Organocatalyzed Asymmetric Michael Addition of 1‑Acetylindolin-3-ones to β,γ-Unsaturated α‑Ketoesters: An Access to Chiral Indolin-3-ones with Two Adjacent Tertiary Stereogenic Centers

Asymmetric Michael addition of 1-acetylindolin-3-ones to β,γ-unsaturated α-ketoesters was investigated for the synthesis of chiral indolin-3-ones with two adjacent tertiary stereogenic centers. Under the catalysis of a chiral bifunctional squaramide derived from l-<i>tert</i>-leucine, a wide range of 1-acetylindolin-3-ones and β,γ-unsaturated α-ketoesters were well-tolerated in this transformation to provide the corresponding novel densely functionalized chiral indolin-3-one derivatives in high yield with excellent diastereo- and enantioselectivity under mild reaction conditions

Stereocontrolled Construction of Tetrahydro­pyrano­[2,3‑<i>c</i>]pyrazole Scaffold via an Organocatalyzed Formal [3 + 3] Annulation

A bifunctional squaramide catalyzed enantioselective formal [3 + 3] annulation reaction with pyrazolin-5-ones and nitroallylic acetates has been developed. Densely substituted tetrahydro­pyrano­[2,3-<i>c</i>]­pyrazoles with two adjacent stereogenic centers are obtained in a highly stereocontrolled manner. Representative transformation of the annulation product to a biologically important fused dihydroisoquinoline is achieved without any appreciable loss in the diastereo- and enantioselectivity

Effect of VIP on degradation and phosphorylation of IκBα, ERK1/2 (p44/p42) MAPK, p38 MAPK, and JNK/SAPK, and expression of TLRs, NF-κB p65, MyD88 and occludin in the ileum.

<p>Cytosolic occludin, IκB-α, p-IκB-α, p44/p42 (ERK1/2), p-p44/p42, p38, p-p38, JNK/SAPK, p-JNK/SAPK, p65, TLR4, TLR2, MyD88, nuclear NF-κB p65 proteins and actin were detected by western blot analysis. Each results is the mean (n = 6)±S.E.M. *<i>P</i><0.05, **<i>P</i><0.01, ***<i>P</i><0.001.</p

Effect of VIP on expression of immune-related molecules in serum from piglets infected with ETEC K88. Each results is the mean (n = 6)±S.E.M. of cytokines levels determined in triplication.

<p>*<i>P</i><0.05, **<i>P</i><0.01, ***<i>P</i><0.001.</p

Effect of VIP on growth performance and diarrhea incidence of piglets challenged with ETEC K88.

<p>Note: ^###<i>P</i><0.001 compared to Control; **<i>P</i><0.01, ***<i>P</i><0.001 compared to ETEC K88. Values are expressed as mean ± SEM. ADG, ADFI, G:F represents average daily gain, average daily feed intake, and feed conversion efficiency (G:F), respectively.</p

Influence of VIP on morphology of intestine in piglets infected by ETEC K88 (H&E).

<p>Influence of VIP on morphology of intestine in piglets infected by ETEC K88 (H&E).</p

Differentially Abundant Features of Caecum Contents^*.

<p>*Bacterial community comparison between the groups in the level of genus; The genus listed in the table are significant between the groups. Among of them, shared genus of bacteria between groups is shown in italics bold.</p

Effect of VIP on morphology of the intestines in weaned piglets infected by ETEC K88.

<p>Note: ^#<i>P</i><0.05, ^##<i>P</i><0.01, ^###<i>P</i><0.001 compared to Control; *<i>P</i><0.05, **<i>P</i><0.01, ***<i>P</i><0.001 compared to ETEC K88. Values are expressed as mean ± SEM (n = 6, each group).</p

Asymmetric Formal [4 + 2] Annulation of <i>o</i>‑Quinone Methides with β‑Keto Acylpyrazoles: A General Approach to Optically Active <i>trans</i>-3,4-Dihydrocoumarins

An asymmetric cascade reaction between β-keto acylpyrazoles and <i>o</i>-quinone methides in a formal [4 + 2] fashion to access potentially pharmacological active <i>trans</i>-3,4-dihydrocoumarins has been achieved efficiently by using a quinine-based chiral squaramide as the catalyst. The desired products were obtained in high yields with excellent diastereo- and enantioselectivities (up to 96% yield, >19/1 dr and 96% ee) under mild reaction conditions

Differentially Abundant Features of Colon Contents^*.

<p>*Bacterial community comparison between the groups in the level of genus; The genus listed in the table are significant between the groups. Among of them, shared genus of bacteria between groups is shown in italics bold.</p