50892-99-4

Upstream product

• 617-90-3 2-furancarbonitrile 

Downstream Products

• 154345-84-3 (D,L)-3-(2-furyl)-5-(2-phenyl-1-tert-butyloxycarbonylaminoethyl)-1,2,4-oxadiazole 
• 61051-44-3 5-(2-chloro-4-nitrophenyl)-3-(2-furanyl)-1,2,4-oxadiazole 
• 61084-44-4 5-(4-Chloro-3-nitrophenyl)-3-(2-furanyl)-1,2,4-oxadiazole 
• 1117842-23-5 5-(4-chloro-2-methylphenyl)-3-(furan-2-yl)-1,2,4-oxadiazole 
• 617-90-3 2-furancarbonitrile 
• 609-38-1 furan-2-carboxylic acid amide 
• 1448510-52-8 3-phenyl-5-(2-furyl)-1,2,4-oxadiazole-4-oxide 
• 309734-72-3 5-(furan-2-yl)-3-phenyl-1,2,4-oxadiazole 
• 1622348-48-4 5-(4-chloro-2-methylphenyl)-3-(furan-2-yl)-4,5-dihydro-1,2,4-oxadiazole 
• 96898-92-9 3-(furan-2-yl)-5-(4-aminophenyl)-1,2,4-oxadiazole 
• 96898-66-7 3-(2-furyl)-5-(4-isothiocyanophenyl)-1,2,4-oxadiazole 
• 61051-45-4 5-(4-amino-2-chlorophenyl)-3-(2-furanyl)-1,2,4-oxadiazole 
• 61051-41-0 [3-Chloro-4-[3-(2-furanyl)-1,2,4-oxadiazol-5-yl]phenyl]carbamic acid, phenyl ester 
• 61051-42-1 [3-chloro-4-[3-(2-furanyl)-1,2,4-oxadiazol-5-yl]phenyl]carbamic acid, 2,2,2-trichloroethyl ester 

Relevant academic research and scientific papers

Novel 5-(quinuclidin-3-ylmethyl)-1,2,4-oxadiazoles to investigate the activation of the α7 nicotinic acetylcholine receptor subtype: Synthesis and electrophysiological evaluation

α7 nicotinic acetylcholine receptors (nAChRs) are relevant therapeutic targets for a variety of disorders including neurodegeneration, cognitive impairment, and inflammation. Although traditionally identified as an ionotropic receptor, the α7 subtype showed metabotropic-like functions, mainly linked to the modulation of immune responses. In the present work, we investigated the structure-activity relationships in a set of novel α7 ligands incorporating the 5-(quinuclidin-3-ylmethyl)-1,2,4-oxadiazole scaffold, i.e. derivatives 21a-34a and 21b-34b, aiming to identify the structural requirements able to preferentially trigger one of the two activation modes of this receptor subtype. The new compounds were characterized as partial and silent α7 nAChR agonists in electrophysiological assays, which allowed to assess the contribution of the different groups towards the final pharmacological profile. Overall, modifications of the selected structural backbone mainly afforded partial agonists, among them tertiary bases 27a-33a, whereas additional hydrogen-bond acceptor groups in permanently charged ligands, such as 29b and 31b, favored a silent desensitizing profile at the α7 nAChR.

Triaryl compound and preparation method and pharmaceutical application thereof

The invention discloses a triaryl compound as shown in a formula I which is described in the specification, physiologically acceptable salt, a preparation method of the compound, a pharmaceutical preparation containing the compound, and application of the

Synthesis of 2,4-Disubstituted Imidazoles via Nucleophilic Catalysis

A convergent, microwave-assisted protocol for the synthesis of disubstituted NH-imidazoles via nucleophilic catalysis is described. The substituted imidazoles are accessed via the intramolecular addition of a variety of amidoxime substrates to activated a

Design, synthesis and biological evaluation of triaryl compounds as novel 20S proteasome inhibitors

Thirty novel triaryl compounds were designed and synthesized based on the known proteasome inhibitor PI-1840. Most of them showed significant inhibition against the β5c subunit of human 20S proteasome, and five of them exhibited IC50 values at the sub-micromolar level, which were comparable to or even more potent than PI-1840. The most active two (1c and 1d) showed IC50 values of 0.12 and 0.18 μM against the β5c subunit, respectively, while they displayed no obvious inhibition against the β2c, β1c and β5i subunits. Molecular docking provided informative clues for the subunit selectivity. The potent and subunit selective proteasome inhibitors identified herein represent new chemical templates for further molecular optimization.

Small Molecule Inhibition of MicroRNA miR-21 Rescues Chemosensitivity of Renal-Cell Carcinoma to Topotecan

Chemical probes of microRNA (miRNA) function are potential tools for understanding miRNA biology that also provide new approaches for discovering therapeutics for miRNA-associated diseases. MicroRNA-21 (miR-21) is an oncogenic miRNA that is overexpressed in most cancers and has been strongly associated with driving chemoresistance in cancers such as renal cell carcinoma (RCC). Using a cell-based luciferase reporter assay to screen small molecules, we identified a novel inhibitor of miR-21 function. Following structure-activity relationship studies, an optimized lead compound demonstrated cytotoxicity in several cancer cell lines. In a chemoresistant-RCC cell line, inhibition of miR-21 via small molecule treatment rescued the expression of tumor-suppressor proteins and sensitized cells to topotecan-induced apoptosis. This resulted in a >10-fold improvement in topotecan activity in cell viability and clonogenic assays. Overall, this work reports a novel small molecule inhibitor for perturbing miR-21 function and demonstrates an approach to enhancing the potency of chemotherapeutics specifically for cancers derived from oncomir addiction.

COMPOSITIONS AND METHODS FOR CONTROL OF DISEASE

Compounds, compositions and methods for controlling root-originating diseases are described herein. The compounds include oxazoles, oxadiazoles and thiadiazoles. The compounds may be administered to plants, seeds, and/or soil.

COMPOSITIONS AND METHODS FOR IMPROVING AGRONOMIC CHARACTERISTICS OF PLANTS

Compounds, compositions and methods for improving one or more agronomic characteristics of desired crop plants are described herein. The compounds include oxazoles, oxadiazoles and thiadiazoles.

Discovery of highly potent triazole antifungal agents with piperidine-oxadiazole side chains

Due to increasing incidence and mortality of invasive fungal infections, discovery and development of new generations of antifungal agents represents a challenging task. On the basis of our previously reported triazole-benzyloxypiperidinyl lead compound, a series of novel triazole antifungal agents containing piperidine-oxadiazole side chains were rationally designed and synthesized. Most of the target compounds showed excellent inhibitory activity against clinically important fungal pathogens. In particular, compounds 6g (MIC = 0.031 μg mL-1) and 11b (MIC = 0.016 μg mL-1) were highly active against Candida albicans including fluconazole-resistant strains. Moreover, they showed inhibitory activity against hyphal formation with low toxicity, which were promising leads for further development. This journal is

ALPHA-KETO HETEROCYCLES AS FAAH INHIBITORS

The invention provides a series of -alpha ketoheterocyclic compounds, for example, compounds of formula (I). The compounds can inhibit fatty acid amide hydrolase and can be useful for treatment of malconditions modulated by fatty acid amide hydrolase. The invention further provides methods of making compounds of formula (I), useful intermediates for the preparation of compounds of formula (I), and methods of using compounds of formula (I) and compositions thereof.

TRIAZOLE OXADIAZOLES DERIVATIVES

The invention relates to compounds of formula (I), wherein R1, R2, Ra, Rb, X have the meanings given in claim 1. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.