- PYRIDINE COMPOUND SUBSTITUTED WITH AZOLE
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The present invention provides a compound represented by formula [I] shown below or a pharmaceutically acceptable salt thereof that has an inhibitory effect on 20-HETE producing enzyme. (in formula [I] above, the structure represented by formula [II] below: represents any of the structures represented by formula group [III] below: R1, R2, R3, and R4 independently represent a hydrogen atom, a fluorine atom, methyl, or the like, R5 represents any of the structures represented by formula group [IV]:
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Paragraph 0882; 1123
(2020/07/07)
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- Design, synthesis and SAR study of hydroxychalcone inhibitors of human β-secretase (BACE1)
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According to the structural characteristics of isoliquiritigenin from Glycyrrhiza uralensis, a series of hydroxychalcones has been designed, synthesized and evaluated for their in vitro inhibitory activities of β-secretase (BACE1). Structure-activity relationship study suggested that inhibitory activity against BACE1 was governed to a greater extent by the hydroxyl substituent on A-and B-ring of the chalcone, and the most active compound was substituted with four hydroxyl group (17, IC50=0.27 μM).
- Ma, Lei,Yang, Zhengyi,Li, Chenjing,Zhu, Zhiyuan,Shen, Xu,Hu, Lihong
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experimental part
p. 643 - 648
(2012/04/10)
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- Towards the first inhibitors of trihydroxynaphthalene reductase from Curvularia lunata: Synthesis of artificial substrate, homology modelling and initial screening
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Trihydroxynaphthalene reductase (3HNR) is an essential enzyme in the biosynthesis of fungal melanin and it represents an emerging target for the development of new fungicides and antimicotics. To promote the discovery of new inhibitors, an improved chemic
- Brunskole, Mojca,Stefane, Bogdan,Zorko, Karmen,Anderluh, Marko,Stojan, Jure,Lanisnik Rizner, Tea,Gobec, Stanislav
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p. 5881 - 5889
(2008/12/20)
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- Synthesis and structure-activity relationships of novel IKK-β inhibitors. Part 3: Orally active anti-inflammatory agents
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A series of 2-amino-3-cyano-4-alkyl-6-(2-hydroxyphenyl)pyridine derivatives was synthesized and evaluated as IκB kinase β (IKK-β) inhibitors. Modification of a novel IKK-β inhibitor 1 (IKK-β IC 50=1500nM, Cell IC50=8000nM) at the 4-p
- Murata, Toshiki,Shimada, Mitsuyuki,Sakakibara, Sachiko,Yoshino, Takashi,Masuda, Tsutomu,Shintani, Takuya,Sato, Hiroki,Koriyama, Yuji,Fukushima, Keiko,Nunami, Noriko,Yamauchi, Megumi,Fuchikami, Kinji,Komura, Hiroshi,Watanabe, Akihiko,Ziegelbauer, Karl B.,Bacon, Kevin B.,Lowinger, Timothy B.
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p. 4019 - 4022
(2007/10/03)
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- Pyridine derivatives
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Pyridine compounds of general formula: wherein —R1represents in which R11is hydrogen, C1-6alkyl, halogen, hydroxy, C1-12alkoxy, nitro, amino, C1-6alkylsulfonylamino, C1-6alkoxycarbonyl, C1-6alkylamino, di(C1-6alkyl)amino, C1-6alkanoylamino, phenyl C1-6alkylamino, phenylsulfonylamino, or —O—(CH2)n—R111; R2represents hydrogen or halogen; R3represents hydrogen, —CR31R32R33, or —NR34R35; R4is hydrogen, carbamoyl, CN, carboxyl, etc.; R5is amino, C1-6alkylamino, di C1-6alkylamino, etc. or salt thereof. The compound has an excellent anti-inflammatory activity, and other biological activity.
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- Na+-glucose cotransporter inhibitors as antidiabetics. I. Synthesis and pharmacological properties of 4'-dehydroxyphlorizin derivatives based on a new concept
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Based on our new concept that inhibitors of the Na+-glucose cotransporter (SGLT) would be useful as antidiabetics, 4'-dehydroxyphlorizin derivatives 1a-f were designed, synthesized, and examined for various pharmacological properties related to
- Tsujihara, Kenji,Hongu, Mitsuya,Saito, Kunio,Inamasu, Masanori,Arakawa, Kenji,Oku, Akira,Matsumoto, Mamoru
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p. 1174 - 1180
(2007/10/03)
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- Benzopyran derivatives and an anti-allergic agent possessing the same as the active ingredient
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The present invention relates to an extremely effective anti-allergic agent with a low toxicity, which possesses as its active ingredient a benzopyran derivative described by the general formula below (in the formula, R1 and R2 are each respectively a hydrogen atom, an acyl group, an alkyl group having 1?12 carbon atoms, or an alkenyl group having 2?10 carbon atoms; and R3 is a hydroxyl group, an acyloxy group, an alkoxy group having 1?10 carbon atoms, or an alkenyloxy group having 2?10 carbon atoms). General Formula STR1
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