- Synthesis of 2,5-Diaryl Nonsymmetric Furans C6-Platform Chemicals via Catalytic Conversion of Biomass and the Formal Synthesis of Dantrolene
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Biomass-derived commodity chemical 5-hydroxymethyl furfural is an underutilized C6-platform chemical derived from cellulose that is ideal to prepare next-generation value-added products. We have developed an efficient synthetic strategy to access 2,5-diar
- Chacón-Huete, Franklin,Lasso, Juan David,Szavay, Paul,Covone, Jason,Forgione, Pat
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p. 515 - 524
(2020/12/22)
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- Furoylamino beta-carboline compound as well as preparation method and application thereof
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The invention discloses a furoylamino beta-carboline compound as well as a preparation method and application thereof. The structural general formula of the compound is shown as a formula I in the specification. The invention discloses a preparation metho
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Paragraph 0036-0039
(2021/04/26)
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- 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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- 2-furoylamide compound and preparation and application thereof
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The invention discloses a 2-furancarboxamide compound and a preparation method and application thereof. The 2-furancarboxamide compound is obtained by reacting a compound as shown in a formula II with9H-pyridino[3,4-b]indole in the presence of an acid-bin
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Paragraph 0036; 0038-0040; 0048
(2020/08/22)
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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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- 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 of carbohydrazides and carboxamides as anti-tubercular agents
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A novel series of furan/thiophene carbohydrazides and carboxamides were synthesized and evaluated for anti-TB and cytotoxic activities. All the synthesized compounds were characterized using 1H and 13C NMR and mass spectral technique
- Kumar, Gautam,Krishna, Vagolu Siva,Sriram, Dharmarajan,Jachak, Sanjay M.
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p. 871 - 884
(2018/07/31)
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- Hedgehog signal pathway inhibitor
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The invention provides a Hedgehog signal pathway inhibitor as well as stereoisomers, tautomers, hydrates, solvates or pharmaceutically acceptable salts thereof, and the structural formula of the inhibitor is as shown in a formula (I). The invention further provides a preparation method and application of a compound. The compound provided by the invention is novel in structure; a signal transduction pathway adjusted by Hedgehog protein, Ptch, Gli and/or Smo can be adjusted through the compound of the formula I.
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Paragraph 0103; 0128
(2017/06/20)
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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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- High-turnover aminopyridine-based Pd-catalysts for Suzuki-Miyaura reaction in aqueous media
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A high-turnover catalytic system based on commercially available aminopyridines (L) and PdCl2 has been developed for Suzuki-Miyaura reaction in aqueous media. Reactions of arylboronic acids with a wide range of aryl iodides, bromides and chlorides proceeded in the presence of these catalysts for a short time in aqueous media to afford the cross-coupling products in high yields. Furthermore, this protocol allows tolerating a wide range of functional groups.
- Bumagin, Nikolay A.
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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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- SAR Studies on tetrahydroisoquinoline derivatives: The role of flexibility and bioisosterism to raise potency and selectivity toward P-glycoprotein
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The development of P-glycoprotein (P-gp) ligands remains of considerable interest, mostly for investigating the proteins structure and transport mechanism. In recent years, many different generations of ligands have been tested for their ability to modulate P-gp activity. The aim of the present work is to perform SAR studies on tetrahydroisoquinoline derivatives in order to design potent and selective P-gp ligands. For this purpose, the effect of bioisosteric replacement and the role of flexibility have been investigated, and four series of tetrahydroisoquinoline ligands have been developed: (a) 2-aryloxazole bioisosteres, (b) elongated analogues, (c) 2H-chromene, and (d) 2-biphenyl derivatives. The results showed that both 2-biphenyl derivative 20b and elongated derivative 6g behaved as strong P-gp substrates. In conclusion, important aspects for developing potent and selective P-gp ligands have been highlighted, providing a solid starting point for further optimization.
