16 results on '"Guo, Meng"'
Search Results
2. Enhanced Selectivity in 4-Quinolone Formation: A Dual-Base System for Palladium-Catalyzed Carbonylative Cyclization with Fe(CO)5
- Author
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Guo, Meng, primary, Wu, Dou, additional, Yang, Hongyu, additional, Zhang, Xiao, additional, Xue, Dong-Xu, additional, and Zhang, Weiqiang, additional
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- 2024
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3. The Tryptophan Metabolite Indole-3-Carboxaldehyde Alleviates Mice with DSS-Induced Ulcerative Colitis by Balancing Amino Acid Metabolism, Inhibiting Intestinal Inflammation, and Improving Intestinal Barrier Function
- Author
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Liu, Mingfei, primary, Wang, Yuxuan, additional, Xiang, Haixin, additional, Guo, Meng, additional, Li, Shirong, additional, Liu, Ming, additional, and Yao, Jingchun, additional
- Published
- 2023
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4. Integrating Multi-Type Component Determination and Anti-Oxidant/-Inflammatory Assay to Evaluate the Impact of Pre-Molting Washing on the Quality and Bioactivity of Cicadae Periostracum
- Author
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Guo, Meng-Fei, primary, Zhang, Huan-Huan, additional, Zhong, Ping, additional, Xu, Jin-Di, additional, Zhou, Shan-Shan, additional, Long, Fang, additional, Kong, Ming, additional, Mao, Qian, additional, and Li, Song-Lin, additional
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- 2022
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5. Design, Synthesis and Antibacterial Evaluation of 3-Substituted Ocotillol-Type Derivatives
- Author
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Kai-Yi Wang, Zhi-Wen Zhou, Heng-Yuan Zhang, Yu-Cheng Cao, Jin-Yi Xu, Cong Ma, Qing-Guo Meng, and Yi Bi
- Subjects
triterpenoid saponin ,ocotillol ,antibacterial activity ,synthesis ,structure-activity relationship ,Organic chemistry ,QD241-441 - Abstract
Antibiotic resistance has become a serious global problem that threatens public health. In our previous work, we found that ocotillol-type triterpenoid saponin showed good antibacterial activity. Based on preliminary structure-activity relationship, novel serious C-3 substituted ocotillol-type derivatives 7–26 were designed and synthesized. The in vitro antibacterial activity was tested on five bacterial strains (B. subtilis 168, S. aureus RN4220, E. coli DH5α, A. baum ATCC19606 and MRSA USA300) and compared with the tests on contrast. Among these derivatives, C-3 position free hydroxyl substituted compounds 7–14, showed good antibacterial activity against Gram-positive bacteria. Furthermore, compound 22 exhibited excellent antibacterial activity with minimum inhibitory concentrations (MIC) values of 2 μg/mL against MRSA USA300 and 4 μg/mL against B. subtilis. The structure-activity relationships of all current ocotillol-type derivatives our team synthesised were summarized. In addition, the prediction of absorption, distribution, metabolism, and excretion (ADME) properties and the study of pharmacophores were also conducted. These results can provide a guide to further design and synthesis works.
