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A series of N-[2-(dimethylamino)ethyl]-4-aryl-1-piperazinecarboxamides was synthesized and evaluated for antiallergy activity. Several derivatives had activity in the passive foot anaphylaxis (PFA) assay, an IgE-mediated model useful in the detection of compounds possessing antiallergic activity, but no derivative tested had activity at 10 mg/kg in the guinea pig anaphylaxis (GPA) assay. One analogue, N-[2-(dimethylamino)ethyl]-4-(4-fluorophenyl)-1-piperazinecarboxamide, had an IC50 = 310 nM for inhibition of tritiated mepyramine binding to H1 histaminic receptors isolated from guinea pig cerebral cortex.

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Reference:
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

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Mass drug administration (MDA) to eliminate lymphatic filariasis is already in place in 32 out of 83 endemic countries. Expansion of the MDA programme to other countries and within large countries such as India is necessary to achieve the goal of lymphatic filariasis elimination. However, expansion and sustenance of the global campaign to eliminate lymphatic filariasis requires commitment and allocation of funds by governments and donor agencies. This could be achieved, at least to some extent, by highlighting the benefits of the programme in relation to costs. On the basis of various studies in south India, this article assesses the costs, effectiveness and economic and social benefits of the MDA programmes aimed at eliminating lymphatic filariasis.

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Reference:
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

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There is an urgent need for new strategies to combat infectious diseases in developing countries. Many pathogens have evolved to elude immunity and this has limited the utility of current therapies. Additionally, the emergence of co-infections and drug resistant pathogens has increased the need for advanced therapeutic and diagnostic strategies. These challenges can be addressed with therapies that boost the quality and magnitude of an immune response in a predictable, designable fashion that can be applied for wide-spread use. Here, we discuss how biomaterials and specifically nanoscale delivery vehicles can be used to modify and improve the immune system response against infectious diseases. Immunotherapy of infectious disease is the enhancement or modulation of the immune system response to more effectively prevent or clear pathogen infection. Nanoscale vehicles are particularly adept at facilitating immunotherapeutic approaches because they can be engineered to have different physical properties, encapsulated agents, and surface ligands. Additionally, nanoscaled point-of-care diagnostics offer new alternatives for portable and sensitive health monitoring that can guide the use of nanoscale immunotherapies. By exploiting the unique tunability of nanoscale biomaterials to activate, shape, and detect immune system effector function, it may be possible in the near future to generate practical strategies for the prevention and treatment of infectious diseases in the developing world.

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Reference:
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

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Filariasis in the new millennium

The Indonesian national fdariasis eradication program in its pursuit in obtaining microfilarial rates below 1% in filariasis endemic locations was on its right track until the monetary crisis started 3 years ago. This crisis which is not over yet at present is complicated by unstable public safety causing population shifts where people from filaria endemic locations seek refuge in non-endemic areas. This updated review will hopefully serve as a timely reminder to our physicians and health workers especially on the mode of filarial transmission as well as on its clinical presentations and presently accepted ways of management. This paper also will serve as an introduction into the present breakthroughs in this new millenium as noted in the field of diagnostics and simplified mass treatment schedules making it possible for the elimination of lymphatic filariasis as a public health problem. A global alliance under the guidance of the World Health Organization with support of the multinational pharmaceutical companies for providing free expensive medication as needed. The WHO also cooperates closely with the Tropical Diseases Research task forces of Filariasis Intervention Research and of Product Development, that in the end will provide the means to eradicate this disease for once and forever from the face of the earth.

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Reference:
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

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Ivermectin ? Old Drug, New Tricks?

Ivermectin is one of the most important drugs in veterinary and human medicine for the control of parasitic infection and was the joint focus of the 2015 Nobel Prize in Physiology or Medicine, some 35 years after its remarkable discovery. Although best described for its activity on glutamate-gated chloride channels in parasitic nematodes, understanding of its mode of action remains incomplete. In the field of veterinary medicine, resistance to ivermectin is now widespread, but the mechanisms underlying resistance are unresolved. Here we discuss the history of this versatile drug and its use in global health. Based on recent studies in a variety of systems, we question whether ivermectin could have additional modes of action on parasitic nematodes.

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Reference:
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

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Mosquito-Borne Diseases as a Global Health Problem: Implications for Pregnancy and Travel

Importance: Mosquitoes are the most common disease vectors worldwide. A combination of factors, including changes in public health policy, climate change, and global travel, has led to the resurgence and spread of these diseases in our modern world. Pregnant women are vulnerable to a number of these illnesses, and obstetricians are likely to encounter pregnant travelers who have been exposed. Objective: This review was conducted to summarize knowledge of mosquito-borne diseases and their relevance in pregnancy. This will allow obstetricians to provide proper advice regarding travel and prepare providers to recognize manifestations of these illnesses in the pregnant woman. Evidence Acquisition: A review of the current literature was performed to summarize the various manifestations of mosquito-borne illnesses in pregnant women and discuss obstetric outcomes and management of disease in pregnancy. Results: Mosquito-borne illnesses usually manifest after a period of incubation lasting from days to weeks. Symptoms usually include a febrile illness but may be nonspecific and may masquerade as pregnancyspecific illnesses such as preeclampsia or HELLP (hemolysis, elevated liver enzyme levels, and low platelet levels); a large number of patients remain asymptomatic. Pregnancy-related outcomes include spontaneous abortion, intrauterine fetal demise, intrauterine transmission to the fetus, and congenital anomalies. Management during pregnancy is mainly supportive. Precautions against disease include protective clothing and insect repellents. Vaccines are either available or in development. Conclusions and Relevance: Mosquito-borne disease should be considered in pregnant women who present with a febrile illness and a relevant exposure history. Prompt recognition can allow supportive treatment to the mother and fetal resuscitation and surveillance. Target Audience: Obstetricians and gynecologists, family physicians. Learning Objectives: After completing this activity, the learner should be better able to describe the presentation, symptoms, and diagnosis of mosquito-borne diseases including malaria, chikungunya, dengue, yellow fever, West Nile virus, Zika, and filariasis; describe the risks of mosquito-borne diseases to the pregnant woman and her fetus; and outline the management considerations for pregnant women with specific mosquito-borne infections.

