are also included...

2,6-Difluorophenylnitrene was reinvestigated both experimentally, in Ar matrices at 10 K, and computationally, by DFT and CASSCF/CASPT2 calculations. Almost-pure samples of both neutral rearrangement products (the bicyclic azirine and the cyclic ketenimine) of a phenylnitrene were prepared and characterized for the first time. These samples were then subjected to X-irradiation in the presence o...

leishmaniasis is a neglected public health problem caused by the protozoan species belonging to the genus leishmania affecting mostly the poor populations of developing countries. the causative organism is transmitted by female sandflies. cutaneous, mucocutaneous, and visceral clinical manifestations are the most frequent forms of leishmaniasis. chemotherapy still relies on the use of pentavale...

Leishmaniasis is a neglected public health problem caused by the protozoan species belonging to the genus Leishmania affecting mostly the poor populations of developing countries. The causative organism is transmitted by female sandflies. Cutaneous, mucocutaneous, and visceral clinical manifestations are the most frequent forms of leishmaniasis. Chemotherapy still relies on the use of pentavale...

A series of photooxidation experiments were conducted in an atmospheric simulation chamber in order to investigate the secondary organic aerosol (SOA) formed from the anthropogenic model gas phase precursor, 1,3,5-trimethylbenzene. Alongside specific aerosol measurements, comprehensive gas phase measurements, primarily by chem-5 ical ionisation reaction time-of-flight mass spectrometry (CIR-TOF...

Abstract TIGIT is an emerging immune checkpoint receptor expressed higher than PD-1 in some tumors especially anti-PD1 resistant tumors. By competing with the co-stimulatory CD226/DNAM-1 for binding to CD155/PVR, transduces inhibitory signals and suppresses response. Therefore, we sought discover inhibitors improving tumor immunotherapy. Through directional cloning, bacterial transformation pha...

The reaction of tetraarylbutatrienes (tetraaryl[3]cumulenes) with tetracyanoethene (TCNE), a strong electron-accepting molecule, at room temperature yielded novel four-membered ring compounds (head-to-tail unsymmetrically substituted diarylallene dimers) by [2 + 2] cycloaddition of the central C=C bond of the butatrienes. This reaction proceeded through a head-to-head symmetrically substituted ...

Leishmania microtubules play an important role not only in cell division, but also in keeping the shape of the parasite and motility of its free-living stages. Microtubules result from the self-assembly of alpha and beta tubulins, two phylogenetically conserved and very abundant eukaryotic proteins in kinetoplastids. The colchicine binding domain has inspired the discovery and development of se...

A novel synthesis of furanodictines A [2-acetamido-3,6-anhydro-2-deoxy-5-O-isovaleryl-D-glucofuranose (1)] and B [2-acetamido-3,6-anhydro-2-deoxy-5-O-isovaleryl-D-mannofuranose (2)] is described starting from 2-acetamido-2-deoxy-D-glucose (GlcNAc). The synthetic protocol is based on deriving the epimeric bicyclic 3,6-anhydro sugars [2-acetamido-3,6-anhydro-2-deoxy-D-glucofuranose (4) and 2-acet...