- Capparelli, Elena,Zinzi, Laura,Cantore, Mariangela,Contino, Marialessandra,Perrone, Maria Grazia,Luurtsema, Gert,Berardi, Francesco,Perrone, Roberto,Colabufo, Nicola A.
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p. 9983 - 9994
(2015/02/05)
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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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scheme or table
p. 121 - 127
(2012/03/27)
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- Palladium-catalyzed decarboxylative cross-coupling reaction between heteroaromatic Carboxylic acids and Aryl halides
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"Chemical Equation Presented" A full overview of the decarboxylative cross-coupling reaction between heteroaromatic carboxylic acids and aryl halides is described. This transformation employs palladium catalysts with short reaction times providing facile synthesis of aryl-substituted heteroaromatics. The effect of each reaction parameter including solvent, base, and additive employed as well as the full substrate scope of this transformation are reported. Mechanistic evidence is also disclosed that sheds light on possible reaction pathways.
- Bilodeau, Francois,Brochu, Marie-Christine,Guimond, Nicolas,Thesen, Kris H.,Forgione, Pat
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experimental part
p. 1550 - 1560
(2010/06/12)
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- Synthesis and antimicrobial activities of some new triazolothiadiazoles bearing 4-methylthiobenzyl moiety
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A series of substituted triazolothiadiazoles (6a-j and 7a-j) have been synthesized by condensing 4-amino-3-[4-methylthiobenzyl]-4H-1,2,4-triazole-5-thiol (5) with substituted aryl furoic acids/aromatic acids in the presence of POCl3. The triazole (5) was obtained by the fusion of 4-methylthiophenyl acetic acid (4) with thiocarbohydrazide. The structures of newly synthesized compounds are characterized by elemental analysis, IR, 1H NMR and mass spectroscopic studies and were screened for their antimicrobial activities. The preliminary results revealed that some of the compounds exhibited promising antimicrobial activities.
- Prasad, D. Jagadeesh,Ashok, Mithun,Karegoudar, Prakash,Poojary, Boja,Holla, B. Shivarama,Kumari, Nalilu Sucheta
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experimental part
p. 551 - 557
(2009/09/08)
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- Synthesis of some thiadiazolotriazinone derivatives as possible antimicrobial agents
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A series of 7-substituted-3-t-butyl 4(H)-1,3,4-thiadiazolo(2,3-c)-1,2,4- triazine-4-one (3) have been synthesized by condensing 4-amino-6-t-butyl-3- mercapto-1,2,4-triazin-5(4H)-one (1) with substituted Arylfuroic acids (2) using POCl3 as a cyclizing agen
- Prasad, D. Jagadeesh,Karthikeyan,Karegoudar, Prakash B.,Poojary, Boja,Holla, B. Shivarama,Kumari, N. Suchetha
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p. 1083 - 1091
(2008/02/01)
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- HETEROCYCLIC CARBONYL COMPOUNDS
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The invention relates to novel heterocyclic compounds of formula (I) wherein R1, D, W, T and T' have the meaning cited in the claim 1. Said compounds are SGK-inhibitors and can be used in the treatment of SGK-related diseases and disorders such as diabetes, obesity, metabolic syndrome (dyslipidemia), systemic and pulmonal hypertension, cardiovascular diseases and renal diseases, and generally for any kind of fibroses and inflammatory processes.
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Page/Page column 53
(2008/06/13)
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- Pd-EDTA as an efficient catalyst for Suzuki-Miyaura reactions in water
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PdCl2-EDTA complex 1 is an efficient catalyst for the Suzuki-Miyaura reactions of aryl and heteroaryl halides with aryl(heteroaryl)boronic acids in water at 20-100°C. Aryl iodides and bromides undergo the cross-coupling with turnover numbers (T
- Korolev, Dmitrii N.,Bumagin, Nikolay A.
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p. 5751 - 5754
(2007/10/03)
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