- Discovery of a series of 5-phenyl-2-furan derivatives containing 1,3-thiazole moiety as potent Escherichia coli β-glucuronidase inhibitors
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Gut microbial β-glucuronidases have drawn much attention due to their role as a potential therapeutic target to alleviate some drugs or their metabolites-induced gastrointestinal toxicity. In this study, fifteen 5-phenyl-2-furan derivatives containing 1,3
- Zhou, Tao-Shun,He, Lu-Lu,He, Jing,Yang, Zhi-Kun,Zhou, Zhen-Yi,Du, Ao-Qi,Yu, Jin-Biao,Li, Ya-Sheng,Wang, Si-Jia,Wei, Bin,Cui, Zi-Ning,Wang, Hong
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- Thiazolidin-2-cyanamides derivatives as novel potent Escherichia coli β-glucuronidase inhibitors and their structure–inhibitory activity relationships
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Gut microbial β-glucuronidases have the ability to deconjugate glucuronides of some drugs, thus have been considered as an important drug target to alleviate the drug metabolites-induced gastrointestinal toxicity. In this study, thiazolidin-2-cyanamide de
- Chen, Jian-Wei,Cui, Zi-Ning,He, Min,Li, Ya-Sheng,Wang, Hong,Wang, Si-Jia,Wang, Ya-Kun,Wei, Bin,Zhang, Hua-Wei,Zhou, Tao-Shun
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p. 1736 - 1742
(2020/09/18)
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- Synthesis and bioactivity of phenyl substituted furan and oxazole carboxylic acid derivatives as potential PDE4 inhibitors
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In this present study, a series of 5-phenyl-2-furan and 4-phenyl-2-oxazole derivatives were designed and synthesized as phosphodiesterase type 4 (PDE4) inhibitors. In vitro results showed that the synthesized compounds exhibited considerable inhibitory ac
- Lin, Yinuo,Ahmed, Wasim,He, Min,Xiang, Xuwen,Tang, Riyuan,Cui, Zi-Ning
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- Synthesis and SAR of 5-aryl-furan-2-carboxamide derivatives as potent urotensin-II receptor antagonists
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The synthesis and biological evaluation as potential urotensin-II receptor antagonists of a series of 5-arylfuran-2-carboxamide derivatives 1, bearing a 4-(3-chloro-4-(piperidin-4-yloxy)benzyl)piperazin-1-yl group, are described. The results of a systemat
- Lim, Chae Jo,Kim, Nam Hui,Park, Hye Jin,Lee, Byung Ho,Oh, Kwang-Seok,Yi, Kyu Yang
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p. 577 - 580
(2019/01/05)
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- Novel S-Thiazol-2-yl-furan-2-carbothioate Derivatives as Potential T3SS Inhibitors against Xanthomonas oryzae on Rice
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Bacterial leaf blight (BLB) caused by Xanthomonas oryzae pv oryzae (Xoo) is considered as the most destructive disease of rice. The use of bactericides is among the most widely used traditional methods to control this destructive disease. The excessive an
- Jiang, Shan,He, Min,Xiang, Xu-Wen,Adnan, Muhammad,Cui, Zi-Ning
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- Furancarbothioate compounds containing 1,2,3,4-tetrazole as well as preparation method and application of compounds
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The invention discloses furancarbothioate compounds containing 1,2,3,4-tetrazole as well as a preparation method and application of the compounds. The compounds have a structure represented by a formula (III) shown in the description, wherein R is one or
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Paragraph 0039-0041
(2019/10/01)
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- (S)-1,3-thiazolyl phenyl furan thioformate compounds and preparation method and application thereof
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The invention discloses (S)-1,3-thiazolyl phenyl furan thioformate compounds and a preparation method and application thereof. The compounds have a strong inhibitory effect on a hpa1 gene promoter ina pathogen T3SS system, and the inhibition rate of some
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Paragraph 0035; 0037
