检索结果-南通市图书馆

Design,synthesis and in vitro evaluation of mono(2,2,2-trifluoroethyl)esters,mono L-amino acid ester prodrugs of acyclic nucleoside phosphonates as anti-HBV agents

在线全文

学校读者我要写书评

暂无评论

Chinese Chemical Letters 2011年第12期22卷 1387-1390页

作者： Xiao Zhong Fu yu Ou Jan Xin yu she yang School of Pharmacy Guiyang Medical CollegeGuiyang 550004China Shanghai Fudan-yueda Bio-Tech Co. Ltd.Shanghai 201203China State Key Laboratory of Drug Research Shanghai Institute of Materia MedicaShanghai Institute for Biological Sciences Chinese Academy of ScienceShanghai 201203China

A series of novel mono（2,2,2-trifluoroethyl） esters,mono L-amino acid ester prodrugs of acyclic nucleoside phosphonates was synthesized and their in vitro anti-HBVactivity was evaluated in HepG 2 2.2.15 *** 1d exhibited more potent anti-HBV activity and lower cytotoxicity than those of adefovir dipivoxil and alamifovir（MCC-478） with EC_（50） and CC_（50） values of 0.01μmol/L and 8000μmol/L respectively.

关键词： Acyclic nucleoside phosphonates L-Amino acid Prodrug

An Efficient Process for Preparing 4-Methyl-2-phenyl Piperazine Hydrochloride and its Derivatives

在线全文

学校读者我要写书评

暂无评论

Chinese Chemical Letters 2003年第4期14卷 365-367页

作者： Bai Shu GUO yu she yang Ru yun JI Institute of Materia Medica Shanghai Institutes for Biological SciencesChinese Academy of SciencesShanghai 200031

An improved method for preparation of 4-methyl-2-phenyl piperazine and its derivatives with higher yield and inexpensive reagents was developed, the products were characterized by 1H-NMR and MS.

关键词： Methyl-2-phenyl piperazine mirtazapine intermediate.

Design and synthesis of novel antifungal triazole derivatives with good activity and water solubility

在线全文

学校读者我要写书评

暂无评论

Chinese Chemical Letters 2013年第4期24卷 303-306页

作者： Xu-Feng Cao Wen-Jing Chu Yong-Bing Cao yu-she yang State Key Laboratory of Drug Research Shanghai Institute of Materia MedicaChinese Academy of Sciences School of Pharmacy Second Military Medical University

In order to find novel antifungal agents with good activity and aqueous solubility, a series of SYN-2869 analogues containing a pyridine ring were synthesized and evaluated for their in vitro antifungal activity and water solubility. The results indicated that some compounds showed potent activity against six pathogenic fungi. In particular, the analogue 17a having an isobutyl substitution on the triazolone exhibited significant broad spectrum antifungal activity. In addition, the water solubility of compound l？a was sufficiently improved over SYN-2869.

关键词： SynthesisAntifungalSYN-2869 analoguesTriazoleWater solubility

Synthesis and antibacterial activity of pleuromutilin derivatives with novel C(14) side chain

在线全文

学校读者我要写书评

暂无评论

Chinese Chemical Letters 2012年第1期23卷 9-12页

作者： Li Qiang Fu Chen yu Ling Xing sheng Guo Hui Li He yu she yang Shanghai Institute of Materia Medica Chinese Academy of SciencesShanghai 201203China

In order to find novel antibacterial agents with superior antibacterial activity and overcoming multidrug resistance,a series of pleuromutilin derivatives with novel C（14） side chain were synthesized and evaluated for their in vitro antibacterial *** results of antibacterial acticities indicated that most of the derivatives showed potent activities against Gram-positive *** particular,compound lOd exhibited the most potent inhibitory activity compared with pleuromutilin and linezoid,emerged as potential molecule for further investigation.

关键词： Synthesis Pleuromutilin Novel side chains Antibacterial activity

Design, synthesis and antibacterial activity of novel pleuromutilin derivatives with 4H-pyran-4-one and pyridin-4-one substitution in the C-14 side chain

在线全文

学校读者我要写书评

暂无评论

Chinese Chemical Letters 2016年第2期27卷 235-240页

作者： Chen-yu Ling yun-Liang Tao Wen-Jing Chu Hui Wang Hai-Dong Wang yu-she yang State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Chinese Academy of Sciences School of Petrochemical Engineering Changzhou University Department of Microbiology China Pharmaceutical University

A series of novel pleuromutilin derivatives with 4H-pyran-4-one and pyridin-4-one substitution in the C-14 side chain have been designed and synthesized. In vitro antibacterial activity evaluation showed that most of the derivatives exhibited potent antibacterial activity against drug resistant Gram-positive strains. Compounds 12 a, 12 d, and 28 are the most active derivatives in this series, displaying activity comparable to that of retapamulin and BC-3781. As the metabolic stability of this series is not satisfactory, further modifications are going on to improve their pharmacokinetic profile.

