- Synthesis of chiral γ-lactones via a RuPHOX-Ru catalyzed asymmetric hydrogenation of aroylacrylic acids
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An asymmetric hydrogenation of aroylacrylic acids catalyzed by RuPHOX-Ru catalyst has been developed, affording the corresponding chiral γ-lactones in high yields and with up to 93% ee. The methodology has the advantage of utilizing easily accessible substrates and has therefore expand the scope of the resulting chiral γ-lactones. Furthermore, high catalytic efficiency was achieved in that the reduction of both the C[dbnd]C and C[dbnd]O double bonds was achieved in one step. The current work provides an alternative and convenient pathway for the synthesis of a wide range of chiral γ-lactones.
- Lu, Yufei,Li, Jing,Zhu, Yue,Shen, Jiefeng,Liu, Delong,Zhang, Wanbin
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supporting information
p. 3643 - 3649
(2019/05/29)
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- Design, synthesis and structure-based optimization of novel isoxazole-containing benzamide derivatives as FtsZ modulators
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Antibiotic resistance among clinically significant bacterial pathogens is becoming a prevalent threat to public health, and new antibacterial agents with novel mechanisms of action hence are in an urgent need. Utilizing computational docking method and structure-based optimization strategy, we rationally designed and synthesized two series of isoxazol-3-yl- and isoxazol-5-yl-containing benzamide derivatives that targeted the bacterial cell division protein FtsZ. Evaluation of their activity against a panel of Gram-positive and -negative pathogens revealed that compounds B14 and B16 that possessed the isoxazol-5-yl group showed strong antibacterial activity against various testing strains, including methicillin-resistant Staphylococcus aureus and penicillin-resistant S. aureus. Further molecular biological studies and docking analyses proved that the compound functioned as an effective inhibitor to alter the dynamics of FtsZ self-polymerization via a stimulatory mechanism, which finally terminated the cell division and caused cell death. Taken together, these results could suggest a promising chemotype for development of new FtsZ-targeting bactericidal agent.
- Bi, Fangchao,Song, Di,Zhang, Nan,Liu, Zhiyang,Gu, Xinjie,Hu, Chaoyu,Cai, Xiaokang,Venter, Henrietta,Ma, Shutao
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- HETEROCYCLIC INHIBITORS OF MCT4
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Disclosed herein are compounds and compositions useful in the treatment of MCT4 mediated diseases, such as proliferative and inflammatory diseases, having the structure of Formula I: Methods of inhibition MCT4 activity in a human or animal subject are also provided.
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Paragraph 0509
(2018/06/30)
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- CERAMIDE GALACTOSYLTRANSFERASE INHIBITORS FOR THE TREATMENT OF DISEASE
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Described herein are compounds, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or disorders associated with the enzyme ceramide galactosyltransferase (CGT), such as, for example, lysosomal storage diseases. Examples of lysosomal storage diseases include, for example, Krabbe disease and Metachromatic Leukodystrophy.
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Paragraph 000562; 000563
(2018/01/17)
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- One pot synthesis of α-ketoamides from ethylarenes and amines: a metal free difunctionalization strategy
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One-pot and metal free synthesis of α-ketoamides has been described through in situ generation of aryl ketones from easily available ethylarenes followed by amidation with various amines. This multiple oxidation protocol involves catalytic I2-pyridine-TBHP (t-butyl hydroperoxide) mediated oxidative benzylic carbonylation and sequential NaI-TBHP mediated oxidative amidation without using any solvent.
- Ramanathan, Mani,Kuo, Chun-Kai,Liu, Shiuh-Tzung
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p. 11446 - 11453
(2016/12/16)
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- Calcium receptor active compounds
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A novel calcium receptor active compound having the formula is provided:Ar1—[CR1R2]P—X—[CR3R4]q—[CR5R6]—NR7—[CR8R9]—Ar2wherein:Ar1 is selected from the group consisting of aryl, heteroaryl, bis(arylmethyl)amino, bis(heteroarylmethyl)amino and arylmethyl(heteroarylmethyl)amino;X is selected from the group consisting of oxygen, sulfur, sulfinyl, sulfonyl, carbonyl and amino;R1, R2, R3, R4, R5, R6, R7, R8 and R9 are, for example, hydrogen or alkyl;Ar2 is selected from the group consisting of aryl and heteroaryl;p is an integer of from 0 to 6, inclusive; and,q is an integer of from 0 to 14, inclusive.
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- Mesomorphic properties of 1-(4'-dodecylbiphenyl-4-yl)-3-(2 or 3-alkoxyphenyl)propane-1,3-diones: the influence of alkoxysubstituent position
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Two homologous series of β-diketones, viz. 1-(4'-dodecylbiphenyl-4-yl)-3-(2-alkoxyphenyl)propane-1,3-diones and 1-(4'-dodecylbiphenyl-4-yl)-3-(3-alkoxyphenyl)propane-1,3-diones have been synthesised.The mesomorphic behaviour of all the compounds has been investigated using optical polarising microscopy and differential scanning colorimetry.The enthalpies associated with the transitions of all the liquid crystalline materials have also been determined.The mesophases exhibited by these compounds are explained on the basis of the structural features associated with such compounds.
- Sadashiva, Bukkinakere K.,Prasad, Veena
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p. 755 - 760
(2007/10/03)
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- Novel allylic oxidation of conjugate ketones with VO(OR)Cl2
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An oxo group is introduced at the allylic position of 3-methyl-2-cyclopenten-1-one and β-ionone on treatment with VO(OR)Cl2 in ROH. VO(OR)Cl2 induces γ-alkoxylation in the case of 2-cyclopenten-1-one. Reaction of 1-acetyl-1-cyclohexene with VO(OEt)Cl2 results in γ-alkoxylation and/or aromatization to give 1-acetyl-3-ethoxy-1-cyclohexene and the corresponding aromatic.
- Hirao,Mikami,Mori,Ohshiro
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p. 1741 - 1744
(2007/10/02)
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