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indole/inflammation
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Indole derivatives inhibit hepatitis C virus replication through induction of pro-inflammatory cytokines.
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Previously, we discovered a series of indole derivatives as a new class of hepatitis C virus (HCV) replication inhibitors by using a target-free chemical genetic strategy. Through a structure-activity relationship study, the compound 12e was identified as the most potent inhibitor of this class
New indole, aminoindole and pyranoindole derivatives with anti-inflammatory activity.
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6-Methoxy-1-methyl-2,3-diphenyl indol-5-carboxaldehyde (2) was demethylated to give the 6-hydroxy derivative (3) which was cyclized to the pyrano[3,2-f]indole derivatives (4a-d) by the action of ethyl acetoacetate, diethyl malonate, malononitrile, ethyl cyanoacetate. When 4c was boiled in acetic
Synthesis, anti-inflammatory, analgesic and anticonvulsant activities of 1,8-dihydro-1-ary1-8-alkyl pyrazolo(3,4-b)indoles.
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A series of 1,8-dihydro-1-aryl-8-alkyl pyrazolo(3,4-b)indoles 4a-j, 5a-j and 6a-j has been synthesized and tested for their anti-inflammatory and anticonvulsant activities. Formation of the pyrazoloindole derivatives was achieved by treating arylhydrazones of N-alkyl indole-3-carbox-aldehydes 1a-j,
Syn-2, 3-diols and anti-inflammatory indole derivatives from Streptomyces sp. CB09001.
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Two new natural diols, (2S, 3S, 4S)-4-methyl-1-phenylhexane-2,3-diol (1) and (2S, 3S)-4-methyl-1-phenylpentane-2,3-diol (2), together with five known compounds, xenocyloins B-D (3-5), lumichrome (6) and thymidine (7) were isolated from Streptomyces sp.
New N-pyridinyl(methyl)-indole-2- and 3-(alkyl)carboxamides and derivatives acting as systemic and topical inflammation inhibitors.
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A series of novel N-substituted-(indol-2-yl)carboxamides (12-18) and (indol-3-alkyl)carboxamides (25-31) were synthesized and evaluated as inhibitors of the inflammation process. Pharmacomodulation at the level of the amidic nitrogen by incorporation of the previously described pharmacophoric
Synthesis of 1,6,7,8-tetrahydro-naphtho[2,3-d]-azepino[4,5-b]indole-9,14-diones and their inhibitory effects on pro-inflammatory cytokines.
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A rapid route to a series of naphthoquinone-fused indole derivatives via irradiation in a modified commercial domestic microwave is reported. The desired products were produced in high yields and short reaction times. The naphthoquinone-fused indole derivatives were evaluated for their
Development of Novel Indole Molecules for the Screening of Anti-Inflammatory Activity.
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In the present work, some new 5-[2(3)-dialkylamino alkoxy] Indole 2,3-diones were prepared from 5-hydroxy isatin. A mixture of 5-hydroxy isatin, dialkylamino alkylhalide in alcoholic potassium hydroxide was stirred at room temperature for 6 h to get the 5-[2(3)-dialkylamino alkoxy] Indole
Effect of anti-inflammatory thiosemicarbazone indoles on hyaluronidase, acid phosphatase and trypsin.
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The present study was designed to evaluate the molecular basis of anti-inflammatory effects of nine 2-aryl-3-[4-(substituted phenyl)-3-thiosemicarbazone] indoles and their interaction with lysosomal and proteolytic enzymes. All compounds exhibited anti-inflammatory activity, which was reflected by
Anti-inflammatory and analgesic activities of Neolamarckia cadamba and its bioactive monoterpenoid indole alkaloids
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Ethnopharmacological relevance: Neolamarckia cadamba has been used traditionally to treat inflammation, fever, and pruritus in the Dai ethnopharmacy in Yunnan province, P.R. China. However, according to literature survey, the action basis
Hirsutine, an indole alkaloid of Uncaria rhynchophylla, inhibits inflammation-mediated neurotoxicity and microglial activation.
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Chronic microglial activation endangers neuronal survival through the release of various pro-inflammatory and neurotoxic factors. As such, negative regulators of microglial activation have been considered as potential therapeutic candidates to reduce the risk of neurodegeneration associated with
Synthesis and anti-inflammatory activity of indole glucosinolates.
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The nitronate and nitrovinyl methods to synthesize indole glucosinolates (GLs) have been investigated. The results were applied to generally the most prevalent natural indole glucosinolates to synthesize 4-methoxyglucobrassicin (MGB) and neo-glucobrassicin (NGB) in moderate overall yield for the
Synthesis and biological evaluation of new 3-substituted indole derivatives as potential anti-inflammatory and analgesic agents.
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Treatment of 3-cyanoacetyl indole 1 with the diazonium salts of 3-phenyl-5-aminopyrazole and 2-aminobenzimidazole afforded the corresponding hydrazones 4 and 5. 3-Cyanoacetyl indole reacted with phenylisothiocyanate to give the corresponding thioacetanilide derivative 7. Treatment of 7 with
Synthesis and biological evaluation of novel indole-2-one and 7-aza-2-oxindole derivatives as anti-inflammatory agents.
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Sepsis, a typically acute inflammatory disease, is the biggest cause of death in ICU (intensive care unit). Novel anti-inflammatory alternatives are still in urgent need. In this study, we designed and synthesized 30 indole-2-one and 7-aza-2-oxindole derivatives based on the skeleton of tenidap, and
Membrane stabilization and inhibition of lipid peroxidation by anti-inflammatory indoles.
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Nine 2-aryl-3-[4-(substituted phenyl)-3-thiosemicarbazone] indoles were evaluated for their ability to protect the human erythrocyte membrane against hypo-osmotic hemolysis and inhibit lipid peroxidation in rat liver homogenate in vitro. All compounds caused membrane stabilization and inhibition of
Design, Synthesis, and Structure-Activity Relationship Study of Novel Indole-2-carboxamide Derivatives as Anti-inflammatory Agents for the Treatment of Sepsis.
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Sepsis is characterized by a systemic inflammatory response syndrome. Derivatives of indole have been reported to exhibit diverse biological activities. This study reports on the design and synthesis of a new series of indole-2-carboxamide derivatives, which are screened for their anti-inflammatory
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