203071-48-1

Upstream product

• 14199-15-6 Methyl 4-hydroxyphenylacetate 
• 109-64-8 1,3-dibromo-propane 

Downstream Products

• 59510-83-7 2-[4-(3-bromopropoxy)phenyl]acetic acid 
• 228577-59-1 methyl 4-(3-(2-propyl-4-phenoxy-phenoxy)-propoxy)phenylacetate 

Relevant academic research and scientific papers

Novel Carboline Fungal Histone Deacetylase (HDAC) Inhibitors for Combinational Treatment of Azole-Resistant Candidiasis

Due to the evolution and development of antifungal drug resistance, limited efficacy of existing drugs has led to high mortality in patients with serious fungal infections. To develop novel antifungal therapeutic strategies, herein a series of carboline fungal histone deacetylase (HDAC) inhibitors were designed and synthesized, which had potent synergistic effects with fluconazole against resistant Candida albicans infection. In particular, compound D12 showed excellent in vitro and in vivo synergistic antifungal efficacy with fluconazole to treat azole-resistant candidiasis. It cooperated with fluconazole in reducing the virulence of C. albicans by blocking morphological mutual transformation and inhibiting biofilm formation. Mechanism studies revealed that the reversion of drug resistance was due to downregulation of the expression of the azole target gene ERG11 and efflux gene CDR1. Taken together, fungal HDAC inhibitor D12 offered a promising lead compound for combinational treatment of azole-resistant candidiasis.

Lipid reducing activity of novel cholic acid (CA) analogs: Design, synthesis and preliminary mechanism study

Bile acids, initially discovered as endogenous ligands of farnesoid X receptor (FXR), play a central role in the regulation of triglyceride and cholesterol metabolism and have recently emerged as a privileged structure for interacting with nuclear receptors relevant to a large array of metabolic processes. In this paper, phenoxy containing cholic acid derivatives with excellent drug-likeness have been designed, synthesized, and assayed as agents against cholesterol accumulation in Raw264.7 macrophages. The most active compound 14b reduced total cholesterol accumulation in Raw264.7 cells up to 30.5% at non-toxic 10 μM and dosage-dependently attenuated oxLDL-induced foam cell formation. Western blotting and qPCR results demonstrate that 14b reduced both cholesterol and lipid in Raw264.7 cells through (1) increasing the expression of cholesterol transporters ABCA1 and ABCG1, (2) accelerating ApoA1-mediated cholesterol efflux. Through a cell-based luciferase reporter assay and molecular docking analysis, LXR was identified as the potential target for 14b. Interestingly, unlike conventional LXR agonist, 14b did not increase lipogenesis gene SREBP-1c expression. Overall, these diverse properties disclosed herein highlight the potential of 14b as a promising lead for further development of multifunctional agents in the therapy of cardiovascular disease.

Beta- tetrahydro-carboline antifungal drug and preparation method and application thereof

The invention discloses a beta-tetrahydro-carboline antifungal compound and a pharmaceutically acceptable salt thereof. The structure of the compound is shown as the general formula I, wherein n is 1to 3; R1 is hydrogen or monosubstituted acetylene or polysubstituted acetylene in any optional position on the benzene ring, X is O or NH, R2 is substituted or unsubstituted aliphatic or aromatic ring; or X is NR3, R2 and R3 are individually lower alkyl and substituted or unsubstituted aliphatic or aromatic ring; or X is N, R2 and X composes substituted or unsubstituted heterocycloalkyl. The invention also discloses a preparation method of the compound and the application of the compound in preparation of antifungal drugs. The compound has the characteristic of well antifungal activity, the result of partial compound is better than that of the control drug fluconazole, and the compound can be utilized to prepare antifungal drugs. The experiment result also show that the combined usage of the partial compound and fluconazole has good synergistic effect to clinically isolated fluconazole-resistant candida albicans.

Cholic acid derivatives and their preparation method and medical application

The invention relates to the field of pharmaceutical chemistry and relates to cholic acid derivatives and their preparation method and medical application and particularly relates to cholic acid derivatives having the general formula (I), their preparation method, a pharmaceutical composition containing the compounds, medical application of the cholic acid derivatives, and medical application of the cholic acid derivatives as drugs for preventing or treating hyperlipidemia, obesity or type II diabetes.

Antileukotrienic N-arylethyl-2-arylacetamides in the treatment of ulcerative colitis

A series of arylacetic acid derivatives bearing methyl(arylethyl)amino groups were prepared and their antileukotrienic activities involving LTB4 were evaluated. Regression analysis has shown a strong dependence of these activities on lipophilic

ARYLTHIAZOLIDINEDIONE DERIVATIVES

Substituted 5-aryl-2,4-thiazolidinediones are potent agonists of PPAR, and are therefore useful in the treatment, control or prevention of diabetes, hyperglycemia, hyperlipidemia (including hypercholesterolemia and hypertriglyceridemia), atherosclerosis, obesity, vascular restenosis, and other PPAR alpha , delta and/or gamma mediated diseases, disorders and conditions.

MODULATORS OF PPAR AND METHODS OF THEIR PREPARATION

The present invention is directed to certain novel compounds represented by Formula (I) and pharmaceutically acceptable salts, solvates, hydrates and prodrugs thereof. The present invention is also directed to methods of making and using such compounds and pharmaceutical compositions containing such compounds to treat or control a number of diseases mediated by PPAR such as glucose metabolism, lipid metabolism and insulin secretion, specifically Type 2 diabetes, hyperinsulinemia, hyperlipidemia, hyperuricemia, hypercholesteremia, atherosclerosis, one or more risk factors for cardiovascular disease, Syndrome X, hypertriglyceridemia, hyperglycemia, obesity and eating disorders.

Substituted aryloximes

The present invention relates to substituted aryl oximes and methods of using them.

Novel thieno oxazine analogues as antihyperglycemic and lipid modulating agents

A series of phenyl acetic acid and α-hydroxy propionic acid derivatives were synthesized. In vivo studies of the compounds indicated compound 2c as the most potent in one of the series, which has both glucose and lipid lowering properties. The syntheses and biological studies have been discussed.

Arylthiazolidinedione derivatives

Substituted 5-aryl-2,4-thiazolidinediones are potent agonists of PPAR, and are therefore useful in the treatment, control or prevention of diabetes, hyperglycemia, hyperlipidemia (including hypercholesterolemia and hypertriglyceridemia), atherosclerosis, obesity, vascular restenosis, and other PPAR α, δ and/or γ mediated diseases, disorders and conditions.