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- 2018
- Full Text
- View/download PDF
6. Synthesis and Antibacterial Evaluation of a Series of 11,12-Cyclic Carbonate Azithromycin-3-O-descladinosyl-3-O-carbamoyl Glycosyl Derivatives
- Author
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Chao-Ming Wang, Feng-Lan Zhao, Lei Zhang, Xiao-Yun Chai, and Qing-Guo Meng
- Subjects
azithromycin ,glycosyl derivatives ,synthesis ,antibacterial activity ,Organic chemistry ,QD241-441 - Abstract
A novel series of 11,12-cyclic carbonate azithromycin-3-O-descladinosyl-3-O-carbamoyl glycosyl derivatives were designed, synthesized, and evaluated for their antibacterial activities in vitro. Most of these compounds had significant antibacterial activity against seven kinds of susceptible strains. In particular, compound G1 exhibited the most potent activity against methicillin-resistant Streptococcus pneumoniae 943 (MIC: 1 μg/mL), Staphylococcus pneumoniae 746 (MIC: 2 μg/mL), Streptococcus pyogenes 447 (MIC: 8 μg/mL), and Escherichia coli 236 (MIC: 32 μg/mL), which were two-, four-, four-, four-, and eight-fold stronger activity than azithromycin, respectively. Additionally, compound G2 exhibited improved activity against methicillin-resistant Staphylococcus aureus MRSA-1 (MIC: 8 μg/mL), Streptococcus pneumoniae 943 (MIC: 2 μg/mL), Staphylococcus pneumoniae 746 (MIC: 2 μg/mL), and Escherichia coli 236 (MIC: 32 μg/mL), which were two-, two-, four-, and eight-fold better activity than azithromycin, respectively. As for methicillin-resistant Staphylococcus aureus MRSA-1, compound G6 presented the most excellent activity (MIC: 4 μg/mL), showing four-fold higher activity than azithromycin (MIC: 16 μg/mL) and erythromycin (MIC: 16 μg/mL). However, compared with other compounds, compounds G7 and G8 with the disaccharide side chain were observed the lower activity against seven strains.
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- 2017
- Full Text
- View/download PDF
7. Synthesis and Antibacterial Evaluation of Novel 3-Substituted Ocotillol-Type Derivatives as Leads
- Author
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Yi Bi, Xian-Xuan Liu, Heng-Yuan Zhang, Xiao Yang, Ze-Yun Liu, Jing Lu, Peter John Lewis, Chong-Zhi Wang, Jin-Yi Xu, Qing-Guo Meng, Cong Ma, and Chun-Su Yuan
- Subjects
ocotillol ,derivatives ,synthesis ,antibacterial activity ,synergistic effect ,Organic chemistry ,QD241-441 - Abstract
Due to the rapidly growing bacterial antibiotic-resistance and the scarcity of novel agents in development, bacterial infection is still a global problem. Therefore, new types of antibacterial agents, which are effective both alone and in combination with traditional antibiotics, are urgently needed. In this paper, a series of antibacterial ocotillol-type C-24 epimers modified from natural 20(S)-protopanaxadiol were synthesized and evaluated for their antibacterial activity. According to the screening results of Gram-positive bacteria (B. subtilis 168 and MRSA USA300) and Gram-negative bacteria (P. aer PAO1 and A. baum ATCC19606) in vitro, the derivatives exhibited good antibacterial activity, particularly against Gram-positive bacteria with an minimum inhibitory concentrations (MIC) value of 2–16 µg/mL. The subsequent synergistic antibacterial assay showed that derivatives 5c and 6c enhanced the susceptibility of B. subtilis 168 and MRSA USA300 to chloramphenicol (CHL) and kanamycin (KAN) (FICI < 0.5). Our data showed that ocotillol-type derivatives with long-chain amino acid substituents at C-3 were good leads against antibiotic-resistant pathogens MRSA USA300, which could improve the ability of KAN and CHL to exhibit antibacterial activity at much lower concentrations with reduced toxicity.