关键词： Multi-drug resistant bacteria Pleuromutilin 4H-Pyran-4-one Antibacterial activity

Synthesis,pharmacokinetics and in vivo antifungal activity of the novel water-soluble prodrugs of itraconazole analogue YL-24

在线全文

学校读者我要写书评

暂无评论

Chinese Chemical Letters 2013年第4期24卷 321-324页

作者： yu Liu Xu-Feng Cao Xin Liu Yong-Bing Cao Wen-Jing Chu yu-she yang State Key Laboratory of Drug Research Shanghai Institute of Materia MedicaChinese Academy of Sciences School of Pharmacy Second Military Medical University State Key Laboratory of Drug Research Shanghai Institute of Materia MedicoChinese Academy of Sciences

To improve the aqueous solubility of an itraconazole analogue, compound 1 （YL-24）, a series of novel prodrugs were synthesized. Among these prodrugs, the phosphate disodium salt compound 7 exhibited excellent aqueous solubility （9.8 mg/mL） at near-neutral pH and sufficient stability in buffer solutions, along with favorable pharmacokinetic profiles. In particular, compounds 1 and 7 provided moderate survival efficacy in murine systemic Candida albicans SC5314 infection model, but their efficacy was weaker than that of fluconazole.

关键词： SynthesisAntifungalWater-soluble prodrugsltraconazole analogue

Synthesis and antibacterial activity of C-2(S)-substituted pleuromutilin derivatives

在线全文

学校读者我要写书评

暂无评论

Chinese Chemical Letters 2010年第5期21卷 507-510页

作者： Li Qiang Fu Xing sheng Guo Xin Liu Hui Li He yu Ling Wang yu she yang Shanghai Institute of Materia Medica Chinese Academy of SciencesShanghai 201203China School of Pharmaceutical Engineering Shenyang Pharmaceutical UniversityShenyang 110016China

In order to probe the effect of C-2(S)-substituted groups in the antibacterial activity,a series of novel C-2(S)-substituted pleuromutilin analogues of SB-225586 were synthesized and evaluated for their in vitro antibacterial *** results of antibacterial activities indicated that C-2(S)-substituted pleuromutilin derivatives retained appreciable antibacterial activity,and the 2-fluorination compounds 6a and 6b are more potent than the corresponding 2-hydroxylation analogues 7a and 7b.

关键词： Synthesis Pleuromutilin C-2(S)-substituted Antimicrobial activity

Design, synthesis and in vitro evaluation of L-amino acid esters prodrugs of acyclic nucleoside phosphonates as anti-HBV agent

在线全文

学校读者我要写书评

暂无评论

Chinese Chemical Letters 2007年第7期18卷 817-819页

作者： Xiao Zhong Fu Sai Hong Jiang Jian Xin yu she yang RU yun Ji School of Pharmacy Guiyang Medical College Guiyang 550004 China State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Shanghai Institute for Biological SciencesChinese Academy of Science Shanghai 201203 China Shanghai Fudan-yueda Bio-Tech Co. Ltd. Shanghai 201203 China

A series of novel L-amino acid esters prodrugs of acyclic nucleoside phosphonates was synthesized and their anti-HBV activity was evaluated in HepG2 2.2.15 cells. Compound 1d exhibited more potent anti-HBV activity and lower cytotoxicity than those of adefovir dipivoxil with EC50 and CC50 values of 0.207 μmol/L and 2530 μmol/L, respectively.

关键词： Acyclic nucleoside phosphonates L-Amino acid Prodrug Anti-HBV activity

Design,synthesis and anti-HBV activity of novel bis(trifluoroethyl)phosphonomethyl ether derivatives of acyclovir

在线全文

学校读者我要写书评

暂无评论

Chinese Chemical Letters 2009年第5期20卷 507-510页

作者： Peng Lu Sai Hong Jiang Jiang Xia Liu yu she yang Ru yun Ji State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Shanghai Institute for Biological Sciences Chinese Academy of Science Shanghai 201203 China Fudan University Shanghai 200032 China

A series of novel bis（trifluoroethyl）phosphonomethyl ether derivatives of acyclovir was synthesized and their in vitro anti-HBV activity was evaluated in HepG2 2.2.15 cells. In contrast to acyclovir, most of the described phosphonates emerged as potent inhibitors of HBV replication. Especially, the most active compound 11 with IC50 value of 2.92 μmol/L was 33 times more potent than acyclovir with ICso value of 100 μmol/L.

关键词： Acyclovir Phosphonate Anti-HBV activity