192332-48-2

Upstream product

• 1011-84-3 4-nitrobenzohydroximoyl chloride 
• 67-56-1 methanol 
• 619-72-7 4-nitrobenzonitrile 
• 586-78-7 para-nitrophenyl bromide 
• 68451-75-2 C₁₄H₁₁N₃O₄ 
• 68451-89-8 C₁₄H₁₀ClN₃O₄ 
• 68451-95-6 (Z)-4-nitro-N'-((4-nitrobenzoyl)oxy)benzimidamide 
• 68451-82-1 C₁₅H₁₃N₃O₅ 
• 124-41-4 sodium methylate 
• 5470-11-1 hydroxylamine hydrochloride 
• 937-31-5 (4-Nitrophenyl)acetylene 
• 584-08-7 potassium carbonate 
• 555-16-8 4-nitrobenzaldehdye 
• 2574-03-0 p-nitrobenzonitrile oxide 

Downstream Products

• 19932-97-9 3-p-nitrophenyl-4,5-dihydro-1,2,4-oxadiazol-5-one 
• 104849-79-8 N-ethoxycarbonyloxy-4-nitro-benzamidine 
• 25283-95-8 3-(4-nitro)phenyl-5-phenyl-[1,2,4]oxadiazole 
• 69792-95-6 5-methyl-3-(4-nitro-phenyl)-2⁽⁴⁾,5-dihydro-[1,2,4]oxadiazole 
• 24794-09-0 1-[3-(4-nitro-phenyl)-[1,2,4]oxadiazol-5-yl]-propan-2-one 
• 3035-86-7 3-(4-nitrophenyl)-5-piperidyl-1,2,4-oxadiazole 
• 32212-23-0 4-(4-nitro-phenyl)-2-o-tolyl-2,3-dihydro-[1,3,5,2]oxadiazaborole 
• 32230-43-6 4-(4-nitro-phenyl)-2-p-tolyl-2,3-dihydro-[1,3,5,2]oxadiazaborole 
• 32212-24-1 2-naphthalen-1-yl-4-(4-nitro-phenyl)-2,3-dihydro-[1,3,5,2]oxadiazaborole 
• 96716-48-2 O-Phenylcarbamoyl-4-nitro-benzamidoxim 
• 32212-22-9 4-(4-nitro-phenyl)-2-phenyl-2,3-dihydro-[1,3,5,2]oxadiazaborole 
• 3706-61-4 3-(4-nitro-phenyl)-5-trichloromethyl-[1,2,4]oxadiazole 
• 142114-77-0 4-methyl-2-(4-nitrophenyl)pyrimidine 3-oxide 
• 85322-19-6 [3-(4-Nitro-phenyl)-4H-[1,2,4]oxadiazin-(5Z)-ylidene]-acetic acid ethyl ester 

Relevant academic research and scientific papers

Novel chalcone/aryl carboximidamide hybrids as potent anti-inflammatory via inhibition of prostaglandin E2 and inducible NO synthase activities: design, synthesis, molecular docking studies and ADMET prediction

Two series of chalcone/aryl carboximidamide hybrids 4a–f and 6a–f were synthesised and evaluated for their inhibitory activity against iNOS and PGE2. The most potent derivatives were further checked for their in?vivo anti-inflammatory activity utilising carrageenan-induced rat paw oedema model. Compounds 4c, 4d, 6c and 6d were proved to be the most effective inhibitors of PGE2, LPS-induced NO production, iNOS activity. Moreover, 4c, 4d, 6c and 6d showed significant oedema inhibition ranging from 62.21% to 78.51%, compared to indomethacin (56.27 ± 2.14%) and celecoxib (12.32%). Additionally, 4c, 6a and 6e displayed good COX2 inhibitory activity while 4c, 6a and 6c exhibited the highest 5LOX inhibitory activity. Compounds 4c, 4d, 6c and 6d fit nicely into the pocket of iNOS protein (PDB ID: 1r35) via the important amino acid residues. Prediction of physicochemical parameters exhibited that 4c, 4d, 6c and 6d had acceptable physicochemical parameters and drug-likeness. The results indicated that chalcone/aryl carboximidamides 4c, 4d, 6c and 6d, in particular 4d and 6d, could be used as promising lead candidates as potent anti-inflammatory agents.

