- Syntheses and evaluation of fluorinated conformationally restricted analogues of GABA as potential inhibitors of GABA aminotransferase
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Inhibition of γ-aminobutyric acid aminotransferase (GABA-AT) could raise the concentration of GABA, an inhibitory neurotransmitter in the human brain, and could have therapeutic applications for a variety of neurological diseases including epilepsy. Four fluorine-containing analogues of GABA with conformations restricted by a cyclohexane ring system were designed and synthesized, but unlike some of their five-membered ring counterparts, minimal inhibition of GABA-AT was observed. It is likely that the rigid chair conformation of these compounds cannot be accommodated well in the enzyme's active site.
- Wang, Zhiyong,Silverman, Richard B.
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Read Online
- Shared biosynthesis of the saliniketals and rifamycins in salinispora arenicola is controlled by the sare1259 -encoded cytochrome P450
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Saliniketals A and B are unusual polyketides from the marine actinomycete Salinispora arenicola that inhibit ornithine decarboxylase induction. The structural similarities between the saliniketals and the ansa chain of the potent rifamycin antibiotics, wh
- Wilson, Micheal C.,Gulder, Tobias A. M.,Mahmud, Taifo,Moore, Bradley S.
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Read Online
- NOVEL GLUCOKINASE ACTIVATORS AND PROCESSES FOR THE PREPARATION THEREOF
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The present invention provides an amide derivative having a stilbene or 1,2-diphenylethane moiety within the molecule thereof, a process for the preparation thereof, and a pharmaceutical composition comprising the same. The amide derivative of the present
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Page/Page column 11
(2012/07/27)
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- Synthesis of potential early-stage intermediates in the biosynthesis of FR900482 and mitomycin c
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Beyond the identification of 3-amino-5-hydroxybenzoic acid (AHBA) and D-glucosamine as biosynthetic precursors to mitomycin C (5) and FR900482 (6), little is known about the pathway Nature uses to prepare these antitumor antibiotics. To gain some insight
- Chamberland, Stephen,Grueschow, Sabine,Sherman, David H.,Williams, Robert M.
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supporting information; experimental part
p. 791 - 794
(2009/08/15)
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- Biosynthesis of tetrapetalones
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The biosynthesis of tetrapetalones (tetrapetalones A, B, C, and D) in Streptomyces sp. USF-4727 was studied by feeding experiments with 1- 13C sodium propanoate, 1-13C sodium butanoate, carbonyl-13C 3-amino-5-hydroxybenzoic acid (AHBA) hydrochloride, and 1-13C glucose, followed by analysis of the 13C-NMR spectra. These feeding experiments revealed that the four tetrapetalones were polyketide compounds constructed from propanoate, butanoate, AHBA, and glucose. The tetrapetalone biosynthetic pathway was also suggested in this study. In this pathway, tetrapetalone A (1) is synthesized by polyketide synthase (PKS) using AHBA as a starter unit, then the side chain of 1 is subjected to acetoxylation to produce tetrapetalone B (2). Additionally, 1 is oxidized and transformed into tetrapetalone C (3). In a similar way, 2 is converted to tetrapetalone D (4). Therefore, the biosynthetic relationship of the four tetrapetalones was indicated. This journal is The Royal Society of Chemistry.
- Komoda, Toshikazu,Sugiyama, Yasumasa,Hirota, Akira
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p. 1615 - 1620
(2008/02/07)
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- A scaleable method for preparing 3-fluorenylmethoxycarbonylamino-5- hydroxybenzoic acid
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A scaleable synthesis of 3-fluorenylmethoxycarbonylamino-5- hydroxybenzoic acid is described.
- Watson,Flynn,Shah
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p. 1379 - 1382
(2007/10/03)
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- Synthesis of Unlabelled and Carboxyl-Labelled 3-Amino-5-hydroxybenzoic Acid
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Efficient syntheses are reported of the natural amino acid 3-amino-5-hydroxybenzoic acid in unlabelled and carboxyl-labelled forms from 3,5-dinitrobenzoic acid and 3,5-dinitroanisole, respectively.
- Herlt, Anthony J.,Kibby, Jeffrey J.,Rickards, Rodney W.
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p. 1319 - 1324
(2007/10/02)
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