51285-13-3

Usage

Uses

N''-Hydroxycyclopropanecarboximidamide

Upstream product

• 5500-21-0 cyclopropropanecarbonitrile 
• 6542-60-5 2-cyclopropylacetonitrile 

Downstream Products

• 135436-92-9 5-(2-aminophenyl)-3-cyclopropyl-1,2,4-oxadiazole 
• 137715-61-8 3-Amino-2-(3-cyclopropyl-1,2,4-oxadiazol-5-yl)-thiophene 
• 1256699-22-5 ((3S,5S)-3-(3-cyclopropyl-1,2,4-oxadiazol-5-yl)-5-(4-(trifluoromethyl)phenyl)piperidin-1-yl)(3-hydroxyazetidin-1-yl)methanone 
• 1256699-23-6 ((3R,5R)-3-(3-cyclopropyl-1,2,4-oxadiazol-5-yl)-5-(4-(trifluoromethyl)phenyl)piperidin-1-yl)(3-hydroxyazetidin-1-yl)methanone 
• 1616398-48-1 3-cyclopropyl-5-(4-methoxyphenyl)-1,2,4-oxadiazole 

Relevant academic research and scientific papers

2-(1,2,4-Oxadiazol-5-yl)anilines Based on Amidoximes and Isatoic Anhydrides: Synthesis and Structure Features

Abstract: An efficient one-pot method was developed for the synthesis of 2-(1,2,4-oxadiazol-5-yl)anilines via the reaction of amidoximes with isatoic anhydrides in a NaOH–DMSO medium at ambient temperature. The method allows to obtain structurally diverse

BAX INHIBITORS AND USES THEREOF

A compound having formula (I) or (II) for use inhibiting Bax mediated cell death and/or apoptosis.

Design, synthesis and biological activities of piperidine-spirooxadiazole derivatives as α7 nicotinic receptor antagonists

α: 7 nicotinic acetylcholine receptors (nAChRs) expressed in the nervous and immune systems have been suggested to play important roles in the control of inflammation. However, the lack of antagonist tools specifically inhibiting α7 nAChR impedes the validation of the channel as therapeutic target. To discover a selective α7 antagonist, we started a pharmacophore-based virtual screening and identified a piperidine-spirooxadiazole derivative T761–0184 that acts as a α7 antagonist. A series of novel piperidine-spirooxadiazole derivatives were subsequently synthesized and evaluated using two-electrode voltage clamp (TEVC) assay in Xenopus oocytes. Lead compounds from two series inhibited α7 with their IC50 values ranging from 3.3 μM to 13.7 μM. Compound B10 exhibited α7 selectivity over other α4β2 and α3β4 nAChR subtypes. The analysis of structure-activity relationship (SAR) provides valuable insights for further development of selective α7 nAChR antagonists.

SSAO INHIBITOR

The present invention provides an SSAO inhibitor and an application thereof in preparing a drug for treating a disease related to SSAO. In particular, the present invention provides a compound shown in formula (IV) and a pharmaceutically acceptable salt thereof.

Continued exploration of 1,2,4-oxadiazole periphery for carbonic anhydrase-targeting primary arene sulfonamides: Discovery of subnanomolar inhibitors of membrane-bound hCA IX isoform that selectively kill cancer cells in hypoxic environment

An expanded set of diversely substituted 1,2,4-oxadiazole-containing primary aromatic sulfonamides was synthesized and tested for inhibition of human carbonic anhydrase I, II, IX and XII isoforms. The initial biochemical profiling revealed a significantly

Discovery of BR102375, a new class of non-TZD PPARγ full agonist for the treatment of type 2 diabetes

As a potential treatment of type 2 diabetes, a novel PPARγ non-TZD full agonist, compound 18 (BR102375) was identified from the original lead BR101549 by the SAR efforts of the labile metabolite control through bioisosteres approach. In vitro assessments

Reactions of pentafluoropyridine with amidoximes

Abstract: In this paper, site reactivity of amidoximes with pentafluoropyridine under basic conditions in dry CH3CN was investigated. The aromatic nucleophilic substitution of pentafluoropyridine with amidoximes occurs in the 4-position of the

Copper-catalyzed one-pot synthesis of 1,2,4-triazoles from nitriles and hydroxylamine

A simple and efficient copper-catalyzed one-pot synthesis of substituted 1,2,4-triazoles through reactions of two nitriles with hydroxylamine has been developed. The protocol uses simple and readily available nitriles and hydroxylamine hydrochloride as th

NEW BICYCLIC COMPOUND FOR MODULATING G PROTEIN-COUPLED RECEPTORS

The present invention relates to a bicyclic compound for modulating G protein-coupled receptors. The inventive compound provides preventing or treating a disease associated with the modulation of G protein-coupled receptors, particularly GPR119 G protein-coupled receptors.

MODULATORS OF THE GPR119 RECEPTOR AND THE TREATMENT OF DISORDERS RELATED THERETO

The present invention relates to compounds of Formula I and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are useful as single pharmaceutical agents or in combination with one or more additional pharmaceutical agents, such as, a DPP-IV inhibitor, a biguanide, an alpha-glucosidase inhibitor, an insulin analogue, a sulfonylurea, an SGLT2 inhibitor, a meglitinide, a thiazolidinedione, or an anti-diabetic peptide analogue, in the treatment of, for example, a disorder selected from: a GPR119-receptor-related disorder; a condition ameliorated by increasing a blood incretin level; a condition characterized by low bone mass; a neurological disorder; a metabolic-related disorder; type 2 diabetes; obesity; and complications related thereto.