Jing Li, Xiangyi Jiang, Shujing Xu, Q. Cui, Ruikun Du, Dongwei Kang, P. Zhan, L. Rong, Xin Liu
{"title":"Medicinal chemistry strategies in seeking coronavirus inhibitors","authors":"Jing Li, Xiangyi Jiang, Shujing Xu, Q. Cui, Ruikun Du, Dongwei Kang, P. Zhan, L. Rong, Xin Liu","doi":"10.16438/J.0513-4870.2020-0131","DOIUrl":"https://doi.org/10.16438/J.0513-4870.2020-0131","url":null,"abstract":"The epidemic caused by coronavirus poses a serious threat to human health, but there is no specific drug or vaccine for the treatment of this kind of virus infection Herein, this article selects typical case studies in recent years and reviews the medicinal chemistry strategies of anti-SARS-CoV, MERS-CoV and other coronavirus drugs from the perspective of medicinal chemistry, and tries to provide some clues to current drug research against-SARS-CoV-2","PeriodicalId":7092,"journal":{"name":"Acta pharmaceutica Sinica","volume":"67 1","pages":"537-553"},"PeriodicalIF":0.0,"publicationDate":"2020-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84048855","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Analysis of chemical drugs applied for clinical trial for the treatment of COVID-19","authors":"Chao Zhang, S. Chen, Jie Zhang, Ying Guo","doi":"10.16438/J.0513-4870.2020-0151","DOIUrl":"https://doi.org/10.16438/J.0513-4870.2020-0151","url":null,"abstract":"The Coronavirus Disease 2019 (COVID-19) caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has spread throughout China and many other countries around the world. The antivirals are important measures to this epidemic; however, there is no drug approved for against coronavirus yet. With the continuously rising number of confirmed/suspected cases of COVID-19, it is urgent to obtain antiviral drugs for the clinical treatment. In response to this situation, drug repurposing strategy becomes one of the best approaches for anti-SARS-CoV-2 drug discovery. By retrieving the clinical trials registered in Chinese Clinical Trial Registry and ClinicalTrials.gov, a total of 14 chemical drugs were registered for COVID-19. In this review, we summarize and analyze the 14 drugs' indications, targets, and research basis related to the activities against viral infections, esp. coronavirus infections. We are making efforts to understand the evidence basis of these drugs for the treatment of SARS-CoV-2 infection applied by various research and clinical institutions in response to this COVID-19 outbreak, and also providing clues for quick response to possible epidemic in future and reasonable expansion of the indications of drugs.","PeriodicalId":7092,"journal":{"name":"Acta pharmaceutica Sinica","volume":"33 1","pages":"355-365"},"PeriodicalIF":0.0,"publicationDate":"2020-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"90595048","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Xin-yang Wang, Min Chen, Duo Wang, Xiang-dong Chen, Yong Ling, Xiao-li Wang, Hui Wang
{"title":"[Synthesis and biological evaluation of novel pleuromutilin derivatives with nitrogen-containing heterocycles as antibacterial agents].","authors":"Xin-yang Wang, Min Chen, Duo Wang, Xiang-dong Chen, Yong Ling, Xiao-li Wang, Hui Wang","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>A series of new pleuromutilins derivatives were designed and synthesized through coupling 2-aminothiazole ring of WL001 with different nitrogen-containing substituted heterocycles in the side chain. Their biological activities were evaluated against both Gram-positive and Gram-negative clinical bacteria in vitro Most new compounds displayed specificity to certain strain of bacteria. Particularly, compounds with saturated nitrogen-containing heterocycles exhibited significant antibacterial activities (0.062 5-8 µg · mL(-1)) superior or similar to those of amoxicillin, tiamulin and levofloxcin. Furthermore, treatment with 15a and 15b having piperidine or morpholine residues also could effectively inhibit Gram-negative bacteria. Therefore, our novel findings may provide a new insight into the design of novel pleuromutilin derivatives and lay the basis for further studies on the treatment of drug-resistance of pathogenic bacteria.