Photooxygenation of 2-phenylnorbornene 1 in the presence of 30% aqueous hydrogen peroxide afforded 1,2-bishydroperoxide 3, which could be cycloalkylated on treatment with silver oxide and a 1,omega-diiodoalkane to provide the tricyclic peroxides 12. Trimethylsilylation of 3 followed by TMSOTf-catalyzed cyclocondensation with carbonyl compounds led to the formation of the tricyclic peroxides 14 containing a 1,2,4,5-tetroxepane structure. Photooxygenation of 1 in the presence of either unsaturated hydroperoxides or unsaturated alcohols followed by bis(collidine)iodine hexafluorophosphate promoted cyclization gave the corresponding cyclic peroxides 15-17. Several of these cyclic peroxides showed substantial antimalarial activity particularly in vitro.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1021/jm020387b | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Evaluating programmatic reactive focal drug administration impact on malaria incidence in northern Senegal: an interrupted time series analysis.
Malar J
January 2025
PATH, 2201 Westlake Ave Ste 200, Seattle, WA, 98121, USA.
Background: The World Health Organization conditionally recommends reactive drug administration to reduce malaria transmission in settings approaching elimination. However, few studies have evaluated the impact of reactive focal drug administration (rFDA) in sub-Saharan Africa, and none have evaluated it under programmatic conditions. In 2016, Senegal's national malaria control programme introduced rFDA, the presumptive treatment of compound members of a person with confirmed malaria, and reactive mass focal drug administration (rMFDA), an expanded effort including neighbouring compounds during an outbreak, in 10 low transmission districts in the north of the country.
View Article and Find Full Text PDFHospital attendance, malaria prevalence and self-medication with an antimalarial drug before and after the start of COVID-19 pandemic in a sentinel site for malaria surveillance in Gabon.
Malar J
January 2025
Department of Parasitology-Mycology and Tropical Medicine, Université Des Sciences de La Santé de Libreville, BP 4009, Libreville, Gabon.
Background: The negative impact of COVID-19 pandemic on healthcare service utilization has been reported in several countries. In Gabon, data on the preparedness for future pandemic are lacking. The aim of the present study was to assess the trends of hospital attendance, malaria and self-medication prevalences as well as ITN use before and during Covid-19 first epidemic waves in a paediatric wards of a sentinel site for malaria surveillance, in Libreville, Gabon.
View Article and Find Full Text PDFManzamine A: A Promising Marine-Derived Cancer Therapeutic for Multi-targeted Interactions with E2F8, SIX1, AR, GSK-3β, and V-ATPase - A Systematic Review.
Eur J Pharmacol
January 2025
Department of Urology, Brown Cancer Center, 505 S Hancock Street, Louisville, KY, USA. Electronic address:
Manzamine A, a natural compound derived from various sponge genera, features a β-carboline structure and exhibits a range of biological activities, including anti-inflammatory and antimalarial effects. Its potential as an anticancer agent has been explored in several tumor models, both in vitro and in vivo, showing effects through mechanisms such as cytotoxicity, regulation of the cell cycle, inhibition of cell migration, epithelial-to-mesenchymal transition (EMT), autophagy, and apoptosis through multi-target interactions of E2F transcriptional factors, ribosomal S6 kinases, androgen receptor (AR), SIX1, GSK-3β, V-ATPase, and p53/p21/p27 cascades. This systematic review evaluates existing literature on the potential application of this marine alkaloid as a novel cancer therapy, highlighting its promising ability to inhibit cancer cell growth while causing minimal side effects.
View Article and Find Full Text PDFGedunin Mitigates -Induced Skin Inflammation by Inhibiting the NF-κB Pathway.
Pharmaceuticals (Basel)
January 2025
Department of Molecular Bioscience, College of Biomedical Science, Kangwon National University, Chuncheon 24341, Republic of Korea.
: , a bacterium residing in hair follicles, triggers acne by inducing monocyte-mediated inflammatory cytokine production. Gedunin, a limonoid derived from (commonly known as neem), is renowned for its antifungal, antimalarial, anticancer, anti-inflammatory, and neuroprotective effects. However, its role in mitigating -induced skin inflammation remains unexplored.
View Article and Find Full Text PDFEllagic Acid from and Antimalarial Activity of Korean Medicinal Plants.
Molecules
January 2025
Department of Medical Environmental Biology and Tropical Medicine, School of Medicine, Kangwon National University, Chuncheon 24341, Republic of Korea.
This study investigates the antimalarial potential of extracts and compounds from various plants used in traditional Korean medicine, in response to the increasing resistance of to standard treatments such as chloroquine and artemisinin. The antimalarial activity screening was conducted on 151 extracts, identifying the top seven candidates, including (50% ethanol and 100% methanol extract), , (hot water and 50% ethanol extract), , and . Among these, was identified as the top priority for further analysis due to its high antimalarial activity and high yield of bioactive compounds.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!