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- 2017
- Full Text
- View/download PDF
8. Design, Synthesis, and Antibacterial Evaluation of Novel Ocotillol Derivatives and Their Synergistic Effects with Conventional Antibiotics
- Author
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Cao Yucheng, Yi Bi, Zhuoyue Shi, Kaiyi Wang, Ruodong Wang, Qing-Guo Meng, and Doudou Zhang
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Methicillin-Resistant Staphylococcus aureus ,Staphylococcus aureus ,HA-MRSA ,Ginsenosides ,medicine.drug_class ,Antibiotics ,Pharmaceutical Science ,Microbial Sensitivity Tests ,Drug resistance ,Pharmacology ,medicine.disease_cause ,Article ,antibiotics ,Analytical Chemistry ,Structure-Activity Relationship ,Minimum inhibitory concentration ,QD241-441 ,Kanamycin ,ocotillol-type derivatives ,Drug Discovery ,medicine ,Physical and Theoretical Chemistry ,Antibacterial agent ,structural modification ,Molecular Structure ,Chemistry ,Chloramphenicol ,Organic Chemistry ,Drug Synergism ,Anti-Bacterial Agents ,Chemistry (miscellaneous) ,Drug Design ,Molecular Medicine ,synergistic effects ,Antibacterial activity ,medicine.drug - Abstract
The improper use of antibiotics has led to the development of bacterial resistance, resulting in fewer antibiotics for many bacterial infections. Especially, the drug resistance of hospital-acquired methicillin-resistant Staphylococcus aureus (HA-MRSA) is distinctly serious. This research designed and synthesized two series of 3-substituted ocotillol derivatives in order to improve their anti-HA-MRSA potency and synergistic antibacterial activity. Among the synthesized compounds, 20–31 showed minimum inhibitory concentration (MIC) values of 1–64 µg/mL in vitro against HA-MRSA 18–19, 18–20, and S. aureus ATCC29213. Compound 21 showed the best antibacterial activity, with an MIC of 1 μg/mL and had synergistic inhibitory effects. The fractional inhibitory concentration index (FICI) value was 0.375, when combined with chloramphenicol (CHL) or kanamycin (KAN). The structure–activity relationships (SARs) of ocotillol-type derivatives were also summarized. Compound 21 has the potential to be developed as a novel antibacterial agent or potentiator against HA-MRSA.
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- 2021
9. Design, Synthesis and Biological Evaluation of a New Series of 1-Aryl-3-{4-[(pyridin-2-ylmethyl)thio]phenyl}urea Derivatives as Antiproliferative Agents
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Xiaoping Liu, Jian Feng, Chun Hu, Xiaoyu Tan, Ning Ding, Qing-Guo Meng, Li Yongpeng, Chuanming Zhang, and Jin Zhe
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antiproliferative activity ,synthesis ,Stereochemistry ,Pharmaceutical Science ,Thio ,Antineoplastic Agents ,urea ,Chemistry Techniques, Synthetic ,Article ,Analytical Chemistry ,lcsh:QD241-441 ,03 medical and health sciences ,chemistry.chemical_compound ,Structure-Activity Relationship ,0302 clinical medicine ,lcsh:Organic chemistry ,Cell Line, Tumor ,Drug Discovery ,Humans ,Physical and Theoretical Chemistry ,IC50 ,030304 developmental biology ,A549 cell ,antiproliferative agent ,0303 health sciences ,Trifluoromethyl ,Molecular Structure ,Aryl ,Phenylurea Compounds ,Spectrum Analysis ,Organic Chemistry ,Cell Cycle ,apoptosis ,Hydrogen Bonding ,In vitro ,chemistry ,Chemistry (miscellaneous) ,030220 oncology & carcinogenesis ,Drug Design ,Urea ,Molecular Medicine ,Drug Screening Assays, Antitumor ,Selectivity - Abstract
To discover new antiproliferative agents with high efficacy and selectivity, a new series of 1-aryl-3-{4-[(pyridin-2-ylmethyl)thio]phenyl}urea derivatives (7a&ndash, 7t) were designed, synthesized and evaluated for their antiproliferative activity against A549, HCT-116 and PC-3 cancer cell lines in vitro. Most of the target compounds demonstrated significant antiproliferative effects on all the selective cancer cell lines. Among them, the target compound, 1-[4-chloro-3-(trifluoromethyl)phenyl]-3-{4-{{[3-methyl-4-(2,2,2-trifluoroethoxy)pyridin-2-yl]methyl}thio}phenyl}urea (7i) was identified to be the most active one against three cell lines, which was more potent than the positive control with an IC50 value of 1.53 ±, 0.46, 1.11 ±, 0.34 and 1.98 ±, 1.27 &mu, M, respectively. Further cellular mechanism studies confirmed that compound 7i could induce the apoptosis of A549 cells in a concentration-dependent manner and elucidated compound 7i arrests cell cycle at G1 phase by flow cytometry analysis. Herein, the studies suggested that the 1-aryl-3-{4-[(pyridin-2-ylmethyl)thio]phenyl}urea skeleton might be regarded as new chemotypes for designing effective antiproliferative agents.