</p>","PeriodicalId":7092,"journal":{"name":"Acta pharmaceutica Sinica","volume":"50 10","pages":"1297-304"},"PeriodicalIF":0.0,"publicationDate":"2015-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138794630","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"[Effect of WS070117M1 on chronic obstructive pulmonary disease in mice and the underling mechanisms of anti-inflammation].","authors":"Shu-hua Cao, Ling-ling Xuan, Dong-mei Wang, Jian-lin Xie, Ren-tao Jiang, Jin-ye Bai, Song Wu, Qi Hou","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The aim of this study is to investigate the anti-inflammatory effect of the adenosine derivative N6-(3-hydroxylaniline) adenosine (WS070117M1) on cigarette smoke plus LPS (lipopolysaccharide)-induced chronic obstructive pulmonary disease (COPD) in mice and its mechanism. COPD model was established by exposing male BALB/c mice to cigarette smoke and challenged with LPS inhalation. Supernatants of bronchoalveolar lavage fluid (BALF) were harvested and IL-1β, IL-6, IL-8 and TGF-β1 levels were measured by ELISA (enzyme-linked immunesorbent assay). The number of total white blood cells and neutrophils in bronchoalveolar lavage fluid was counted separately. Lung tissue was stained with Mayer 's hematoxylin and eosin for histopathologic examination. pAMPKa protein expression and distribution of lung tissue were analyzed by immunohistochemistry method. In vitro, levels of AMPKα phosphorylation in phorbol-12- myristate-13-acetate (PMA) differentiated THP-1 cells was detected by immunohistochemistry, IL-8 level in supernatants of cigarette smoke condensate stimulating PMA differentiated THP-1 cells was measured by ELISA. The results showed that WS070117M1 treatment significantly activated AMPKa in the lung tissue. It also resulted in down regulation of IL-1β, IL-6, IL-8 and TGF-β1 levels in bronchoalveolar lavage fluid and IL-8 level in cigarette smoke condensate stimulating PMA differentiated THP-1 cells. In addition, WS070117M1 could inhibit the recruitment of total white blood cells and neutrophils. These results suggest that WS070117M1 may alleviate the airway inflammation by activating AMPK in the lung tissue.</p>","PeriodicalId":7092,"journal":{"name":"Acta pharmaceutica Sinica","volume":"50 8","pages":"986-92"},"PeriodicalIF":0.0,"publicationDate":"2015-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138794633","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Wen-jie Lu, Qi-kang Ya, Jia-yuan Chen, Bu-ming Liu
{"title":"[A new flavonol glycoside from Baeckea Frutescens L].","authors":"Wen-jie Lu, Qi-kang Ya, Jia-yuan Chen, Bu-ming Liu","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>To study the chemical constituents of the traditional Chinese herb Baeckea Frutescens L., a new flavonol glycoside, named 6, 8-dimethylkaempferol-3-O-alpha-L-rhamnoside (1), together with seven known compounds: quercetin (2), quercetin-3-O-alpha-L-rhamnoside (3), myricetin (4), myricetin-3-O-alpha-L-rhamnoside (5), gallic acid (6), ursolic acid (7) and 1,3-dihydroxy-2-(2'-methoxylpropionyl)-5-methoxy-6-methylbenzene (8) were isolated by using silica gel column chromatography, polyamide column chromatography and recrytallization. Their structures were identified on the basis of physicochemical properties and spectroscopic analysis. Among them, compounds 2-7 were isolated from this plant for the first time and compound 8 was first isolated from plant.</p>","PeriodicalId":7092,"journal":{"name":"Acta pharmaceutica Sinica","volume":"43 10","pages":"1032-5"},"PeriodicalIF":0.0,"publicationDate":"2008-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138794627","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Advances in chromatography","authors":"Zhou Th","doi":"10.1201/crcadvchroma","DOIUrl":"https://doi.org/10.1201/crcadvchroma","url":null,"abstract":"329 The volume of M.S. Tswett’s selected works pre pared by the Russian Academy of Sciences includes the major part of the body of the doctoral dissertation by the inventor of chromatography, defended in 1911. This voluminous dissertation was published as a sepa rate monograph (Khromofilly v Rastitel’nom i Zhivot nom Mire (Chromophylls in the Plant and Animal Kingdom), Warsaw, 1910)). Though the title of the book was not “chromatographic,” it described the results of the author’s work on the technique of chro matography. However, the first book devoted to this method is usually considered Zechmeister and Chol noky’s monograph published in German in 1937 [1]; it played a significant role in the development of chro matography, in the approval of its name, and the rec ognition of Tswett’s priority.","PeriodicalId":7092,"journal":{"name":"Acta pharmaceutica Sinica","volume":"6 1","pages":"976"},"PeriodicalIF":0.0,"publicationDate":"1983-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88167168","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}