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A formal [2 + 2 + 2] cycloaddition reaction between a 1,3-dione, an olefin, and molecular oxygen mediated by light is reported, which delivers endoperoxides in good yield through the formation of two C-O and one C-C bond in one step. The resulting 1,2-dioxanes are stable compounds and can be further derivatized at the hemiacetal position via alkylation or acetylation. All compounds have been evaluated against Plasmodium falciparum, and the best compound displayed an IC50-value of 180 nM. A potential mechanistic rationale for the formation of these compounds is presented.
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Name: Organic letters
We describe the design and application of tailored aminoallyl precursors for catalytic (3+2) cycloaddition with conjugated dienes via a Pd-aminoallyl intermediate. The new cycloaddition reactions over...
A TiCl-promoted cascade formal [3 + 2] cycloaddition/double ring-opening/chlorination of 2-furylcyclobutanols with alkyl or aryl azides is described. This highly efficient transformation involves the ...
Under cooperative catalysis of iridium and a Brønsted acid, different C4-substituted azlactones react with vinyl benzoxazinones via a formal [4+2] cycloaddition or substitution reaction in a chemo- a...
An efficient method for preparing highly functionalized chiral nonspiro-phosphonylpyrazolines via an asymmetric formal 1,3-dipolar cycloaddition reaction of α-diazomethylphosphonate with activated, a...
The asymmetric formal hydroamination of enamines using Cu-H catalyst is reported. The method provides a straightforward and efficient approach for the synthesis of chiral 1,2-dialkyl amines in good yi...
The newly introduced antimalarial drug artemether-lumefantrine is currently recommended as second line antimalarial in Sudan. Recurrent infection after treatment with this drug has been as...
The study compares the efficacy of bowel cleansing between the standard preparation (2 L polyethylene glycol electrolyte solution, 2 L PEG-ELS), low-volume preparation (10 mg bisacodyl plu...
Background: - The disease malaria can cause very serious health problems. Researchers want to see if malaria affects the way T cells and vaccines work in the body. If it does, they may ne...
A study that seeks to establish an effective way of preventing anaemia in children at the community level using two known interventions - Iron supplementation and or antimalarial. Children...
Although adequate bowel preparation is essential for successful colonoscopy, the 23% of patients had shown inadequate bowel preparation. Inadequate bowel preparation may results in incompl...
Formal instruction, learning, or training in the preparation, dispensing, and proper utilization of drugs in the field of medicine.
Formal education and training in preparation for the practice of a profession.
A biguanide compound which has little antimalarial activity until metabolized in the body to the active antimalarial agent cycloguanil. The usefulness of proguanil is limited by the rapid development of drug resistance by the malarial parasite. The hydrochloride is used for the casual prophylaxis of falciparum malaria, to suppress other forms of malaria, and to reduce transmission of infection (From Martindale, The Extra Pharmacopoeia, 30th ed, p405)
Synthetic compounds that are analogs of the naturally occurring prostaglandin endoperoxides and that mimic their pharmacologic and physiologic activities. They are usually more stable than the naturally occurring compounds.
Interactional process combining investigation, discussion, and agreement by a number of people in the preparation and carrying out of a program to ameliorate conditions of need or social pathology in the community. It usually involves the action of a formal political, legal, or recognized voluntary body.
Malaria is a serious tropical disease spread by mosquitoes. If malaria is not diagnosed and treated promptly, it can be fatal. What causes malaria? Malaria is caused by a type of parasite known as Plasmodium. There are many different types of Plasmod...