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Reference:
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

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Lymphatic filariasis control in Tanzania: Infection, disease perceptions and drug uptake patterns in an endemic community after multiple rounds of mass drug administration

Background: Lymphatic filariasis (LF) control in most countries of sub-Saharan Africa is based on annual mass drug administration (MDA) with a combination of ivermectin and albendazole, in order to interrupt transmission. However, attaining and maintaining high treatment coverage has been a challenge in many LF control programmes. This study was designed to elucidate reasons for continued transmission of LF in an endemic area of Tanga, northeastern Tanzania, where control activities based on MDA had been in place for eight years by the time of this study in 2012. Methods: A cross-sectional questionnaire survey was conducted in three sentinel villages used for monitoring the impact of MDA on LF transmission. A total of 747 individuals were interviewed, out of which 172 (23.0%), 27 (3.6%) and 49 (6.5%) had been shown to have circulating filarial antigens (CFA), microfilaraemia (MF) and LF gross lesions, respectively, prior to the interviews. Results: The interviewed population had a mean age of 33.7 years and a male to female ratio of 0.8. Males, individuals aged 30 years and above, peasants/fishermen and recent immigrants to the study communities were significantly more affected (CFA, MF and/ or LF gross lesions) than the other population groups. However, drug uptake rates were not significantly different between LF affected (those with CFA, MF and/ or LF gross lesions) and non-affected individuals. Likewise, drug uptake rates were not significantly different across different demographic parameters of the study population, some of which differed significantly in the level of infection. Moreover, it was found that misconceptions on how LF can be acquired were still evident, linking its transmission to witchcraft, heredity and sexual behaviour. Conclusions: The findings indicated that misconceptions about LF and its transmission still existed despite eight years of control activities in the area. Improved communication on the rationale of MDA and an enhanced drug delivery strategy that is adapted to the local settings and targeting important demographic groups that serve as reservoir of infection will help in reaching the elimination target within a reasonable timeframe.

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Reference:
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

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Pharmacokinetics of diethylcarbamazine: Prediction by concentration in saliva

The concentration of diethylcarbamazine in saliva was used to determine pharmacokinetic parameters, in comparison to plasma and urine concentrations. Six healthy adult male volunteers were administered 150 mg diethylcarbamazine with 400 ml of water. At seven different time intervals, blood, urine and saliva samples were taken, and different pharmacokinetic parameters measured. The plasma-saliva concentration ratio was calculated as 1.53 whereas the observed ratio was 3.82. The half lives, times to reach peak plasma concentration, and elimination rate constants did not show any significant difference in the different samples. The plasma peak concentration and areas under the curve were significantly (p<0.05) increased from those of the saliva. At 24 h, when diethylcarbamazine was absent in urine, the plasma and saliva concentrations were almost zero. Diethylcarbamazine is secreted in saliva, and its concentration in saliva can be used to monitor drug therapy. If you’re interested in learning more about 3105-95-1, below is a message from the blog Manager. Related Products of 4730-54-5

Reference:
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

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Human Migration and the Spread of the Nematode Parasite Wuchereria bancrofti

The human disease lymphatic filariasis causes the debilitating effects of elephantiasis and hydrocele. Lymphatic filariasis currently affects the lives of 90 million people in 52 countries. There are three nematodes that cause lymphatic filariasis, Brugia malayi, Brugia timori, and Wuchereria bancrofti, but 90% of all cases of lymphatic filariasis are caused solely by W. bancrofti (Wb). Here we use population genomics to reconstruct the probable route and timing of migration of Wb strains that currently infect Africa, Haiti, and Papua New Guinea (PNG). We used selective whole genome amplification to sequence 42 whole genomes of single Wb worms from populations in Haiti, Mali, Kenya, and PNG. Our results are consistent with a hypothesis of an Island Southeast Asia or East Asian origin of Wb. Our demographic models support divergence times that correlate with the migration of human populations. We hypothesize that PNG was infected at two separate times, first by the Melanesians and later by the migrating Austronesians. The migrating Austronesians also likely introduced Wb to Madagascar where later migrations spread it to continental Africa. From Africa, Wb spread to the New World during the transatlantic slave trade. Genome scans identified 17 genes that were highly differentiated among Wb populations. Among these are genes associated with human immune suppression, insecticide sensitivity, and proposed drug targets. Identifying the distribution of genetic diversity in Wb populations and selection forces acting on the genome will build a foundation to test future hypotheses and help predict response to current eradication efforts.

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Reference:
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

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Leukotrienes: One step in our understanding of asthma

The steps leading to the discovery of leukotrienes and the researchers that played a major part in this long process are presented. The pharmacology of these exquisitely potent compounds shows that they express bronchoconstrictor activity and numerous cellular effects via very specific receptors. Experimental evidence strongly suggests that these mediators play a significant role in asthma physiopathology. Numerous approaches were taken to block their effects on the lungs and this led to the discovery of selected drugs used for asthma treatment. The complexity of this disease and its treatment is emphasized.

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Reference:
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI