148342-52-3

Upstream product

• 108-91-8 cyclohexylamine 
• 13623-94-4 1,1-di(methylsulfanyl)-2-nitroethylene 
• 75-52-5 nitromethane 
• 54208-97-8 N-cyclohexyl carbonimidodithioic acid dimethyl ester 

Downstream Products

• 1072452-14-2 N-(1-(3-(5-methyl-1H-imidazol-1-yl)propylamino)-2-nitrovinyl)cyclohexanamine 
• 1070654-67-9 N-(3-(1H-imidazol-1-yl)propyl)-N'-cyclohexyl-2-nitroethene-1,1-diamine 

Relevant academic research and scientific papers

Synthesis and biological evaluation of sulfonylcyanoguanidines and sulfonamidonitroethylenes as bioisosteres of hypoglycemic sulfonylureas

Sulfonylcyanoguanidines and sulfonamidonitroethylenes are bioisosteres of hypoglycemic sulfonylureas and were prepared and evaluated for their insulin release potency from rat pancreatic islets. At 25 μM, both bioisosteres of glibenclamide, sulfonylcyanoguanidine 22 and sulfonamidonitroethylene 23, were as patent as their parent on insulin secretion.

CATALYTIC AND COMPUTER SIMULATION STUDIES OF CARBON-SULPHUR BOND CLEAVAGE OVER ZEOLITE-Y

N-Substituted carbonimidodithioic acid dimethyl esters, when reacted with an active methylene compound such as nitromethane, undergo carbon-carbon bond formation followed by carbon-sulphur bond cleavage in the presense of zeolite catalysts to give 1-subst

Design, synthesis, and anticonvulsant activity of 1-(pyrid-3- ylsulfonamido)-2-nitroethylenes

The lipophilic 1-cycloalkylamino-1-(pyrid-3-yl-sulfonamido)-2- nitroethylenes were synthesized as bioisosteres of BM-34, an anticonvulsant sulfonylthiourea. Compound 17 (ip) emerged from the maximal electroshock seizure (MES) test with a 50% effective dos

An efficient synthesis of N-substituted 3-nitrothiophen-2-amines

A novel protocol for the synthesis of 3-nitro-N-aryl/alkylthiophen-2-amines in good yields from the reaction of α-nitroketene N,S-aryl/alkylaminoacetals and 1,4-dithiane-2,5-diol in the presence of K2CO3 in refluxing ethanol is descr

Synthesis and biological evaluation of novel 2,3-disubstituted quinoxaline derivatives as antileishmanial and antitrypanosomal agents

Quinoxalines belong to the N-containing heterocyclic compounds that stand out as having promising biological activity due to their privileged scaffold. In this work, we report the synthesis, antileishmanial, and antitrypanosomal properties of 46 new 2,3-disubstituted quinoxaline and 40 previously reported derivatives. Among all of the compounds screened for in vitro activity against epimastigotes and trypomastigotes of Trypanosoma cruzi and promastigotes of Leishmania amazonensis as well as mammalian toxicity on LLCMK2 cells and J774 macrophages, analogues from series 5, 6, 7, 9, 12, and 13 displayed high activity at micromolar IC50 and EC50 concentrations. Sixteen quinoxaline derivatives were selected and evaluated on T. cruzi and/or L. amazonensis amastigotes. The most active compounds were 6a-b and 7d-e, on all evolutive forms of L. amazonensis and T. cruzi evaluated with IC50 values 0.1-0.8 μM on promastigotes and epimastigotes 1.4-8.6 on amastigotes. Compounds 5k, 12b and 13a were the most selective (SI = 19.5-38.4) on amastigotes of T. cruzi. In general their activity was directly related to the methylsulfoxyl, methylsulfonyl, and amine groups as well as the presence of chorine or bromine in the molecules. The current results indicate that these quinoxaline derivatives are novel and promising agents for further development towards a treatment for Chagasg € disease and leishmaniasis.

Microwave-Assisted synthesis of nitroketene N, S-arylaminoacetals

In this paper we report the use of microwaves as heat source to promote the synthesis of a series of nitroketene N, S-acetals with good to excellent isolated yields. These compounds are very useful intermediates for synthesizing nitrogen-containing hetero

Inhibitors for human glutaminyl cyclase by structure based design and bioisosteric replacement

The inhibition of human glutaminyl cyclase (hQC) has come into focus as a new potential approach for the treatment of Alzheimer's disease. The hallmark of this principle is the prevention of the formation of Aβ 3,11(pE)-40,42, as these Aβ-speci

NITROVINYL-DIAMINE DERIVATIVES AS GLUTAMINYL CYCLASE INHIBITORS

The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers, stereoisomers and polymorphs thereof, wherein A, B

Benzene-sulphonamide derivatives and their uses

Benzene-sulphonamide derivatives complying with the general formula (I): in which the different symbols have different meanings, their optical isomers and the salts pharmacologically acceptable of these derivatives, as well as their uses for drug manufacture and as radiolabelled pharmacological tools of the thromboxan A2 receptors.

Unique zeolite-catalyzed synthesis of nitroketene S,N-acetals

Dimethyl carbonimidodithioates (4a-g, 7a-c) derived from various primary amines and amino acid esters [glycine, (L)-alanine and (L)-phenylalanine] have been condensed with nitromethane in the presence of the rare-earth exchanged zeolite RE(70%)Na Y to give the S,N-acetals (5a-g, 8a-c). Mercuric chloride catalyzed hydrolysis of these (8a-c) has led to the nitroacetyl derivatives (9a-c). The glycine derivative (7a) gives a dimeric product (11) when heated alone with the zeolite.