- Published
- 2019
10. Synthesis, Characterization, and Anticancer Activities Evaluation of Compounds Derived from 3,4-Dihydropyrimidin-2(1H)-one
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Hongbo Wang, Zong-liang Liu, Ye Liu, Yan Guo, Jiaqi Liu, Qing-Guo Meng, Ren-mei Zhang, and Yuan Sun
- Subjects
Alkylation ,Biginelli reaction ,Pharmaceutical Science ,Antineoplastic Agents ,Pyrimidinones ,010402 general chemistry ,01 natural sciences ,Article ,Catalysis ,Analytical Chemistry ,Polar surface area ,lcsh:QD241-441 ,chemistry.chemical_compound ,Mice ,lcsh:Organic chemistry ,Cell Line, Tumor ,Drug Discovery ,Structure–activity relationship ,Animals ,Humans ,Physical and Theoretical Chemistry ,010405 organic chemistry ,Tetrabutylammonium hydroxide ,Aryl ,structure-activity relationship ,Organic Chemistry ,Glioma ,3,4-dihydropyrimidin-2(1H)-ones ,in vivo experiments ,Combinatorial chemistry ,Xenograft Model Antitumor Assays ,0104 chemical sciences ,anticancer activities ,chemistry ,Chemistry (miscellaneous) ,Solvents ,Molecular Medicine ,N1-alkylation ,Pharmacophore ,Lead compound - Abstract
3,4-dihydropyrimidin-2(1H)-one compounds (DHPMs) possess extensive biological activities and are mainly prepared via Biginelli reaction and N-alkylation. In the present study, selective alkylation of N1 was investigated by using tetrabutylammonium hydroxide. In vitro cytotoxicity study on all synthesized compounds demonstrated that introduction of the aryl chain in the R3 as well as the low electron-donating group in the R1 of DHPMs contributed to the anti-proliferative potency. A larger value of the partition coefficient (Log P) and suitable polar surface area (PSA) values were both found to be important in order to maintain the antitumor activity. The results from in vivo study indicated the great potential of compound 3d to serve as a lead compound for novel anti-tumor drugs to treat glioma. Pharmacophore study regarding the structure-activity relations of DHPMs were also conducted. Our results here could provide a guide for the design of novel bioactive 3,4-dihydropyrimidin-2(1H)-one compounds.
- Published
- 2019
11. Design, Synthesis, and Biological Evaluation of Novel Nitrogen Heterocycle-Containing Ursolic Acid Analogs as Antitumor Agents
- Author
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Wang Wenzhi, Zhi Liu, Hongbo Wang, Qing-Guo Meng, and Lei Lei
- Subjects
synthesis ,Nitrogen ,Pharmaceutical Science ,Antineoplastic Agents ,01 natural sciences ,Article ,Analytical Chemistry ,lcsh:QD241-441 ,HeLa ,03 medical and health sciences ,chemistry.chemical_compound ,Mice ,Structure-Activity Relationship ,lcsh:Organic chemistry ,Ursolic acid ,In vivo ,Heterocyclic Compounds ,Neoplasms ,Drug Discovery ,Animals ,Humans ,antitumor activity ,Physical and Theoretical Chemistry ,IC50 ,030304 developmental biology ,Cell Proliferation ,ursolic acid analogues ,0303 health sciences ,biology ,Molecular Structure ,010405 organic chemistry ,Apoptosis Regulator ,Organic Chemistry ,apoptosis ,biology.organism_classification ,Xenograft Model Antitumor Assays ,Triterpenes ,0104 chemical sciences ,Piperazine ,chemistry ,Biochemistry ,Chemistry (miscellaneous) ,Apoptosis ,Cell culture ,Drug Design ,Molecular Medicine ,nitrogen heterocycles ,Drug Screening Assays, Antitumor ,HeLa Cells - Abstract
Nineteen ursolic acid analogues were designed, synthesized, and evaluated for their antiproliferative activity against the Hela and MKN45 cell lines. Some compounds containing a piperazine moiety displayed moderate to high levels of antitumor activities against the tested cancer cell lines. The most potent compound shares the IC50 value of 2.1 µ, M and 2.6 µ, M for the Hela and MKN45 cell lines, respectively. Further mechanism studies and in vivo antitumor studies have shown that it decreased the apoptosis regulator (BCL2/BAX) ratio, disrupted mitochondrial potential and induced apoptosis, and suppressed the growth of Hela xenografts in nude mice.
