- Pyrones V-The Mass Spectra and Fragmentation Mechanism of Some 3(5)-Methoxy-4-pyrones
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The mass spectra of methyl kojate (2-hydroxymethyl-5-methoxy-4H-pyran-4-one), two deuterated analogues and 14 related 3(5)-methoxy-4-pyrones have been studied.These compounds fragment according to a common mechanism, initiated by primary rearrangement of the molecular ion(s).Guidelines which indicate the presence of 3(5)-methoxy-4-pyrones and allow sructural determinations to be made from their mass spectra are presented.For the majority of substituents studied, the nature of the substituent has no major effect upon the fragmentation pattern; the cyano group does.The hydroxy counterparts of the above compounds are readily converted for analysis by simple methylation.
- McGillivray, David L.,Poulton, Gerald A.
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- Inhibitory activity of novel kojic acid derivative containing trolox moiety on melanogenesis
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A novel kojic acid derivative containing a trolox moiety, (±)-5-hydroxy-4-oxo-4H-pyran-2-yl methyl 6-hydroxy-2,5,7,8- tetramethylchroman-2-carboxylate (3a), was synthesized. The two biologically active compounds, namely, kojic acid and trolox, were conjug
- Ahn, Soo Mi,Rho, Ho Sik,Baek, Heung Soo,Joo, Yung Hyup,Hong, Yong Deog,Shin, Song Seok,Park, Young-Ho,Park, Soo Nam
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- Kojyl cinnamate ester derivatives promote adiponectin production during adipogenesis in human adipose tissue-derived mesenchymal stem cells
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The subcutaneous fat tissue mass gradually decreases with age, and its regulation is a strategy to develop anti-aging compounds to ameliorate the photo-aging of human skin. The adipogenesis of human adipose tissue-mesenchymal stem cells (hAT-MSCs) can be
- Rho, Ho Sik,Hong, Soo Hyun,Park, Jongho,Jung, Hyo-Il,Park, Young-Ho,Lee, John Hwan,Shin, Song Seok,Noh, Minsoo
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- Depigmenting activities of kojic acid derivatives without tyrosinase inhibitory activities
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We synthesized benzoate ester derivatives of kojic acid with and without adamantane moiety. Benzoate derivatives 2a-e that did not contain an adamantane moiety showed potent tyrosinase inhibitory activities. However, depigmenting activity was not noted in a cell-based assay. Contrasting results were obtained for benzoate derivatives (3a-e) containing an adamantane moiety. Compounds 3a-e showed potent depigmenting activities without tyrosinase inhibitory activities. To the best of our knowledge, this is the first study showing the depigmenting activities of kojic acid derivatives without tyrosinase inhibitory activities.
- Cho, Jun-Cheol,Rho, Ho Sik,Joo, Yung Hyup,Lee, Chang Seok,Lee, Jaekyoung,Ahn, Soo Mi,Kim, Jung Eun,Shin, Song Seok,Park, Young-Ho,Suh, Kyung-Do,Park, Soo Nam
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scheme or table
p. 4159 - 4162
(2012/07/03)
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- A NEW PEPTIDE DEFORMYLASE INHIBITOR COMPOUND AND MANUFACTURING PROCESS THEREOF
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The present invention relates to the novel antibacterial compounds having potent antibacterial activity as inhibitors of peptide deformylase. This invention further relates to pharmaceutically acceptable salts thereof, to processes for their preparation, and to pharmaceutical compositions containing them as an active ingredient.
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Page/Page column 11
(2010/07/08)
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- Discovery of 4-(benzylaminomethylene)isoquinoline-1,3-(2H,4H)-diones and 4-[(pyridylmethyl)aminomethylene]isoquinoline-1,3-(2H,4H)-diones as potent and selective inhibitors of the cyclin-dependent kinase 4
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The series of 4-(benzylaminomethylene)isoquinoline-1,3-(2H,4H)-dione and 4-[(pyridylmethyl)aminometh-ylene]isoquinoline-1,3-(2H,4H)-dione derivatives reported here represents a novel class of potential antitumor agents, which potently and selectively inhibit CDK4 over CDK2 and CDK1. In the benzylamino headpiece, a 3-OH substituent is required on the phenyl ring for CDK4 inhibitory activity, which is further enhanced when an iodo, aryl, heteroaryl, t-butyl, or cyclopentyl substituent is introduced at the C-6 position of the isoquinoline-1,3-dione core. To circumvent the metabolic liability associated with the phenolic OH group on the 4-substituted 3-OH phenyl headpiece, we take two approaches: first, introduce a nitrogen o- or p- to the 3-OH group in the phenyl ring; second, replace the phenyl headpiece with N-substituted 2-pyridones. We present here the synthesis, SAR data, metabolic stability data, and a CDK4 mimic model that explains the binding, potency, and selectivity of our CDK4 selective inhibitors.
- Tsou,Liu, Xiaoxiang,Birnberg, Gary,Kaplan, Joshua,Otteng, Mercy,Tran, Tritin,Kutterer, Kristina,Tang, Zhilian,Suayan, Ron,Zask, Arie,Ravi, Malini,Bretz, Angela,Grillo, Mary,Mcginnis, John P.,Rabindran, Sridhar K.,Ayral-Kaloustian, Semiramis,Mansour, Tarek S.
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scheme or table
p. 2289 - 2310
(2010/02/28)
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- A NEW PEPTIDE DEFORMYLASE INHIBITOR COMPOUND AND MANUFACTURING PROCESS THEREOF
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The present invention relates to the novel antibacterial compounds having potent antibacterial activity as inhibitors of peptide deformylase. This invention further relates to pharmaceutically acceptable salts thereof, to processes for their preparation, and to pharmaceutical compositions containing them as an active ingredient.
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Page/Page column 22
(2009/01/24)
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