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Objective To study the antifungal activity of a new series of triazole compounds with n-propyl side chain and disubstituted benzyl structure. Methods Eleven target compounds were designed and synthesized. The structures were confirmed by 1H NMR, and some compounds were confirmed by 13C NMR or HRMS. Three fungal strains were selected as experimental strains, and the antifungal activity was tested in vitro according to the standardized antifungal sensitivity test method recommended by National Committee for Clinical Laboratory Standards (NCCLS). Results Compound B11 showed better activity against candida albicans SC5314 than fluconazole and was comparable to posaconazole; Compounds B10, B11 and B4 showed better activity against cryptococcus neoformanis H99 than fluconazole, while compounds B2, B3, B5, B6 and B7 showed similar activity to fluconazole against cryptococcus neoformanis H99; while all compounds showed poor activity against aspergillus fumigatus. Conclusion Some of the target compounds with n-propyl side chain and disubstituted benzyl group structure had certain antifungal activity and could be identified as potential lead antifungal drugs.
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ObjectiveTo investigate the epidemiological characteristics and analyze the incidence trend of SARS-CoV-2 infection in Shanghai， China， and compare with the characteristics of the infection in Jilin Province of China during the same period in 2022 and Wuhan at the beginning of 2020. MethodsInformation of new locally-transmitted confirmed SARS-CoV-2 cases， imported confirmed COVID-19 cases， local asymptomatic SARS-CoV-2 carriers and imported asymptomatic SARS-CoV-2 carriers in Shanghai from March 1 to April 18， 2022 was collected for descriptive analysis. ResultsFrom March 1 to April 18， 2022， a total of 397 933 locally-transmitted SARS-CoV-2 cases were reported in Shanghai. Of those， 27 613 were clinically confirmed cases and 21 were severe cases. Ten deaths were related to COVID-19. The pathogen is Omicron variant BA.2 of SARS-CoV-2. The number of the infected subjects increased rapidly after March 24 and lead to a disease outbreak. Severe and deceased cases had severe comorbidity and were mostly unvaccinated with SARS-CoV-2 vaccines. Asymptomatic SARS-CoV-2 carriers accounted for 93.06%， which is significantly higher than that in Jilin Province during the same period （48.07%， P<0.001）. Daily increase in the number of clinically confirmed COVID-19 cases in Shanghai in 2022 was much lower than that in Wuhan， Hubei Province， in 2020. Number of daily newly imported confirmed COVID-19 cases and imported asymptomatic SARS-CoV-2 carriers declined during this period. ConclusionThe Omicron variant in Shanghai 2022 is highly infectious and less pathogenic. Omicron variant BA.2 replicates rapidly in asymptomatic carriers， which makes the carriers the major source of infection. Full-term vaccination of inactivated SARS-CoV-2 vaccine might decrease the pathogenicity and fatality of SARS-CoV-2 variants. SARS-CoV-2 of the Omicron BA2 strain is likely transmitted through aerosols and droplets， which poses a great challenge to the control of the COVID-19 pandemic in large cities with high population density and sophisticated public transportation.
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Objective To optimize novel triazole antifungal compounds synthesis of key intermediates.Methods The or-thogonal experimental design is used,emphasizing on four factors including the reaction temperature,the weight ratio of mate-rial,reaction time and solvent on the yield.Results The effect of reaction temperature on the reaction yield is the most signifi-cant,followed by reaction time ;the weight ratio of material and solvent on the yield impact is not obvious.Conclusion The new technology has several advantages and yields up to about 50%,less reactive impurities,easy post processing.
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Fluconazole,the third generation of triazole-antifungal drug,becomes the first choice in the treatment of fun-gal infection due to its broad antifungal spectrum,good water solubility and low toxicity.With an increasingly drug-resistant strain,developing new fluconazole derivatives is becoming an attractive topic.This review mainly indicates that people can get new fluconazole derivatives used by clinic through structural modification of fluconazole,which will give clues for advanced re-search.
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Glycosylation is the key step of the synthesis of GM3 ,its reaction conditions are very harsh ,the stereoselec‐tivities are usually poor ,and the configuration of anomeric carbon is difficult to control .Whetherαglycosidic bond can be con‐structed efficiently in sialylation reactions is an important criteria used to evaluate the reaction quality .Studies of GM3 and de‐rivatives methods generally relates to following areas :the choice of the donor compounds and receptor compounds ,the control of stereoselectivity ,and the development of some new glycosidic reaction catalyst .In recent years ,important progress has been made in this research area .Now ,we predominately make a summary and review on the progress of methods for the synthesis of GM3 and derivatives .
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Objective Anthrax is an anthropozoonosis caused by the bacterium Bacillus anthracis .Bacillus anthracis is an aerobic ,spore-forming ,rod-shaped bacterium ,which infects human through ingestion or inhalation of the spores .The exos-porium of spores of Bacillus anthracis contains tetrasaccharide antigen with specific chemical structure ,which can be used in preparation of glycoconjugates vaccines ,inducing an immune response .This paper reviewed articles in the last decade that re-ported research advances in chemical synthesis of anthrax tetrasaccharide ,presented the methods for synthesis ,and compared the advantages and limitations among different methods .