Aryl azides were treated with allenylmagnesium bromide to generate 1,5-disubstituted butynyl 1,2,3-triazoles in a domino fashion, which upon Cu(I) catalyzed 1,3-dipolar cycloaddition with aryl azides afforded novel bis-1,2,3-triazoles in quantitative yields. The final products were analyzed for their antimicrobial activities against a panel of bacterial and fungal strains which revealed the products to be potent antimicrobials.
Objectives: The objectives of the study were the gas chromatography-mass spectrometry (GC-MS) identification and comparison of the chemical constituents, evaluation of the antifungal and anticancer activities of two species of genus Chenopodium, for example, Chenopodium ambrosioides (Ca) and Chenopodium botrys (Cb) growing in Kashmir, Himalayan region.Methods: The hydrodistilled essential oil of Ca and Cb was subjected to GC-MS analysis and antifungal activity for minimum inhibitory concentration (MIC) determination against different human pathogenic fungal strains using broth microdilution assay in 96-well microtiter plates as per the protocol of the clinical and laboratory standards institute (2008 M27-A3). The anti-proliferative ability of the essential oils was also evaluated against the two cell lines MCF-7 (human mammary carcinoma cells) and A549 (Human lung adenocarcinoma epithelial cells).Results: A total of 34 compounds identified in Ca with α-terpinene (37.17%), isoascaridole (20.48%), and ascaridole (14.83%) as the key compounds. The key compounds of Cb were shyobunol (18.91%), and hedycaryol (9.51%), germacrene-D-4-ol (8.57%), with 65 identified compounds. Both the species were found to have comparable antifungal activities against human pathogenic fungi with MIC80 values in the range of 0.031 mg/ml– 0.256 mg/ml for Ca and 0.031 mg/ml–0.126 mg/ml in case of Cb. Maximum anti-proliferative activity was observed at 125 μg/ml concentration in A549 cell line, while as the oils inhibited the growth of MCF-7 cell line at a lower concentration of 31.25 μg/ml.Conclusion: The essential oils of Ca and Cb were found to have potent anticancer and antifungal activities and can have potential use as a natural fungicide.
SARS-CoV-2, the virus that causes coronavirus disease 2019 (COVID-19), was first reported in Wuhan, China, in December 2019. Since then, the virus has stretched its grip to almost all the countries in the world, affecting millions of people and causing enormous casualties. The World Health Organization (WHO) declared COVID-19 a pandemic on March 11, 2019. As of June 12, 2020, almost 7.30 million people have already been infected globally, with 413,000 reported casualties. In the United States alone, 2.06 million people have been infected and 115,000 have succumbed to this pandemic. A multipronged approach has been launched toward combating this pandemic, with the main focus on exhaustive screening, developing efficacious therapies, and vaccines for long-term immunity. Several pharmaceutical companies in collaboration with various academic institutions and governmental organizations have started investigating new therapeutics and repurposing approved drugs so as to find fast and affordable treatments against this disease. The present communication is aimed at highlighting the efforts that are currently underway to treat or prevent SARS-CoV-2 infection, with details on the science, clinical status, and timeline for selected investigational drugs and vaccines. This article is going to be of immense help to the scientific community and researchers as it brings forth all the necessary clinical information of the most-talked-about therapeutics against SARS-CoV-2. All the details pertaining to the clinical status of each therapeutic candidate have been updated as of June 12, 2020.
The flowers of Artemisia dubia wall ex Bess., on hydrodistillation provided a refreshing violet-blue viscous essential oil with sweet woody odour. The oil was found to be a complex mixture of monoterpenes, sesquiterpenes and their esters. A total of 67 chemical constituents comprising 79.43 % of the oil were characterized with the help of gas chromatography and mass spectrometry (GC/MS). Major chemical constituents of the oil were characterized as nerylisovalerate (9.79 %), 1,8-cineole (8.32 %), neryl-2-methyl-butanoate (7.32 %), chamazulene (5.92 %), linalool (4.15 %), camphor (4.10 %), germacrene D (4.04 %), nerol (3.37 %), linalyl propionate (3.32 %). The investigations performed on the flower essential oil of A. dubia allowed the distinction of this plant growing in the temperate Kashmir region of western Himalayas from the same plant with different varieties growing in different parts of the world. The essential oil was evaluated for its antifungal activity against Candida species and was found to be active against the tested strains with more sensitivity against C. paropsilosis and C. krusei strains. The antioxidant activity evaluated by 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay and thiobarbituric acid reactive substances (TBARS) assay evidenced that the essential oil has moderate antioxidant activity. The antiproliferative ability of the oil was evaluated by MTT assay against the two cell lines A549 (human lung adenocarcinoma epithelial cells) and HCT-116 (human colon cancer cells). The essential oil effectively inhibits the growth of A549 and HCT-116 cancer cells at 62.5 and 31.25 μg/mL concentration, respectively.
A series of 1,5-diaryl pyrazoline pregnenolones were synthesized and screened for 5α-reductase inhibitory activities. Synthesis of the analogs is multistep and proceeds in good overall yields. The key step in the synthesis of 1,5-disubstituted pyrazolinyl pregnenolones (5a-l) is the heterocyclization of bezylidine derivatives (3) in presence of phenylhydrazines (4) through the initial formation of the phenylhydrazones, which undergo concomitant cyclization to generate the stable pyrazoline derivatives. All compounds were tested for their prostate cancer cell inhibitory, 5α-reductase and 17α-hydroxylase-C17,20-lyase inhibitory activities. Amongst all the compounds screened for their 5α-reductase inhibitory activities, compound 5c, 5e, 5g and 5l were found to be the most active. Further, compounds 5g and 5h were found to have moderate 17α-hydroxylase-C17,20-lyase inhibitory activities.
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