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- 2019
- Full Text
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12. Design, Synthesis and Antibacterial Evaluation of 3-Substituted Ocotillol-Type Derivatives
- Author
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Kaiyi Wang, Jinyi Xu, Yi Bi, Cao Yucheng, Hengyuan Zhang, Zhou Zhiwen, Qing-Guo Meng, and Cong Ma
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0301 basic medicine ,Staphylococcus aureus ,Ginsenosides ,synthesis ,Pharmaceutical Science ,Microbial Sensitivity Tests ,Gram-Positive Bacteria ,01 natural sciences ,Article ,Analytical Chemistry ,lcsh:QD241-441 ,03 medical and health sciences ,Antibiotic resistance ,lcsh:Organic chemistry ,antibacterial activity ,Drug Discovery ,Escherichia coli ,Structure–activity relationship ,Physical and Theoretical Chemistry ,triterpenoid saponin ,ADME ,Triterpenoid saponin ,chemistry.chemical_classification ,biology ,Molecular Structure ,010405 organic chemistry ,Chemistry ,structure-activity relationship ,Organic Chemistry ,biology.organism_classification ,Combinatorial chemistry ,In vitro ,0104 chemical sciences ,Anti-Bacterial Agents ,ocotillol ,030104 developmental biology ,Chemistry (miscellaneous) ,Molecular Medicine ,Pharmacophore ,Antibacterial activity ,Bacteria ,Bacillus subtilis - Abstract
Antibiotic resistance has become a serious global problem that threatens public health. In our previous work, we found that ocotillol-type triterpenoid saponin showed good antibacterial activity. Based on preliminary structure-activity relationship, novel serious C-3 substituted ocotillol-type derivatives 7&ndash, 26 were designed and synthesized. The in vitro antibacterial activity was tested on five bacterial strains (B. subtilis 168, S. aureus RN4220, E. coli DH5&alpha, A. baum ATCC19606 and MRSA USA300) and compared with the tests on contrast. Among these derivatives, C-3 position free hydroxyl substituted compounds 7&ndash, 14, showed good antibacterial activity against Gram-positive bacteria. Furthermore, compound 22 exhibited excellent antibacterial activity with minimum inhibitory concentrations (MIC) values of 2 &mu, g/mL against MRSA USA300 and 4 &mu, g/mL against B. subtilis. The structure-activity relationships of all current ocotillol-type derivatives our team synthesised were summarized. In addition, the prediction of absorption, distribution, metabolism, and excretion (ADME) properties and the study of pharmacophores were also conducted. These results can provide a guide to further design and synthesis works.
