- Design and Optimization of an Acyclic Amine Series of TRPV4 Antagonists by Electronic Modulation of Hydrogen Bond Interactions
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Investigation of TRPV4 as a potential target for the treatment of pulmonary edema associated with heart failure generated a novel series of acyclic amine inhibitors displaying exceptional potency and PK properties. The series arose through a scaffold hopp
- Patterson, Jaclyn R.,Terrell, Lamont R.,Donatelli, Carla A.,Holt, Dennis A.,Jolivette, Larry J.,Rivero, Ralph A.,Roethke, Theresa J.,Shu, Arthur,Stoy, Patrick,Ye, Guosen,Youngman, Mark,Lawhorn, Brian G.
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- CYCLIC PEPTIDE ANTIBIOTICS
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Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of lipoprotein signal peptidase II (LspA), a key protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.
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Paragraph 00283
(2020/09/27)
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- 2,4-diaminobutyric acid derivative and preparation method thereof
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The invention relates to a 2,4-diaminobutyric acid derivative and a preparation method thereof and relates to the field of medicine synthesis. An aspartic acid derivative serves as an initiator, and the 2,4-diaminobutyric acid derivative is obtained through simple reduction and substitution reaction. Different from the prior art, a reagent adopted for the method is small in toxicity, reaction conditions are mild, requirements for a device are not high, synthesis steps are simple, the 2,4-diaminobutyric acid derivative can be obtained at a high total yield, and the 2,4-diaminobutyric acid derivative facilitates large-scale industrial production and can be well applied to medicine synthesis.
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Paragraph 0035; 0036; 0037
(2017/07/20)
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- Constrained cyano compounds
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Certain constrained cyano compounds are useful as inhibitors of post-proline/alanine cleaving amino-dipeptidases. Accordingly, these compounds can be employed, alone or with another therapeutic agent, to treat diabetes (especially, Type II diabetes), hyperglycemia, Syndrome X, diabetic complications, hyperinsulinemia, obesity, atherosclerosis and related diseases, as well as various immunomodulatory diseases and chronic inflammatory bowel disease.
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Page/Page column 20-21
(2010/02/15)
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- A novel dipeptide, N-γ-glutamyl boletine, and a cyclic iminium toxin from the mushroom Tylopilus sp. (Boletaceae)
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N-γ-Glutamyl boletine and a toxin, 2-butyl-1-azacyclohexene iminium salt, were isolated from the mushroom Tylopilus sp. (Boltaceae). The absolute stereostructure of N-γ-glutamyl boletine was clarified based on spectroscopic analysis, acidic hydrolysis and total synthesis. N-γ-Glutamyl boletine exhibited moderate antibacterial activity. 2-Butyl-1-azacyclohexene iminium salt exhibited moderate acute toxicity against ddY mice. We proposed feasible biosynthetic pathway of piperidine alkaloids that the cyclic iminium compound might be biosynthesized from boletine, a new amino acid containing an δ-amino ketone moiety.
- Watanabe, Reiko,Kita, Masaki,Uemura, Daisuke
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p. 6501 - 6504
(2007/10/03)
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- β-Turned dipeptoids as potent and selective CCK1 receptor antagonists
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To improve our knowledge of the bioactive conformation of CCK1 antagonists, we previously described that replacement of the α-MeTrp residue of dipeptoids with the (2S,5S,11bR)-2-amino-3-oxohexahydroindolizino[8,7-b]indole-5-carboxylate (IBTM) s
- Martin-Martinez,De la Figuera,Latorre,Herranz,Garcia-Lopez,Cenarruzabeitia,Del Rio,Gonzalez-Muniz
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p. 3770 - 3777
(2007/10/03)
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- A facile synthesis of chiral N-protected β-amino alcohols
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Chiral N-protected β-amino alcohols are easily obtained by NaBH4 reduction of mixed anhydrides of N-protected α-amino acids in an organic/aqueous medium. The alcohols obtained from side chain or main chain reduction of N-protected aspartic acid are converted in good yields into lactones.
- Rodriguez,Llinares,Doulut,Heitz,Martinez
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p. 923 - 926
(2007/10/02)
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