- Analogues of 2′-hydroxychalcone with modified C4-substituents as the inhibitors against human acetylcholinesterase
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A series of C4-substituted tertiary nitrogen-bearing 2′-hydroxychalcones were designed and synthesised based on a previous mixed type acetylcholinesterase inhibitor. Majority of the 2′-hydroxychalcone analogues displayed a better inhibition against acetyl
- Sukumaran, Sri Devi,Nasir, Shah Bakhtiar,Tee, Jia Ti,Buckle, Michael J. C.,Othman, Rozana,Rahman, Noorsaadah Abd.,Lee, Vannajan Sanghiran,Bukhari, Syed Nasir Abbas,Chee, Chin Fei
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p. 130 - 137
(2020/12/03)
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- In Vitro Osteogenic Differentiation and Antibacterial Potentials of Chalcone Derivatives
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Chalcone derivatives have been investigated as therapeutic agents for the anticancer, antioxidant, and anti-inflammatory fields. In this study, we have synthesized four different types of chalcone derivatives and demonstrated in vitro bioactivities. We divided these derivatives into two groups of chalcones on the basis of similar substituents on the aromatic rings, and we tested cell viability and proliferation potentials, which indicated that the methoxy substituent on the A ring could enhance cytotoxicity and antiproliferation potential depending on the chalcone concentration. We also investigated osteogenic differentiation of C2C12 cells by ALP staining, the early marker for osteogenesis, which demonstrated that the chalcones could not only induce activity of BMP-2 but also inhibit the activity of noggin, a BMP antagonist. In addition, chalcone bearing hydroxyl groups at the 2-, 4-, and 6-position on the A ring inhibited treptococcus mutans growth, a major causative agent of dental caries. Therefore, we concluded that the chalcone derivatives synthesized in this research can be good candidates for therapeutic agents promoting bone differentiation, with an expectation of inhibiting S. mutans, in dentistry.
- Choi, Daheui,Park, Jin Chan,Lee, Ha Na,Moon, Ji-Hoi,Ahn, Hyo-Won,Park, Kwangyong,Hong, Jinkee
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p. 3197 - 3204
(2018/07/25)
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- Flavokawain derivative or pharmaceutically acceptable salt thereof having inhibitory activity on Hsp90 and medical use thereof
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The present invention relates to a flavokawain derivative or a pharmaceutically acceptable salt thereof having an activity for inhibiting Hsp90 and a medical use thereof wherein the flavokawain derivative comprises good effect of inhibiting Hsp90 and accordingly leads to decomposition of Hsp 90 client protein causing diseases related to cancer or neurodegenerative diseases by inhibiting Hsp90, thereby being used in drug medicine and healthy food products for preventing or treating Hsp 90 which is a mediated disease like diseases related to cancer or neurodegenerative diseases.COPYRIGHT KIPO 2015
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Paragraph 0079-0082
(2016/10/10)
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- Synthesis and evaluation of novel carbamate-substituted flavanone derivatives as potent acetylcholinesterase inhibitors and anti-amnestic agents
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This study was designed to synthesize and evaluate flavanone derivatives with phenylcarbamate moiety as potent acetylcholinesterase (AChE) inhibitors and anti-amnestic agents for management of AD. The synthesis of carbamate-substituted flavanone derivativ
- Anand, Preet,Singh, Baldev
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p. 1648 - 1659
(2013/07/26)
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- Antispasmodic activity of xanthoxyline derivatives: Structure-activity relationships
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The antispasmodic activity of several xanthoxyline derivatives against acetylcholine-induced contraction of the guinea pig ileum was evaluated in vitro. The acetophenones with two methoxyl groups, mainly in the 3,4 positions, exhibited potent antispasmodic activity. Modification of the hydroxyl group in xanthoxyline by the introduction of benzoyl, acetyl, or tosyl groups produced inactive compounds, whereas the introduction of benzyl or p-methoxybenzyl groups furnished compounds that were four- to eight-fold more potent than xanthoxyline. In marked contrast, the introduction of a methyl group gave a compound that caused contractant activity. Modification of the carbonyl group of xanthoxyline lead to inactive compounds, whereas the condensation of xanthoxyline with benzaldehydes gave chalkones that were about fivefold more potent than xanthoxyline. The introduction of benzyl and styrene groups, on the basis of the similarity with papaverine, improves the antispasmodic action of the xanthoxyline derivatives. Our results suggest that the methoxyl and carbonyl groups are critical structural points for the antispasmodic activity of xanthoxyline derivatives. The hydroxyl group improves antispasmodic activity, but is not fundamental to its manifestation.
- Filho,Miguel,Nunes,Calixto,Yunes
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p. 473 - 475
(2007/10/02)
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