- Published
- 2018
- Full Text
- View/download PDF
13. Synthesis and Antibacterial Evaluation of Novel 3-Substituted Ocotillol-Type Derivatives as Leads
- Author
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Chun-Su Yuan, Chong-Zhi Wang, Xiao Yang, Qing Guo Meng, Peter J. Lewis, Xian Xuan Liu, Jin Yi Xu, Heng Yuan Zhang, Jing Lu, Cong Ma, Ze Yun Liu, and Yi Bi
- Subjects
0301 basic medicine ,Ginsenosides ,synthesis ,medicine.drug_class ,Antibiotics ,Pharmaceutical Science ,Microbial Sensitivity Tests ,Biology ,01 natural sciences ,Analytical Chemistry ,Microbiology ,lcsh:QD241-441 ,03 medical and health sciences ,Structure-Activity Relationship ,antibacterial activity ,synergistic effect ,lcsh:Organic chemistry ,Drug Discovery ,medicine ,Physical and Theoretical Chemistry ,chemistry.chemical_classification ,Molecular Structure ,010405 organic chemistry ,Chloramphenicol ,Communication ,Organic Chemistry ,Kanamycin ,Drug Synergism ,biochemical phenomena, metabolism, and nutrition ,biology.organism_classification ,In vitro ,0104 chemical sciences ,Amino acid ,Anti-Bacterial Agents ,ocotillol ,030104 developmental biology ,chemistry ,Chemistry (miscellaneous) ,derivatives ,Molecular Medicine ,Epimer ,Antibacterial activity ,Bacteria ,medicine.drug - Abstract
Due to the rapidly growing bacterial antibiotic-resistance and the scarcity of novel agents in development, bacterial infection is still a global problem. Therefore, new types of antibacterial agents, which are effective both alone and in combination with traditional antibiotics, are urgently needed. In this paper, a series of antibacterial ocotillol-type C-24 epimers modified from natural 20(S)-protopanaxadiol were synthesized and evaluated for their antibacterial activity. According to the screening results of Gram-positive bacteria (B. subtilis 168 and MRSA USA300) and Gram-negative bacteria (P. aer PAO1 and A. baum ATCC19606) in vitro, the derivatives exhibited good antibacterial activity, particularly against Gram-positive bacteria with an minimum inhibitory concentrations (MIC) value of 2–16 µg/mL. The subsequent synergistic antibacterial assay showed that derivatives 5c and 6c enhanced the susceptibility of B. subtilis 168 and MRSA USA300 to chloramphenicol (CHL) and kanamycin (KAN) (FICI < 0.5). Our data showed that ocotillol-type derivatives with long-chain amino acid substituents at C-3 were good leads against antibiotic-resistant pathogens MRSA USA300, which could improve the ability of KAN and CHL to exhibit antibacterial activity at much lower concentrations with reduced toxicity.
- Published
- 2017
14. Synthesis, Characterization, and Biological Activity of a Novel Series of Benzo[4,5]imidazo[2,1-b]thiazole Derivatives as Potential Epidermal Growth Factor Receptor Inhibitors
- Author
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Qingqing Ma, Deng Xinshan, Ce Wang, Xiaoyu Tan, Qing-Guo Meng, Chun Hu, Jin Zhe, and Tiantian An
- Subjects
synthesis ,Pharmaceutical Science ,Antineoplastic Agents ,Article ,Analytical Chemistry ,lcsh:QD241-441 ,HeLa ,03 medical and health sciences ,chemistry.chemical_compound ,0302 clinical medicine ,Gefitinib ,lcsh:Organic chemistry ,Neoplasms ,Acetamides ,Drug Discovery ,Human Umbilical Vein Endothelial Cells ,medicine ,Humans ,antitumor activity ,Epidermal growth factor receptor ,Physical and Theoretical Chemistry ,Thiazole ,030304 developmental biology ,EGFR inhibitors ,0303 health sciences ,biology ,Organic Chemistry ,Biological activity ,molecular docking ,biology.organism_classification ,ErbB Receptors ,Gene Expression Regulation, Neoplastic ,Molecular Docking Simulation ,Thiazoles ,chemistry ,Biochemistry ,Chemistry (miscellaneous) ,Cell culture ,030220 oncology & carcinogenesis ,biology.protein ,Molecular Medicine ,Human umbilical vein endothelial cell ,HeLa Cells ,heterocycle ,medicine.drug - Abstract
