Oseltamivir modified bovine serum albumin inhibits neuraminidase activity and accumulates virion particles to disturb influenza virus replication.

The preparation of oseltamivir-bovine serum albumin conjugate (OS-BSA) for use as a multivalent influenza neuraminidase (NA) inhibitor is reported. Briefly, the oseltamivir azidohexyl ester was synthesized and covalently bound via an orthogonal attachment to bicyclononyne-modified BSA using copper-free click chemistry. Primary antiviral assays on NA protein and cellular levels showed that the synthetic multivalent OS-BSA conjugate was a more effective inhibitor than monomeric OS azidohexyl ester.

Four new fatty acid derivatives from sp. T24, an endophytic fungus isolated from .

The endophytic fungus sp. is known to contain many secondary metabolites, but fatty acid derivatives have rarely been found. In this study, four new fatty acid derivatives (-), together with four known compounds (-), were isolated from sp.

Thiosialoside-decorated polymers use a two-step mechanism to inhibit both early and late stages of influenza virus infection.

We describe the preparation of thiosialoside-modified poly (methyl vinyl ether-alt-maleic anhydride) as second-generation polymeric conjugates for the inhibition of influenza virus infection. These synthetic glycopolymers show significantly enhanced neuraminidase inhibitory and antiviral activity in enzyme and cellular levels, respectively. The polyvalent thiosialosides also exhibit comparable inhibitory activity to the first-line anti-influenza drugs Zanamivir® and Oseltamivir® against the PR8 influenza virus strain in virus growth inhibition assays, which may be attributed to multivalent binding to neuraminidase on the virion particles, leading to the virion aggregation and further inhibiting the attaching/fusion and releasing steps in the influenza virus life-cycle.

Polyvalent effect enhances diglycosidic antiplasmodial activity.

An efficient and facile total synthesis of diglycoside Matayoside D isolated from the root bark of Matayba guianensis with antiplasmodial activity have been accomplished in 11 steps with 5% overall yields starting from commercially available glucose and rhamnose. Furthermore, a class of the diglycosidic derivatives with different lengths of the linker and valences were also prepared and evaluated for their antiplasmodial activities against chloroquine-susceptible (3D7) and chloroquine-resistant (W2) strains of Plasmodium falciparum. Low valent and short linker attached diglycoside show no enhancement of the antiplasmodial activity while polyvalent conjugates showed enhanced antiplasmodial activity with IC50 value at least 20 fold better than that of the corresponding diglycosidic monomer.

Calix[4]arenes containing thiourea and amide moieties: neutral receptors towards alpha,omega-dicarboxylate anions.

Two-armed neutral anion receptors (4,5), were prepared and examined for their anion-binding ability using UV-vis, fluorescence and 1H NMR spectra in DMSO. The results of non-linear curve fitting indicate that 4 or 5 form 1 : 1 stoichiometric complexes with dicarboxylate anions by multiple hydrogen bonding interactions and the sensitivity for recognition of dicarboxylate depends on the chain length of these dicarboxylate anions. Receptors 4 and 5 have no binding ability with acetate, dihydrogen phosphate and the halogen (Cl-, Br-, I-) anions.