Herein, we report the first palladium/MPAA catalyzed enantioselective C-H activation/[4 + 1] annulation of diarylmethyltriflamide and olefins to construct chiral -1,3-disubstituted isoindoline derivatives. The use of a readily accessible mono-N-protected amino acid as a chiral ligand improves the efficiency and enantioselectivity of the catalytic transformation. The developed method provides access to both enantiomers of a product using either d or l-phenylalanine derivative as a chiral ligand facilitating the synthesis of both optically active 1,3-disubstituted isoindoline derivatives.
View Article and Find Full Text PDFChem Commun (Camb)
October 2021
The enantioselective first total syntheses of marine pentacyclic indolosesquiterpenoids xiamycins D (4) and E (5) have been described for the first time to the best of our knowledge. The synthetic approach was designed to feature functionalization of enantiopure Wieland-Miescher ketone, Michael addition followed by Heck-type annulation/aromatization, regioselective sp(C-H) activation, benzylic oxidation and diastereoselective reduction.
View Article and Find Full Text PDFUse of nitromethane as an electrophilic methylene source for the synthesis of symmetrical dithioacetals and bisarylmethanes has been showcased using Sc(OTf) as a catalyst. The procedure allows straightforward access to the densely functionalized dithioacetals and bisarylmethanes under mild conditions. Additionally, the method has been applied for the synthesis of antimalarial tetramethyl mellotojaponin C and anticancer dimeric phloroglucinol derivative.
View Article and Find Full Text PDFWHO South East Asia J Public Health
January 2014
Background: Vector-borne diseases (VBDs) caused by parasites and viruses are a major cause of morbidity and mortality in Madhya Pradesh (MP), central India. These diseases are malaria, lymphatic filariasis, dengue and chikungunya. Epidemiological information is lacking on different VBDs that are commonly prevalent in rural-tribal areas of MP, except on malaria.
View Article and Find Full Text PDFBackground: Malaria due to both Plasmodium falciparum and Plasmodium vivax is a major public health problem in India. The quantification of malaria transmission for the classification of malaria risk has long been a concern for epidemiologists. Results are presented from 30 cross-sectional surveys which measured spleen rates (SR) and infant parasite rates (IPR) in the forested districts of Madhya Pradesh during malaria outbreaks to assess whether both IPR and SR can still be used as indicators of malaria endemicity as spleen examination has lost much of its value as an epidemiological indicator in areas where anti-malarials drugs are widely used.
View Article and Find Full Text PDFThe aim of this preliminary study was to investigate the plasma cytokine profiles in a group of patients suffering from Plasmodium vivax malaria during the peak of its transmission season. Plasma samples of 173 P. vivax patients and 34 healthy individuals were analyzed for IFN-gamma, TNF-alpha, IL-10 and IP-10 levels by ELISA.
View Article and Find Full Text PDFBackground: Past studies in India included only symptomatic pregnant women and thus may have overestimated the proportion of women with malaria. Given the large population at risk, a cross sectional study was conducted in order to better define the burden of malaria in pregnancy in Jharkhand, a malaria-endemic state in central-east India.
Methods: Cross-sectional surveys at antenatal clinics and delivery units were performed over a 12-month period at two district hospitals in urban and semi-urban areas, and a rural mission hospital.
A study on the clinicoepidemiology of cerebral malaria (CM) and mild malaria (MM) among adults and children attending NSCB medical college hospital Jabalpur and civil hospital Maihar, Satna, in central India was undertaken. Of 1,633 patients, 401 were Plasmodium falciparum and 18 P. vivax.
View Article and Find Full Text PDFBackground: Malaria presents a diagnostic challenge in tribal belt of central India where two Plasmodium species, Plasmodium falciparum and Plasmodium vivax, are prevalent. In these areas, rapid detection of the malaria parasites and early treatment of infection remain the most important goals of disease management. Therefore, the usefulness of a new rapid diagnostic (RDT), the First Response(R) Combo Malaria Ag (pLDH/HRP2) card test was assessed for differential diagnosis between P.
View Article and Find Full Text PDFAzithromycin has demonstrated activity in a prevention of Plasmodium vivax infection, but no controlled treatment studies have been performed. We conducted a double-blinded trial in P. vivax malaria in which patients were randomized to either azithromycin 1,000 mg q.
View Article and Find Full Text PDFBackground: Azithromycin has demonstrated in vitro and in vivo activity against Plasmodium falciparum, but small treatment studies have given mixed results.
Methods: Participants with fever and with both a blood smear and a rapid diagnostic test positive for falciparum malaria were randomly assigned to groups that were treated with either azithromycin or chloroquine or to matched groups receiving a placebo. After an interim analysis, open-label combination therapy with both drugs was initiated.