Based on the analysis of epidermal growth factor receptor (EGFR) complexes with gefitinib with molecular docking, the scaffold-hopping strategy, combination of the active substructures, and structural optimization of EGFR inhibitors, a novel series of benzo[4,5]imidazo[2,1-b]thiazole derivatives was designed, synthesized, and evaluated for antitumor activity in human cancer cell lines and cellular toxicity against human normal cell lines using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) colorimetric assay and EGFR inhibitory activities in vitro. Some target compounds such as 2-(benzo[4,5]imidazo[2,1-b]thiazol-3-yl)-N-(2-hydroxyphenyl)acetamide (D04) and 2-(benzo[4,5]imidazo[2,1-b]thiazol-3-yl)-N-(naphthalen-1-yl)acetamide (D08) have shown significant antitumor activity against the EGFR high-expressed human cell line HeLa. All the target compounds showed hardly any antitumor activity against the EGFR low-expressed human cell line HepG2, and nearly no cellular toxicity against the human normal cell lines HL7702 and human umbilical vein endothelial cell lines (HUVEC). The inhibitory activities against EGFR kinase in vitro of the three target compounds were greatly consistent with the anti-proliferative activities. The preliminary structure&ndash, activity relationships of the target compounds were summarized. Conclusively, the novel benzo[4,5]imidazo[2,1-b]thiazole derivatives as novel potential EGFR inhibitors may be used as the potential lead compounds for the development of antitumor agents.
- Published
- 2019
15. Development of Functional Phthalocyanine-Based Associate towards an Effective Fluorimetric Detection of Hg(II)
- Author
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Du, Guang-Xin, primary, Zhou, Tao, additional, Guo, Meng-Lin, additional, Huang, Ping, additional, Deng, Ya-Bin, additional, and Li, Dong-Hui, additional
- Published
- 2018
- Full Text
- View/download PDF
16. Synthesis and Antibacterial Evaluation of a Series of 11,12-Cyclic Carbonate Azithromycin-3-Odescladinosyl-3-O-carbamoyl Glycosyl Derivatives.
- Author
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Chao-Ming Wang, Feng-Lan Zhao, Lei Zhang, Xiao-Yun Chai, and Qing-Guo Meng
- Subjects
AZITHROMYCIN ,CARBAMOYL compounds ,GLYCOSIDES ,SACCHARIDES ,CHEMICAL synthesis ,ANTIBACTERIAL agents - Abstract
A novel series of 11,12-cyclic carbonate azithromycin-3-O-descladinosyl-3-O-carbamoyl glycosyl derivatives were designed, synthesized, and evaluated for their antibacterial activities in vitro. Most of these compounds had significant antibacterial activity against seven kinds of susceptible strains. In particular, compound G1 exhibited the most potent activity against methicillin-resistant Streptococcus pneumoniae 943 (MIC: 1 μg/mL), Staphylococcus pneumoniae 746 (MIC: 2 μg/mL), Streptococcus pyogenes 447 (MIC: 8 μg/mL), and Escherichia coli 236 (MIC: 32 μg/mL), which were two-, four-, four-, four-, and eight-fold stronger activity than azithromycin, respectively. Additionally, compound G2 exhibited improved activity against methicillin-resistant Staphylococcus aureus MRSA-1 (MIC: 8 μg/mL), Streptococcus pneumoniae 943 (MIC: 2 μg/mL), Staphylococcus pneumoniae 746 (MIC: 2 μg/mL), and Escherichia coli 236 (MIC: 32 μg/mL), which were two-, two-, four-, and eight-fold better activity than azithromycin, respectively. As for methicillin-resistant Staphylococcus aureus MRSA-1, compound G6 presented the most excellent activity (MIC: 4 μg/mL), showing four-fold higher activity than azithromycin (MIC: 16 μg/mL) and erythromycin (MIC: 16 μg/mL). However, compared with other compounds, compounds G7 and G8 with the disaccharide side chain were observed the lower activity against seven strains. [ABSTRACT FROM AUTHOR]
- Published
- 2017
- Full Text
- View/download PDF
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