(2019/10/15)
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- Synthesis and biological evaluation of 2,5-disubstituted furan derivatives as P-glycoprotein inhibitors for Doxorubicin resistance in MCF-7/ADR cell
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Multidrug resistance (MDR) is a tendency in which cells become resistant to structurally and mechanistically unrelated drugs, which is mediated by P-glycoprotein (P-gp). It is one of the noteworthy problems in cancer therapy. As one of the most important
- Li, Ya-Sheng,Zhao, Dong-Sheng,Liu, Xing-Yu,Liao, Yi-Xian,Jin, Hong-Wei,Song, Gao-Peng,Cui, Zi-Ning
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p. 546 - 556
(2018/04/17)
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- Synthesis and bioactivity of 3,5-dimethylpyrazole derivatives as potential PDE4 inhibitors
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A series of 3,5-dimethylpyrazole derivatives containing 5-phenyl-2-furan moiety were designed and synthesized as phosphodiesterase type 4 (PDE4) inhibitors. Bioassay results showed that the title compounds exhibited considerable inhibitory activity agains
- Hu, De-Kun,Zhao, Dong-Sheng,He, Min,Jin, Hong-Wei,Tang, Yong-Mei,Zhang, Lian-Hui,Song, Gao-Peng,Cui, Zi-Ning
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p. 3276 - 3280
(2018/08/22)
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- Tetrahydroquinoline and tetrahydroisoquinoline derivatives as potential selective PDE4B inhibitors
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Tetrahydroquinoline and tetrahydroisoquinoline derivatives containing 2-phenyl-5-furan moiety were designed and synthesized as phosphodiesterase type 4 (PDE4) inhibitors. The bioassay results showed that title compounds showed good inhibitory activity aga
- Li, Ya-Sheng,Liu, Xing-Yu,Zhao, Dong-Sheng,Liao, Yi-Xian,Zhang, Lian-Hui,Zhang, Feng-Zhi,Song, Gao-Peng,Cui, Zi-Ning
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p. 3271 - 3275
(2018/08/22)
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- Synthesis and bioactivity of pyrazole and triazole derivatives as potential PDE4 inhibitors
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A series of pyrazole and triazole derivatives containing 5-phenyl-2-furan functionality were designed and synthesized as phosphodiesterase type 4 (PDE4) inhibitors. The bioassay results showed that title compounds exhibited considerable inhibitory activit
- Li, Ya-Sheng,Tian, Hao,Zhao, Dong-Sheng,Hu, De-Kun,Liu, Xing-Yu,Jin, Hong-Wei,Song, Gao-Peng,Cui, Zi-Ning
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p. 3632 - 3635
(2016/07/21)
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- Synthesis and bioactivity of novel carvacrol and thymol derivatives containing 5-phenyl-2-furan
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A series of novel carvacrol and thymol derivatives containing 5-phenyl-2-furan were synthesized. The antitumor tests showed that the title compounds exhibited promising activity against Bel-7402 and KB. The fungicidal tests showed that most of the title c
- Cui, Zining,Li, Xinghai,Nishida, Yoshihiro
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p. 877 - 885
(2014/07/21)
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- Synthesis and fungicidal activity of novel 2,5-disubstituted-1,3,4- oxadiazole derivatives
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A novel series of 1,3,4-oxadiazole derivatives containing a 5-phenyl-2-furan moiety were synthesized from the intermediates diacylhydrazine 3 and acylhydrazone 5 via an efficient approach under microwave irradiation in good yields. Their structures were characterized by IR, 1H NMR, and elemental analysis. The antifungal tests indicated that the title compounds showed in vivo fungicidal activity against Botrytis cinerea and Rhizoctonia solanii at 500 μg/mL obviously. Some tested compounds even had a superiority effect over the commercial fungicides 40% Pyrimethanil SC and 3% Validamycin AS. The activity between the title compound and their precursors diacylhydrazine 3 and acylhydrazone 5 was also compared and discussed.
