CARBOXAMIDE

作品数:64被引量:95H指数:5
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相关领域:理学医药卫生更多>>
相关作者:冯卫生郑晓珂陈满生更多>>
相关机构:河南中医药大学广西师范大学衡阳师范学院更多>>
相关期刊:《Journal of Crystallization Process and Technology》《Chinese Journal of Chemistry》《Journal of Animal Science and Biotechnology》《Science China(Life Sciences)》更多>>
相关基金:国家自然科学基金国家重点基础研究发展计划广东省自然科学基金天津市自然科学基金更多>>
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Discovery of a novel thiophene carboxamide analogue as a highly potent and selective sphingomyelin synthase 2 inhibitor for dry eye disease therapy
《Acta Pharmaceutica Sinica B》2025年第1期392-408,共17页Jintong Yang Yiteng Lu Kexin Huf Xinchen Zhang Wei Wang Deyong Ye Mingguang Mo Xin Xiao Xichen Wan Yuqing Wu Shuxian Zhang He Huang Zhibei Qu Yimin Hu Yu Cao Jiaxu Hong Lu Zhou 
supported by the National Key R&D Program of China(2023YFC3603303 and 2023YFA0915000);the National Natural Science Foundation of China(22077019 and 82171102);Shanghai Municipal Committee of Science and Technology(21TQ016 and 21XD1420600,China);the Shanghai Medical Innovation Research Program(22Y21900900,China);the Shanghai Key Clinical Research Program(SHDC2020CR3052B,China);the Class IV Peak Disciplines(Shanghai Institute of Precision Medicine)from the Shanghai Municipal Education Commission.The authors would like to thank Professor Weiyun Shi(Shandong Eye Hospital,Ji’nan,China).
Dry eye disease(DED)is a prevalent and intractable ocular disease induced by a variety of causes.Elevated sphingomyelin(SM)levels and pro-inflammatory cytokines were detected on the ocular surface of DED patients,part...
关键词:Sphingomyelin synthase 2 Thiophene carboxamide SMS2inhibitor 
Discovery of an enantiopure N-[2-hydroxy-3-phenyl piperazine propyl]-aromatic carboxamide derivative as highly selectiveα_(1D/1A)-adrenoceptor antagonist and homology modelling
《Chinese Chemical Letters》2024年第11期435-441,共7页Junjun Huang Ran Chen Yajian Huang Hang Zhang Anran Zheng Qing Xiao Dan Wu Ruxia Duan Zhi Zhou Fei He Wei Yi 
supported by Natural Science Foundation of Guangdong Province(Nos.2021A1515010101,2021A1515011372,2023A1515011895);National Natural Science Foundation of China(Nos.21807017,82273759,32371529);Guangzhou Medical University Scientific Research Capacity Improvement Project(No.02-410-2405104)。
α_(1)-Adrenergic receptor(AR)blockers can be effective for the treatment of benign prostatic hyperplasia/lower urinary tract symptoms(BPH/LUTS),their usage is limited by cardiovascular-related side effects that are c...
关键词:Benign prostatic hyperplasia α_(1)-AR antagonist Phenylpiperazine Homology modelling Subtype selectivity 
Bactericidal bissulfone B7 targets bacterial pyruvate kinase to impair bacterial biology and pathogenicity in plants
《Science China(Life Sciences)》2024年第2期391-402,共12页Awei Zhang Haizhen Zhang Ronghua Wang Hongfu He Baoan Song Runjiang Song 
supported by the National Key Research and Development Program of China(2022YFD1700300);Program of Introducing Talents of Discipline to Universities of China(111Program,D20023);the Key Technologies R&D Program of Guizhou Province in China(2017-5788-1)。
The prevention and control of rice bacterial leaf blight(BLB)disease has not yet been achieved due to the lack of effective agrochemicals and available targets.Herein,we develop a series of novel bissulfones and a nov...
关键词:2-bissulfone-N-phenylhydrazine-1-carboxamide derivatives XOO antibacterial activities pyruvate kinase regulatory mechanism 
Structure-based drug discovery of novel fusedpyrazolone carboxamide derivatives as potent and selective AXL inhibitors
《Acta Pharmaceutica Sinica B》2023年第12期4918-4933,共16页Feifei Fang Yang Dai Hao Wang Yinchun Ji Xuewu Liang Xia Peng Jiyuan Li Yangrong Zhao Chunpu Li Danyi Wangh Yazhou Li Dong Zhang Dan Zhang Meiyu Geng Hong Liu Jing Ai Yu Zhou 
supported by the Natural Science Foundation of China for Innovation Research Group(81821005);the National Natural Science Foundation of China(21977106 and 82173834);the Collaborative Innovation Cluster Project of Shanghai Municipal Commission of Health and Family Planning(2020CXJQ02);the Shanghai Post-doctoral Excellence Program(2022231,China);the Shanghai Sail Program(22YF1460700,China);Lingang Laboratory(LG202103-02-07,China);Lingang Laboratory(LGGG-202204-02,China).
a novel and promising antitumor target,AXL plays an important role in tumor growth,metastasis,immunosuppression and drug resistance of various malignancies,which has attracted extensive research interest in recent yea...