Novel 1,2,4-oxadiazole-chalcone/oxime hybrids as potential antibacterial DNA gyrase inhibitors: Design, synthesis, ADMET prediction and molecular docking study

New antibacterial drugs are urgently needed to tackle the rapid rise in multi-drug resistant bacteria. DNA gyrase is a validated target for the development of new antibacterial drugs. Thus, in the present investigation, a novel series of 1,2,4-oxadiazole-

Ferrocenylethenyl-substituted oxadiazoles with phenolic and nitro anchors as sensitizers in dye sensitized solar cells

Three new ferrocenyl oxadiazoles, viz. (E)-2-(4-hydroxyphenyl)-5-(2-ferrocenyl-ethen-1-yl)-1,3,4-oxadiazole (D2), (E)-2-(4-nitrophenyl)-5-(2-ferrocenyl-ethen-1-yl)-1,3,4-oxadiazole (D3) and (E)-3-(4-nitrophenyl)-5-[5-(2-ferroceneylethen-1-yl)-1,3,4-oxadia

Design and synthesis of new triarylimidazole derivatives as dual inhibitors of BRAFV600E/p38α with potential antiproliferative activity

Recent studies have shown that combining kinase inhibitors has additive and synergistic effects. BRAFV600E and p38α have been extensively studied as potential therapeutic targets for a variety of diseases. In keeping with our interest in developing multi-targeted anticancer agents, a series of novel triaryl-imidazole-based analogues containing 3-aryl-1,2,4-oxadiazoles moiety (4a-h, Scaffold B) and their reaction intermediates aryl carboximidamides moiety (3a-h, Scaffold A) have been rationally designed, synthesized, and evaluated in vitro for their antiproliferative activity as dual p38α/BRAFV600E inhibitors. The results revealed that the presence of the carboximidamide moiety is required for activity, and the best activity correlates with the Ar = 1,2-benzodioxole (3e) ≥ 4-CH3O-C6H5-(3c) > 2-naphthyl (3h) > 4-Cl-C6H5 (3b). Ring closure of carboximidamide to 1,2,4-oxadiazole significantly reduces the activity. The results of docking study into p38α revealed higher binding affinities for compounds 3c, 3e, and 3h compared to the co-crystallized ligand, SB2. However, the docking study of compounds 3c and 3e into BRAFV600E revealed slightly lower affinities than vemurafenib.

New 1,2,4-oxadiazole derivatives with positive mGlu4 receptor modulation activity and antipsychotic-like properties

Considering the allosteric regulation of mGlu receptors for potential therapeutic applications, we developed a group of 1,2,4-oxadiazole derivatives that displayed mGlu4 receptor positive allosteric modulatory activity (EC50 = 282–656 nM). Selectivity screening revealed that they were devoid of activity at mGlu1, mGlu2 and mGlu5 receptors, but modulated mGlu7 and mGlu8 receptors, thus were classified as group III-preferring mGlu receptor agents. None of the compounds was active towards hERG channels or in the mini-AMES test. The most potent in?vitro mGlu4 PAM derivative 52 (N-(3-chloro-4-(5-(2-chlorophenyl)-1,2,4-oxadiazol-3-yl)phenyl)picolinamide) was readily absorbed after i.p. administration (male Albino Swiss mice) and reached a maximum brain concentration of 949.76 ng/mL. Five modulators (34, 37, 52, 60 and 62) demonstrated significant anxiolytic- and antipsychotic-like properties in the SIH and DOI-induced head twitch test, respectively. Promising data were obtained, especially for N-(4-(5-(2-chlorophenyl)-1,2,4-oxadiazol-3-yl)-3-methylphenyl)picolinamide (62), whose effects in the DOI-induced head twitch test were comparable to those of clozapine and better than those reported for the selective mGlu4 PAM ADX88178.

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

Synthesis of 3(5)-aryl-5(3)-pyrazolyl-1,2,4-oxadiazole nitro derivatives

[Figure not available: see fulltext.] A method was developed for the synthesis of 3(5)-aryl-5(3)-pyrazolyl-1,2,4-oxadiazoles by acylation of amidoximes with acyl chlorides, followed by cyclization of pyrazolyl-O-acylamidoximes into the respective oxadiazoles. Nitration of these products was studied, in combination with nucleophilic substitution reactions in the obtained nitro derivatives.

One-pot synthesis of 1,2,4-oxadiazoles from chalcogen amino acid derivatives under microwave irradiation

A series of sulfur- and selenium-bearing, amino acid-derived 1,2,4-oxadiazoles were obtained by a simple procedure. The method consists of EDC-promoted coupling of chalcogen amino acid derivatives with arylamidoximes in acetone, followed by solvent removal and microwave irradiation in water medium. Influence of amidoxime substituents, of the chalcogen atom and of the amino acid side chain is discussed. The results showed this to be a fast, easy and effective method to obtain these compounds, with good functional-group tolerance, potentially favouring future applications in organic synthesis.

Imidazole hydrochloride promoted synthesis of 3,5-disubstituted-1,2,4-oxadiazoles

Imidazole hydrochloride as an additive promotes the reaction of amidoximes and DMA derivatives to generated 3,5-disubstituted-1,2,4-oxadiazoles in low to excellent yields without the use of coupling reagents, oxidants, strong acids or bases and other additives.

NEW PROCESS FOR THE PREPARATION OF AMENAMEVIR

The present invention relates to an improved process for the preparation of Amenamevir and derivatives thereof via a four component Ugi reaction.