- Cui, Zi-Ning,Shi, Yan-Xia,Zhang, Li,Ling, Yun,Li, Bao-Ju,Nishida, Yoshihiro,Yang, Xin-Ling
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p. 11649 - 11656
(2013/02/22)
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- Synthesis and bioactivities of novel pyrazole and triazole derivatives containing 5-phenyl-2-furan
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A series of novel pyrazole and triazole derivatives containing 5-phenyl-2-furan functionality were designed and synthesized. Their toxicities were predicted using in silico assays and proven to be less toxic. The antitumor results showed that the activity
- Cui, Zi-Ning,Shi, Yan-Xia,Cui, Jing-Rong,Ling, Yun,Li, Bao-Ju,Yang, Xin-Ling
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experimental part
p. 121 - 127
(2012/03/27)
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- Synthesis and bioactivity of N-benzoyl-N'-[5-(2'-substituted phenyl)-2-furoyl] semicarbazide derivatives
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In order to find novel chitin synthesis inhibitors (CSIs) with good activity, benzoylphenylurea, a typical kind of CSIs, was chosen as the lead compound and 15 novel derivatives containing furan moieties were designed by converting the urea linkage of benzoylphenylureas into a semicarbazide and changing the aniline part into furoyl groups. The title compounds were synthesized by the reaction of substituted benzoyl isocyanates with 5-(substituted phenyl)-2-furoyl hydrazine, and the structures were confirmed by IR, 1H-NMR, elemental analysis and single crystal X-ray diffraction analyses (compound E2). The bioassay results indicated that the title compounds exhibit good insecticidal activity, especially towards Plutella xylostella L., but had lower fungicidal activity. Inspiringly, the title compounds possessed obvious anticancer activity against human promyelocytic leukemic cell line (HL-60), and some of the title compounds also had activity against human hepatocellular carcinoma cell line (Bel-7402), human gastric carcinoma cell line (BGC-823), and human nasopharyngeal carcinoma cell line (KB). The results indicated that the linkage in the lead compounds was important to the bioactivity and spectra. The modification on the urea linkage is an effective strategy to discover new pesticide and drug candidates.
- Cui, Zining,Ling, Yun,Li, Baoju,Li, Yongqiang,Rui, Changhui,Cui, Jingrong,Shi, Yanxia,Yang, Xinling
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scheme or table
p. 4267 - 4282
(2010/10/03)
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- Synthesis and bioactivity of novel N,N′-diacylhydrazine derivatives containing furan(II)
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Diacylhydrazines have been found as molting hormone analogs since RH-5849 was reported as the first nonsteroidal ecdysone agonist in 1988. Optimizations on diacylhydrizines with benzoheterocycle containing oxygen were widely explored in recent years. In o
- Li, Xichen,Yang, Xinling,Cui, Zining,Li, Ying,He, Hongwu,Ling, Yun
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experimental part
p. 1233 - 1239
(2010/11/19)
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- Synthesis of heterocycles from arylation products of unsaturated compounds: XVIII. 5-Arylfuran-2-carboxylic acids and their application in the synthesis of 1,2,4-thiadiazole, 1,3,4-oxadiazole, and [1,2,4]triazolo[3,4-b][1,3,4] thiadiazole derivatives
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Arylation of furan-2-carboxylic acid or its methyl ester with arenediazonium chlorides in the presence of copper(II) chloride gave the corresponding 5-arylfuran-2-carboxylic acids or methyl 5-arylfuran-2- carboxylates. 5-Arylfuran-2-carbonyl chlorides rea
- Gorak,Obushak,Matiichuk,Lytvyn
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experimental part
p. 541 - 550
(2009/08/17)
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- A novel class of potent influenza virus inhibitors: Polysubstituted acylthiourea and its fused heterocycle derivatives
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A series of polysubstituted and fused heterocycle derivatives of acylthiourea was prepared and the biological activity against influenza virus was evaluated. Of the analogues that demonstrated IC50s 0.1 μM, acylthiourea derivatives 16 and 50 were further investigated as candidates with the most potential for future development. The SAR of these compounds are discussed and they represent a novel class of highly potent and selective inhibitors of influenza virus.