关键词:Potential AXL inhibitor Antitumor activity Structure-based drug design Fused-pyrazolone carboxamide 
Synthesis,Crystal Structure and Anti-fungal/Anti-oomycete Activity of New Pyrazole-benzene Carboxamide Derivatives
《Chinese Journal of Structural Chemistry》2022年第3期253-259,I0014,共8页YANG Zi-Hui LIU Qing-Song SUN Yue SUN Xue-Bao GU Wen 
supported by the National Natural Science Foundation of China (31770616);the Natural Science Foundation for Colleges and Universities in Jiangsu Province (17KJA220002)
Four novel pyrazole-benzene carboxamide derivatives 2a~2d were synthesized and characterized by NMR,HRMS spectral method and X-ray diffraction analysis,and were further conducted for screening the anti-fungal/anti-oom...
关键词:pyrazole-benzene carboxamide crystal structure antifungal activity anti-oomycete activity 
Synthesis,Crystal Structure and Antifungal Activity of New Furan-1,3,4-oxadiazole Carboxamide Derivatives
《Chinese Journal of Structural Chemistry》2022年第2期98-104,I0010,共8页SUN Yue YANG Zi-Hui GU Wen 
supported by the National Natural Science Foundation of China (31770616);the Natural Science Foundation for Colleges and Universities in Jiangsu Province (17KJA220002)。
A series of novel furan-1,3,4-oxadiazole carboxamide derivatives (5a~5e) were designed,synthesized and characterized by spectroscopic methods including HR-MS,^(1)H-and ^(13)C-NMR.The crystal structure of compound 5a w...
关键词:furan-1 3 4-oxadiazole carboxamide SYNTHESIS crystal structure antifungal activity 
怀中1号鲜地黄化学成分研究被引量:5
《药学学报》2021年第11期3097-3103,共7页范锡玲 刘晏灵 曹彦刚 任英杰 王梦娜 陈旭 何晨 郑晓珂 冯卫生 
国家重点研发计划:中医药现代化研究重点专项-地黄特色中药材产业链关键技术研究(2017YFC1702800);河南省重大科技专项:地黄、山药、牛膝豫产道地药材品质保障关键技术与品质特色研究(171100310500)。
采用Toyopreal HW-40C、Sephadex LH-20、硅胶和半制备液相等多种色谱学技术从怀中1号鲜地黄中分离得到20个化合物。根据理化性质与波谱数据鉴定其结构,分别为3-methyl-2-(hydroxymethyl)-4H-pyrone-4-one(1)、3-氨基-2-吡啶乙醇(2)、(5...
关键词:玄参科 鲜地黄 化学成分 3-methyl-2-(hydroxymethyl)-4H-pyrone-4-one 3-氨基-2-吡啶乙醇 (5’S)-2-oxo-N-phenylpyrrolidine-3-carboxamide 
AIC AR and Decitabine Enhance the Sensitivity of K562 Cells to Imatinib by Promoting Mitochondrial Activity
《Current Medical Science》2020年第5期871-878,共8页Xiao-ying ZHU Wen LIU Hai-tao LIANG Ling TANG Ping ZOU Yong YOU Xiao-jian ZHU 
Although the advent of tyrosine kinase inhibitors(TKIs)has dramatically improved the survival of patients with chronic myeloid leukaemia(CML),acquired drug resistance and TKI-insensitive leukaemic stem cells(LSCs)rema...
关键词:chronic myeloid leukaemia mitochondrial activity 5-aminoimidazole-4-carboxamide ribotide(AICAR) DECITABINE 
Characterization of inthomycin biosynthetic gene cluster revealing new insights into carboxamide formation被引量:1
《Chinese Journal of Natural Medicines》2020年第9期677-683,共7页WANG Yong-Jiang WANG Li HE Xin XU Dong-Dong TANG Jun MA Ya-Tuan YAN Yi-Jun GU Yu-Cheng YANG Jing HUANG Sheng-Xiong 
supported by the National Natural Science Foundation of China (Nos. U1702285,21708045 and21502203);the Natural Science Foundation of Yunnan Province(Nos. 2019FJ007,2019FA034 and 2018HC012);the Key Research Program of Frontier Sciences and the Strategic Priority Research Program,CAS (Nos. QYZDB-SSW-SMC051 and XDB27020205);the Syngenta Postgraduate Studentship Awarded to WANG Yong-Jiang (2019-2020)。
Inthomycins are polyketide antibiotics which contain a terminal carboxamide group and a triene chain. Inthomycin B(1) and its two new analogues 2 and 3 were isolated from the crude extract of Streptomyces pactum L8. I...
关键词:Inthomycins BIOSYNTHESIS Gene cluster CARBOXAMIDE P450 
Design, synthesis and pharmacological evaluation of 4-(3-chloro-4-(3-cyclopropylthioureido)-2-fluorophenoxy)-7-methoxyquinoline-6-carboxamide (WXFL-152):a novel triple angiokinase inhibitor for cancer therapy被引量:3
《Acta Pharmaceutica Sinica B》2020年第8期1453-1475,共23页Yuqin Yao Zhuowei Liu Manyu Zhao Zhengxia Chen Peng Li Yang Zhang Yuxi Wang Chengjian Zhao Chaofeng Long Xiaoxin Chen Jinliang Yang 
supported by the National Major Scientific and Technological Special Project(Nos.2018ZX09201002,2018ZX09711001-011 and 2019ZX09201001);the National Natural Science Foundation of China(No.81773375)
Angiokinases, such as vascular endothelial-, fibroblast-and platelet-derived growth factor receptors(VEGFRs, FGFRs and PDGFRs) play crucial roles in tumor angiogenesis. Anti-angiogenesis therapy using multi-angiokinas...
关键词:inhibited CLINICAL SYNTHESIS 
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