In this study we achieved an efficient metal-catalyzed radical “miniemulsion” polymerization with ferrocene (FeCp2) as a cocatalyst in conjunction with a thermoresponsive PEG containing ruthenium catalyst for the polymerization of methacrylate monomers. The iron-cocatalysis worked well even in...

The reaction of [(η5-C5Me5)Ru(PPh3)2Cl] (1) with acetonitrile in the presence of excess NH4PF6 leads to the formation of the cationic ruthenium(II) complex [(η5-C5Me5)Ru(PPh3)2(CH3CN)]PF6 (2). The complex (2) reacts with a series of N,N′ donor Schiff base ligands viz. para-substituted N-(pyri...

The heterogeneous three-component reaction of 2-aminopyridines, acetophenones and benzyl cyanide was achieved in NMP at 120 °C by using an MCM-41-anchored L-proline‑copper(I) complex [MCM-41-L-Proline-CuI] as catalyst under air, yielding a wide variety of 3-cyanoimidazo[1,2-a]pyridines in moder...

An inclusion complex of prostaglandin E1 (PGE1) with β-cyclodextrin (β-Cyd) or O-carboxymethyl-O-ethyl-β-cyclodextrin (CME-β-CyD) was made as topical preparations in a fatty alcohol/propylene glycol ointment base. When the PGE1 preparations were applied onto the skin of hairless mice, the va...

Heterocyclic compounds are the interesting core structures for the development of new bioactive compounds. Fatty acids are derived from renewable raw materials and exhibit various biological activities. Several researchers are amalgamating these two bioactive components to yield bioactive hybrid...

This paper provides an overview of the synthesis and biological activity of the most representative benzohydroxamic acid-based histone deacetylase inhibitors published to date. Benzohydroxamic acids comprise an important class of HDAC inhibitors, and recently several of these structures have bee...

Starting from (E)-β-substituted-β-nitroacrylates and α,β-unsaturated ketones, a stereoselective organocatalyzed one-pot methodology allowed to synthesize highly decorated chiral 2-nitro-cyclohexane carboxylic esters. The reaction is promoted by Cinchona alkaloid-derived primary amines in the...

In 1887, Claisen and Lowman1 reported that the condensation of 2 mol of an ester, such as ethyl acetate, in the presence of base gave the β-keto ester, ethyl acetoacetate (ethyl 3-oxobutanoate; equation 1). The intramolecular equivalent was recognized by Dieckmann in 1894.2 He found that heatin...

2-(1-Aminoalkyl)oxazole-4 and 5-carboxylates are available, without detectable racemisation, by a sequence involving N-acylation of isoxazol-5(2H)one carboxylates with phthalimidoamino acids, photolysis of the acylated product, and hydrazinolysis. An application of the procedure to the synthesis...

9-(2-phosphonylmethoxyethyl)adenine (PMEA) and its closely related structural analogue (R)-9-(2-phosphonylmethoxypropyl)adenine (PMPA) are potent inhibitors of retroviruses and hepatitis B virus. In its oral prodrug form (adefovir dipivoxil), PMEA is currently the subject of advanced phase II/II...

To determine the efficacy of 9-(2-phosphonylmethoxyethyl)adenine (PMEA) as a prophylactic chemotherapeutic agent for the treatment of lentivirus infections, three groups of specific pathogen free cats were treated with 0, 3, or 6 mg kg−1 twice daily doses of PMEA beginning 24 h prior to virus ch...

PMEA (9-(2-phosphonylmethoxyethyl)adenine) is a potent inhibitor of DNA viruses and retroviruses able to enhance natural immune functions such as natural killer cell activity and interferon production. The results reported in this paper show that the treatment with PMEA significatively decreased...

The antiviral drug, 9-(2-phosphonylmethoxyethyl) adenine (PMEA) was linked to a synthetic and neutral polymer bearing mannosyl residues to allow its internalization by macrophages via membrane lectins. PMEA bound to the mannosylated polymer was more efficient in vitro than free PMEA in preventin...

9-(2-Phosphonylmethoxyethyl)adenine (PMEA; 1) was acylated with chloromethyl pivalate to afford bis(pivaloyloxymethyl) PMEA (2). The ester prodrug demonstrated enhanced in vitro potency against HSV-2 greater than 150-fold higher than the parent compound. The antiviral activity of 2 was 50-fold b...

In order to evaluate the influence of antiviral nucleoside analogues upon the natural immune system, we investigated the immunomodulatory activity of 9-(2-phosphonylmethoxyethyl)adenine (PMEA), a nucleotide analogue with potent anti-HIV and anti-herpes activity, in a murine system. C57BL/6 mice ...

Following exposure to 9-(2-phosphonylmethoxyethyl)adenine (an inhibitor of the cellular DNA polymerases α, δ and ϵ), human erythroleukemia K562, human T-lymphoid CEM and murine leukemia L1210 cells markedly accumulated in the S phase of the cell cycle. In contrast to DNA replication, RNA synth...

After repeated passages of herpes simplex type 1 (HSV-1) KOS virus in the presence of 9-(2-phosphonylmethoxyethyl)adenine (PMEA) a mutant denoted PMEAr HSV-1 was isolated which grew well in the presence of 50–100 μg·ml−1 of the drug. PMEAr HSV-1 was still sensitive to the related phosphonate ...

An ultra sensitive method for the direct measurement of 9-(2-phosphonylmethoxyethyl)adenine (PMEA), an antiviral agent for hepatitis B, in human serum using high performance liquid chromatography/tandem mass spectrometry (LC–MS/MS) has been developed. This method involves the addition of [13C]P...

SummaryObjectives/HypothesisTo evaluate the degree of dysplasia following cidofovir injections while documenting human papillomavirus (HPV) type in patients with recurrent respiratory papillomatosis (RRP).

After allogeneic hematopoietic stem cell transplantation (HSCT), BK virus–associated hemorrhagic cystitis (BKV-HC) is a common complication. Although supportive measures have been the standard of care for many years, several studies suggested the efficacy of cidofovir. The aim of this study was...