Molecules, Vol. 24, Pages 4095: The Development of Novel Compounds Against Malaria: Quinolines, Triazolpyridines, Pyrazolopyridines and Pyrazolopyrimidines

Molecules, Vol. 24, Pages 4095: The Development of Novel Compounds Against Malaria: Quinolines, Triazolpyridines, Pyrazolopyridines and Pyrazolopyrimidines Molecules doi: 10.3390/molecules24224095 Authors: Luiz C. S. Pinheiro Lívia M. Feitosa Marilia O. Gandi Flávia F. Silveira Nubia Boechat Based on medicinal chemistry tools, new compounds for malaria treatment were designed. The scaffolds of the drugs used to treat malaria, such as chloroquine, primaquine, amodiaquine, mefloquine and sulfadoxine, were used as inspiration. We demonstrated the importance of quinoline and non-quinoline derivatives in vitro with activity against the W2 chloroquine-resistant (CQR) Plasmodium falciparum clone strain and in vivo against Plasmodium berghei-infected mouse model. Among the quinoline derivatives, new hybrids between chloroquine and sulfadoxine were designed, which gave rise to an important prototype that was more active than both chloroquine and sulfadoxine. Hybrids between chloroquine–atorvastatin and primaquine–atorvastatin were also synthesized and shown to be more potent than the parent drugs alone. Additionally, among the quinoline derivatives, new mefloquine derivatives were synthesized. Among the non-quinoline derivatives, we obtained excellent results with the triazolopyrimidine nucleus, which gave us prototype I that inspired the synthesis of new heterocycles. The pyrazolopyrimidine derivatives stood out as non-quinoline deriv...
Source: Molecules - Category: Chemistry Authors: Tags: Review Source Type: research

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This study aims to investigate the antiatherogenic effects of the ethanol extract of U. diffracta and its mechanism.MethodA high fat diet and VD3 were used to establish the atherosclerotic rat model, with 0.004 g/kg/d of simvastatin as a positive control, fed with 0.7, 1.4, and 2.8 g/kg/d of Usnea ethanol extract for 21 days. The blood, liver, and aorta samples from each rat were collected after the last administration. Pharmacodynamic effects were evaluated. The inflammation related factors, the gene expressions of Toll-like receptor 5 (TLR5), myeloid differentiating factor 88 (MyD88), and nuclear factor-κB (NF-...
Source: Biomedicine and Pharmacotherapy - Category: Drugs & Pharmacology Source Type: research
CONCLUSIONS: Compared with the model group, simvastatin and ethanol extract of U. diffracta can significantly reduce the serum levels of triglyceride (TG), low-density lipoprotein cholesterol (LDL-C), Ca2+, AST, ALT, the liver contents of total cholesterol (TC), TG, AI and liver index, as well as significantly increase the contents of high-density lipoprotein cholesterol (HDL-C) both in serum and liver (p 
Source: Biomedicine and pharmacotherapy = Biomedecine and pharmacotherapie - Category: Drugs & Pharmacology Authors: Tags: Biomed Pharmacother Source Type: research
We examined 9293 individuals from the Copenhagen General Population Study using nuclear magnetic resonance spectroscopy measurements of total cholesterol, free- and esterified cholesterol, triglycerides, phospholipids, and particle concentration. Fourteen subclasses of decreasing size and their lipid constituents were analysed: six subclasses were very low-density lipoprotein (VLDL), one intermediate-density lipoprotein (IDL), three low-density lipoprotein (LDL), and four subclasses were high-density lipoprotein (HDL). Remnant lipoproteins were VLDL and IDL combined. Mean nonfasting cholesterol concentration was 72...
Source: Fight Aging! - Category: Research Authors: Tags: Newsletters Source Type: blogs
For the 16 years that Dr. Brian Westerberg, a Canadian surgeon, worked volunteer missions at the Mulago National Referral Hospital in Kampala, Uganda, scarcity was the norm. The patients usually exceeded the 1,500 allotted beds. Running water was once cut off when the debt-ridden hospital was unable to pay its bills. On some of his early trips, Westerberg even brought over drugs from Canada in order to treat patients. But as low-cost generics made in India and China became widely available through Uganda’s government and international aid agencies in the early 2000s, it seemed at first like the supply issue had been ...
Source: TIME: Health - Category: Consumer Health News Authors: Tags: Uncategorized generic drugs medication medicine Source Type: news
Malaria can progress to malaria-associated ARDS (MA-ARDS), with a mortality rate of up to 80%. Since it is caused by sequestration of parasitized cells in the lung and a deregulated host immune response, the use of an antimalarial drug associated with an anti-inflammatory compound could improve MA-ARDS outcomes. We evaluated the effects of Rosuvastatin (ROSU), a statin with immunomodulatory properties largely used for treatment of cardiovascular diseases, and its association with dihydroartemisinin (DHA) in an experimental model. C57/BL6 mice were infected with Plasmodium berghei NK65, treated with ROSU(3mg/Kg), DHA(20mg/K...
Source: European Respiratory Journal - Category: Respiratory Medicine Authors: Tags: Mechanisms of Lung Injury and Repair Source Type: research
In conclusion, I would never advise John McCain and his family, or any other GBM patient, as to which of these treatments—or which combination of treatments—they should use. I hope they will learn about all of them, and decide on their own which one or ones they would like to try. I would also encourage them to do their own research, or to hire a researcher with experience in finding sensible, science-based, cutting-edge treatments. I am very worried that they will not know about these treatments, and others like them, and will just use the standard of care. That would be a shame. It might also be a death sent...
Source: HONEST MEDICINE: My Dream for the Future - Category: Consumer Health News Authors: Source Type: blogs
CHOLESTEROL can cause heart disease, heart attack, and stroke, but may be lowered through statins. These drugs may also be used to fight infectious diseases, such as malaria and typhoid, according to new research.
Source: Daily Express - Health - Category: Consumer Health News Source Type: news
From portable genome sequencers until genetic tests revealing distant relations with Thomas Jefferson, genomics represents a fascinatingly innovative area of healthcare. As the price of genome sequencing has been in free fall for years, the start-up scene is bursting from transformative power. Let’s look at some of the most amazing ventures in genomics! The amazing journey of genome sequencing Genome sequencing has been on an amazing scientific as well as economic journey for the last three decades. The Human Genome Project began in 1990 with the aim of mapping the whole structure of the human genome and sequencing ...
Source: The Medical Futurist - Category: Information Technology Authors: Tags: Genomics Personalized Medicine AI artificial intelligence bioinformatics cancer DNA dna testing DTC gc3 genetic disorders genetics genome sequencing personal genomics precision medicine Source Type: blogs
By, SAURABH JHA MD Recently, the Harvard Chan School of Public Health, in their press release, reported about the effect of surgical checklists in South Carolina. The release was titled, “South Carolina hospitals see major drop in post-surgical deaths with nation’s first proven statewide Surgical Safety Checklist Program.” The Health News Review, for which I review, grades coverage of research in the media. Based on their objective criteria, the Harvard press release would not score highly. The title exudes certainty – “nation’s first proven.” The study, not being a randomized cont...
Source: The Health Care Blog - Category: Consumer Health News Authors: Tags: Uncategorized Source Type: blogs
Atovaquone proves effective in wide range of cancers Related items from OnMedica Malaria prophylaxis Put case for adding leukaemia drug to Cancer Drugs Fund, NICE tells company Study shows huge global variation in cancer drug costs Statins might not cut colorectal cancer risk after all Aspirin trialled to see if it prevents cancer recurrence
Source: OnMedica Latest News - Category: UK Health Source Type: news
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