- Synthesis and antioxidant activities of berberine 9-: O -benzoic acid derivatives
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Although berberine (BBR) shows antioxidant activity, its activity is limited. We synthesized 9-O-benzoic acid berberine derivatives, and their antioxidant activities were screened via ABTS, DPPH, HOSC and FRAP assays. The para-position was modified with halogen elements on the benzoic acid ring, which led to an enhanced antioxidant activity and the substituent on the ortho-position was found to be better than the meta-position. Compounds 8p, 8c, 8d, 8i, 8j, 8l, and especially 8p showed significantly higher antioxidant activities, which could be attributed to the electronic donating groups. All the berberine derivatives possessed proper lipophilicities. In conclusion, compound 8p is a promising antioxidant candidate with remarkable elevated antioxidant activity and moderate lipophilicity.
- Liu, Yanfei,Long, Shuo,Zhang, Shanshan,Tan, Yifu,Wang, Ting,Wu, Yuwei,Jiang, Ting,Liu, Xiaoqin,Peng, Dongming,Liu, Zhenbao
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p. 17611 - 17621
(2021/05/29)
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- COMPOUNDS USEFUL FOR THE TREATMENT OF METABOLIC DISORDERS AND SYNTHESIS OF THE SAME
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The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.
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Page/Page column 86
(2014/10/18)
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- Design, synthesis and activity evaluation of N-(pyridin-4-yl) salicylamides as antimycobacterial agents
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A series of N-(pyridin-4-yl) salicylamides derivatives were prepared through acylation of the corresponding acetylsalicyloyl chlorides with substituted 4-amino-pyridines. These compounds were evaluated in vitro for antimycobacterial activities against Myc
- Dian, He,Zhou, De-Bin,Mou, Jian-Ping,Yang, Zhu-Qing,Zhong, Jia,Ding, Xiao-Quan,Li, Chong,Wang, Xiao-Hong,Zhang, Jian-Gang
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p. 7269 - 7275
(2015/04/22)
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- Development of 5-nitrothiazole derivatives: Identification of leads against both replicative and latent Mycobacterium tuberculosis
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Twenty eight 5-nitrothiazole derivatives were synthesized and evaluated for in vitro activities against Mycobacterium tuberculosis (MTB), cytotoxicity against HEK 293T. Among the compounds, 5-nitro-N-(5-nitrothiazol-2-yl)furan-2- carboxamide (20) was found to be the most active compound in vitro with MICs of 5.48 μM against log-phase culture of MTB and also non-toxic up to 100 μM.
- Jeankumar, Variam Ullas,Chandran, Manoj,Samala, Ganesh,Alvala, Mallika,Koushik, Pulla Venkat,Yogeeswari, Perumal,Salina, Elena G.,Sriram, Dharmarajan
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p. 7414 - 7417
(2013/02/22)
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- Synthesis of novel thiopyrimidines: An investigation of anti-tubercular and antimicrobial activity
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A variety of novel sulfur-containing tricyclic pyrimidine derivatives have been synthesized via the reaction of 2-amino-4-oxo-4H-chromene-3-carbonitriles 3(a-f) with different reagents and characterized by IR, 1H NMR, 13C NMR, mass spectrometry and elemen
- Haveliwala, Dhaval D.,Kamdar, Nimesh R.,Mistry, Prashant T.,Patel, Saurabh K.
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experimental part
p. 451 - 462
(2012/06/30)
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- COMPOUNDS AND COMPOSITIONS FOR DELIVERING ACTIVE AGENTS
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Compounds and compositions for the delivery of active agents are provided. Methods of administration and preparation are provided as well.
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- A highly practical route to 2-methylchromones from 2-acetoxybenzoic acids
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2-Methylchromones were accessed via a keto ester condensation on 2-acetoxybenzoyl chloride, followed by cyclization and decarboxylation. No column chromatography was required in the process.
- Jung,Min,Park
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p. 1837 - 1845
(2007/10/03)
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- Synthesis and biological activity of novel 1,3-benzoxazine derivatives as K+ channel openers
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A new series of 1,3-benzoxazine derivatives with a 2-pyridine 1-oxide group at C4 was designed to explore novel K+ channel openers. Synthesis was carried out by using a palladium(0)-catalyzed carbon-carbon bond formation reaction of imino-triflates with organozinc reagents and via a new one-pot 1,3-benzoxazine skeleton formation reaction of benzoylpyridines. The compounds were tested for vasorelaxant activity in tetraethylammonium chloride (TEA) and BaCl2-induced and high KCl-induced contraction of rat aorta to identify potential K+ channel openers, and also for oral hypotensive effects in spontaneously hypertensive rats. An electron- withdrawing group with the proper shape at C6 and a methyl or halogens group at C7 of the 1,3-benzoxazine nucleus were required for the development of optimal vasorelaxant and hypotensive activity. In particular, 2-(6-bromo-7- chloro-2,2-dimethyl-2H-1,3-benzoxazin-4-yl)pyridine 1-oxide (71) showed more potent vasorelaxant activity (EC50=0.14 μM) against TEA and BaCL2- induced contraction and longer-lasting hypotensive effects than cromakalim (1).
- Yamamoto, Satoshi,Hashiguchi, Shohei,Miki, Shokyo,Igata, Yumiko,Watanabe, Toshifumi,Shiraishi, Mitsuru
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p. 734 - 745
(2007/10/03)
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- Analogs of 3-(1-Phenyl-3-oxobutyl)-4-hydroxycoumarin (Warfarin) Prepared from Substituted Salicylic Acids
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Some derivatives of salicylic acid containing substituents meta to the carboxyl group were used to prepare analogs of the anticoagulant drug warfarin, 3-(1-phenyl-3-oxobutyl)-4-hydroxycoumarin, containing substituents in either the 6- or 8-position of the coumarin ring.When the substituent was the hydroxyl group, the resulting products are previously identified metabolites of warfarin.The substituted salicylic acid is first acetylated with acetic anhydride, then either converted to the acid chloride and condensed with diethyl malonate in the presence of sodium hydroxide or converted to the mixed anhydride with formic acid and condensed with ethoxymagnesium diethyl malonate to yield, in either case, the corresponding 3-carbethoxy-4-hydroxycoumarin substituted in the 6- or 8-position of the coumarin ring.These compounds readily condense with benzalacetone to form the corresponding substituted warfarin in the presence of 5 mole percent tertiary amine catalyst.This method offers an improved route for the synthesis or 8-hydroxywarfarin.
- Obaseki, Andrew O.,Steffen, James E.,Porter, William R.
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p. 529 - 533
(2007/10/02)
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- Substituted 2-amino chromones and process for the preparation thereof
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This invention relates to substituted 2-amino chromones of the general structure I: SPC1 wherein R1, R2, R3, and R4 may be hydrogen, hydroxy, lower alkyl or lower alkoxy of 1-6 carbon atoms, halogen such as chloro or bromo, or aryl such as phenyl, and X may be cyano or carboxamido. Two novel procedures for preparing substituted 2-amino chromones having the Formula I, starting with salicylic acid or substituted salicylic acid, are described. The compounds of this invention are active in the prevention of allergic and asthmatic reactions in mammals.
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