- Sun, Chuanwen,Huang, Hai,Feng, Meiqing,Shi, Xunlong,Zhang, Xiaodong,Zhou, Pei
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p. 162 - 166
(2007/10/03)
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- Synthesis and evaluation of a new series of substituted acyl(thio)urea and thiadiazolo [2,3-a] pyrimidine derivatives as potent inhibitors of influenza virus neuraminidase
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A series of substituted acyl(thio)urea and 2H-1,2,4-thiadiazolo [2,3-a] pyrimidine derivatives were prepared and both of their cell culture and enzymatic activity toward influenza virus were tested. Their in vitro neuraminidase inhibitory activities were in good agreement with the corresponding activities in cultured cells and they were evaluated as potent neuraminidase inhibitors. Of the analogues that demonstrated IC50s 0.1 μM, 16 and 60 were further investigated as candidates with the most potential for future development. The molecular docking work of the representative compound was described to provide more insight into their mechanism of action and further rationalize the observations of this new series herein, which represents a novel class of highly potent and selective inhibitors of influenza virus.
- Sun, Chuanwen,Zhang, Xiaodong,Huang, Hai,Zhou, Pei
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p. 8574 - 8581
(2008/02/07)
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- Metalloform-selective inhibition: Synthesis and structure-activity analysis of Mn(II)-form-selective inhibitors of Escherichia coli methionine aminopeptidase
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Methionine aminopeptidase (MetAP) is a promising target for development of novel antibacterial, antifungal and anticancer agents. However, its physiologically relevant metal ion remains to be defined, and its inhibitors need to inhibit the in vivo metallo
- Huang, Qing-Qing,Huang, Min,Nan, Fa-Jun,Ye, Qi-Zhuang
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p. 5386 - 5391
(2007/10/03)
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- Phase transfer catalyzed synthesis under ultrasonic irradiation and bioactivity of N′-(4, 6-disubstituted-pyrimidin-2-yl)-N-(5-aryl-2-furoyl) thiourea derivatives
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Ten new N′-(4, 6-disubstituted-pyrimidin-2-yl)-N-(5-aryl-2-furoyl) thioureas have been synthesized using PEG-400 as solid-liquid phase transfer catalyst under ultrasonic irradiation. Their structures were exactly confirmed by IR, 1H NMR and ele
- Ke, Shao-Yong,Wei, Tai-Bao,Xue, Si-Jia,Duan, Li-Ping,Li, Jing-Zhi
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p. 1957 - 1960
(2007/10/03)
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- Ultrasonic irradiated synthesis of N-(5-aryl-2-furoyl)thiourea derivatives containing substituted pyrimidine ring under phase transfer catalysis
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A series of N-(5-aryl-2-furoyl)thiourea derivatives containing substituted pyrimidine ring were synthesized in good yield using PEG-400 as solid-liquid phase transfer catalyst under ultrasonic irradiation. The structures of all newly synthesized compounds
- Xue, Si-Jia,Ke, Shao-Yong,Wei, Tai-Bao,Duan, Li-Ping,Guo, Yan-Ling
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p. 1013 - 1018
(2007/10/03)
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- Synthesis of aryl 5-(2-chlorophenyl)-2-furoates under phase transfer catalysis
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The steric hindered esters, aryl 5-(2-chlorophenyl)-2-furoates (3a-o), are synthesized via the reaction of 5-(2-chlorophenyl)-2-furoic acid (1) with thionyl chloride and phenols under liquid-liquid phase transfer catalysis in excellent yield.
- Li, Zheng,Wang, Xicun
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p. 3081 - 3086
(2007/10/03)
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