The growing population and health-care burden (due to STIs and HIV) imposes a particular economic crisis over resource-poor countries. Thus a novel approach as vaginal microbicides emerges as integrated tool to control both population and anti-STIs/HIV. Our continued efforts in this field led to...

Caffeine is one of the most worldwide consumed methylxanthines. It is well-known for its thermogenic and cell metabolism modulating effects. Based on methylxanthines' chemical structure, 8-(3-phenylpropyl)-1,3,7-triethylxanthine (PTX) is a novel adenosine antagonist with higher receptor aff...

The synthesis of racemic 3-aminobicyclo[3.3.0]octane-1,3-dicarboxylic acids (2 and 3) which are conformationally constrained ACPD analogues, has been achieved in seven steps starting from the readily available Weiss diketone (4). Partial reduction of of 4 to 5, followed by phenyl ring oxidation ...

(1S,3R)-Aminocyclopentane-1,3-dicarboxylic acid 1, a widely used metabotropic glutamate receptor agonist has been synthesized. Hydrolysis followed by Curtius rearrangement of 5 derived from dimethyl (S)-malate gave 6 with excellent diastereofacial selectivity (>97% de), which was converted into ...

1-(3-Oxocyclobutyl) carboxylic acid (4a) was converted into N-Boc-protected 1-(3-oxocyclobutyl) urea (5a), a key intermediate for the preparation of agonists of metabotropic glutamate receptor 5, in one-step when treated with diphenyl phosphoryl azide and triethylamine in tert-butanol. The mecha...

Novel routes for the synthesis of spiro derivatives of Meldrum’s acid and 2-substituted malonic acid derivatives have been developed. Meldrum’s acid was monoalkylated using a Michael addition reaction. Mono-Michael adducts were then alkylated using substituted haloalkanes, which on condensatio...

A Friedel-Crafts condensation of 1,7-dimethoxynaphthalene with the anhydride IV gave a mixture of products from which, after esterification, the ketoesters IX and X could be isolated in 16 and 4·25% yield, respectively. These were hydrogenolysed with PdC to the desoxyesters XI and XII. Cyclod...

The preparation of enantiopure (1R,2S)-2-chloromethyl-3-oxocyclopentanecarboxylic acid 9, an interesting possible precursor of the antitumor agent sarkomycin, from a camphor-derived 3-hydroxymethylnorbornan-2-one is reported. The described procedure constitutes the first stereocontrolled approac...

N-Substituted amino-2(5H)-oxazolones A are a novel class of insecticides acting as nicotinic acetylcholine receptor (nAChR) agonists and show potent activity against hemipteran insect species. Here we report the discovery and preparation of this class of chemistry. Our efforts in SAR elucidation...

The production yields of ϒ(1S), ϒ(2S), and ϒ(3S) quarkonium states are measured through their decays into muon pairs in the CMS detector, in PbPb and pp collisions at the centre-of-mass energy per nucleon pair of 2.76 TeV. The data correspond to integrated luminosities of 166μb−1 and 5.4pb−1 fo...

The effect of solvent composition on the uv–visible spectrum of methyl orange was investigated for application to the quantitative determination of ethanol. At fixed pH, there was a hypsochromic shift of the absorbance band of methyl orange with increasing ethanol concentration. Using acetate b...

An extensive study has been carried out where CO2 has been used both as solvent and antisolvent to appreciate orange leaves as a source of powerful antioxidant nanoparticles. In the former case, the leaves were processed directly to yield particles in the nano or micrometer range. In the latter ...

In this study, MgO modified diatomite (MgO-D) was used for recovery of microalgae (Chlorella pyrenoidosa FACHB-9), NH4+-N and phosphate from wastewater. The effects of adsorbent dosage, solution pH, contact time, and coexisting substances were investigated. The results showed that MgO-D exhibite...

Simultaneous ammonium and phosphate removal characteristics and mechanism, as well as the major influencing factors, such as pH, temperature and co-existing ions, onto NaOH-activated and lanthanum-impregnated zeolite (NLZ) were investigated. The phosphate adsorption increases from 0.2 mg g−1 for...

The induction of Fusarium wilt by continuous cropping has become a severe problem for watermelon cultivation around the world. Here, the feasibility and underlying mechanism of soil fumigation with ammonium bicarbonate (AB) or metam sodium (MS) under high temperature (HT) were investigated for t...

Biological methods are a promising approach to treating wastewater in order to produce water of an appropriate quality for sub-potable water purposes, thus reducing pressure on potable water sources. Daphnia magna are organisms that filter on small suspended particles and bacteria and so may be ...

Publisher SummaryAdenosine exerts physiological effects on the nervous system through interactions with cell surface receptors. In the nervous system adenosine has been shown to alter levels of cyclic adenosine 3', 5’-monophosphate (CAMP), inhibit synaptic activity and neuronal excitabilit...

A new family of thirteen phosphoramidate prodrugs (ProTides) of different 6-substituted-5-fluorouridine nucleoside analogues were synthesized and evaluated as potential anticancer agents. In addition, antiviral activity against Chikungunya (CHIKV) virus was evaluated using a cytopathic effect in...

Certain freshwater turtles and fish are extremely anoxia-tolerant, capable of surviving hours of anoxia at high temperatures and weeks to months at low temperatures. There is great interest in understanding the cellular mechanisms underlying anoxia-tolerance in these groups because they are anox...

Adenosine has been shown to initiate apoptosis through different mechanisms: (i) activation of adenosine receptors, (ii) intracellular conversion to AMP and stimulation of AMP-activated kinase, (iii) conversion to S-adenosylhomocysteine (AdoHcy), which is an inhibitor of S-adenosylmethionine (Ad...