Synthesis and biological evaluation of some 4-(1H-indol-3-yl)-6-phenyl-1,2,3,4-tetrahydropyrimidin- -2-ones/thiones as potent anti-inflammatory agents* MOHAMMAD AMIR* SADIQUE AKHTAR JAVED
نویسنده
چکیده
portant molecules, pyrimidine has played an important role in medicinal chemistry. A survey of literature has shown that compounds having a pyrimidine nucleus possess a broad range of biological activities such as anticancer (1), antiviral (2), antibacterial (3), antimalarial (4), antihypertensive (5) and anti-inflammmatory activities (6, 7). Moreover, chemistry and synthesis of 1,2,3,4-tetrahydropyrimidin-2-ones/thiones have been attracting extensive attention. The importance of these tetrahydropyrimidines is mainly due to their close structural relationship to the clinically important dihydropyrimidine
منابع مشابه
Synthesis and biological evaluation of some 4-(1H-indol-3-yl)-6-phenyl-1,2,3,4-tetrahydropyrimidin-2-ones/thiones as potent anti-inflammatory agents.
Twelve new 4-(1H-indol-3-yl)-6-phenyl-1,2,3,4-tetrahydropyrimidin-2-ones/thiones (7-18) have been synthesized by reacting 1-aryl-3-(1H-indol-3-yl)-2-propen-1-one with urea and thiourea in ethanolic potassium hydroxide. Their structures have been confirmed by IR, 1H NMR and mass spectral data. The compounds were tested for their anti-inflammatory activity. Test results revealed that compounds sh...
متن کاملSynthesis and evaluation of the biological activities of some 3-{[5-(6-methyl-4-aryl-2-oxo-1,2,3,4-tetrahydropyrimidin-5-yl)-1,3,4-oxadiazol-2-yl]-imino}-1,3-dihydro-2H-indol-2-one derivatives.
Reaction of ethyl-6-methyl-2-oxo-4-aryl-1,2,3,4-tetrahydropyrimidin-5-carboxylates (1a-i) with hydrazine hydrate yielded 6-methyl-2-oxo-4-aryl-1,2,3,4-tetrahydropyrimidin-5-carbohydrazides (2a-i). These products, on reaction with cyanogen bromide, gave 5-(5-amino-1,3,4-oxadiazol-2-yl)-6-methyl-4-aryl-3,4-dihydropyrimidin-2 (1H)-ones (3a-i). The resultant aminooxadiazolylpyrimidinones were conde...
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A series of new 5-(1H-indol-3-yl)methyl-4-(substituted aryl)-2,4-dihydro-3H-1,2,4-triazole-3-thiones (4a-g), 5-(1H-indol-3-yl)methyl-N-(substituted aryl)-1,3,4-oxadiazol-2-amines (5a-g) and 5-(1H-indol-3-yl)methyl-N-(substituted aryl)-1,3,4-thiadiazol-2-amines (6a-g) were prepared by treating 2-(1H-indol-3-yl)acetyl-N-(substituted phenyl) hydrazine carbothioamides (3a-g) with suitable reagents....
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A new series of the title compounds incorporated into diverse N and O heterocyclic moieties of pharmacoavailability as anti-inflammatory and analgesic agents, were synthesized starting with 6,8-dibromo-2-phenyl-4H-3,1-benzoxazin-4-one (I) by its fusion with p-aminoacetophenone to give the new intermediate compound, 6,8-dibromo-2-phenyl-3-(4-acetylphenyl)-4(3H)-quinazolinone (II). The one pot re...
متن کاملDesign, Synthesis, Characterization and Biological Evaluation of Some Novel 1, 5 Disubstituted Tetrazole as Potential Anti-inflammatory Agents
In attempt to find new pharmacologically active molecules, we report here the synthesis and in vitro anti-inflammatory activity of various 1-[5-(substituted phenyl)-1-phenyl-4,5dihydro-1H-pyrazol-3-yl]-5-phenyl-1H-tetrazole (IV a-h).The anti-inflammatory activity of title compounds were examined by denaturation of proteins method. All the compounds exhibited weak to potent anti-inflammatory act...
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تاریخ انتشار 2008