58015-02-4

Upstream product

• 5428-32-0 N,N'-bis(4-methoxybenzylidene)ethylenediamine 
• 64-18-6 formic acid 
• 123-11-5 4-methoxy-benzaldehyde 
• 107-15-3 ethylenediamine 

Downstream Products

• 67360-10-5 4,4'-((ethane-1,2-diylbis(azanediyl))bis(methylene))diphenol 
• 103168-98-5 1,3-bis-(4-methoxy-benzyl)-2-phenyl-imidazolidine 
• 103169-09-1 2-[1,3-bis-(4-methoxy-benzyl)-imidazolidin-2-yl]-phenol 
• 111033-61-5 1,3-bis-(4-methoxy-benzyl)-2-methyl-imidazolidine 
• 102753-66-2 2-tert-butyl-1,3-bis-(4-methoxy-benzyl)-imidazolidine 
• 7248-51-3 1,3-bis-(4-methoxy-benzyl)-2-propyl-imidazolidine 
• 102556-27-4 2-isopropyl-1,3-bis-(4-methoxy-benzyl)-imidazolidine 
• 102946-59-8 1,3-bis-(4-methoxy-benzyl)-2-o-tolyl-imidazolidine 

Relevant academic research and scientific papers

Synthesis and biological evaluation of novel cYY analogues targeting Mycobacterium tuberculosis CYP121A1

The rise in multidrug resistant (MDR) cases of tuberculosis (TB) has led to the need for the development of TB drugs with different mechanisms of action. The genome sequence of Mycobacterium tuberculosis (Mtb) revealed twenty different genes coding for cy

H2depda: An acyclic adjuvant potentiates meropenem activity in vitro against metallo-β-lactamase-producing enterobacterales

Metallo-β-lactamase (MBL)-producing carbapenem-resistant Enterobacterales (CRE) pose an emerging threat to public health worldwide. An effective inhibitor of MBLs is therefore urgently needed for clinical use. In this study, two acyclic pyridine-containin

Design, synthesis and evaluation against Mycobacterium tuberculosis of azole piperazine derivatives as dicyclotyrosine (cYY) mimics

Three series of azole piperazine derivatives that mimic dicyclotyrosine (cYY), the natural substrate of the essential Mycobacterium tuberculosis cytochrome P450 CYP121A1, were prepared and evaluated for binding affinity and inhibitory activity (MIC) against M. tuberculosis. Series A replaces one phenol group of cYY with a C3-imidazole moiety, series B includes a keto group on the hydrocarbon chain preceding the series A imidazole, whilst series C explores replacing the keto group of the piperidone ring of cYY with a CH2-imidazole or CH2-triazole moiety to enhance binding interaction with the heme of CYP121A1. The series displayed moderate to weak type II binding affinity for CYP121A1, with the exception of series B 10a, which displayed mixed type I binding. Of the three series, series C imidazole derivatives showed the best, although modest, inhibitory activity against M. tuberculosis (17d MIC = 12.5 μg/mL, 17a 50 μg/mL). Crystal structures were determined for CYP121A1 bound to series A compounds 6a and 6b that show the imidazole groups positioned directly above the haem iron with binding between the haem iron and imidazole nitrogen of both compounds at a distance of 2.2 ?. A model generated from a 1.5 ? crystal structure of CYP121A1 in complex with compound 10a showed different binding modes in agreement with the heterogeneous binding observed. Although the crystal structures of 6a and 6b would indicate binding with CYP121A1, the binding assays themselves did not allow confirmation of CYP121A1 as the target.

One-pot synthesis of imidazolinium salts via the ring opening of tetrahydrofuran

A new one-pot synthesis of C2-hydroxypropyl-substituted imidazolinium salts via the ring opening of tetrahydrofuran (THF) with N,N′-disubstituted diamines has been developed. Preliminary studies of the reaction mechanism suggest the CO2-promoted oxidative ring opening of THF followed by Hg(ii)-mediated oxidation of an imidazolidine intermediate. These novel C2-substituted imidazolinium salts have shown to be active catalysts for the aza-Diels-Alder reactions.

Metal beta-lactamase inhibitor open chain pyridine carboxylic acid derivative and preparation method thereof

Belonging to the field of medicinal chemistry, the invention discloses a metal beta-lactamase inhibitor open chain pyridine carboxylic acid derivative and a preparation method thereof. The compound has the following structure shown as the specification. T

FBXO3 INHIBITORS

The present application discloses benzathine and related compounds and their use as FBXO-3 inhibitors.

Synthesis, cytotoxicity, antibacterial and antileishmanial activities of imidazolidine and hexahydropyrimidine derivatives

This paper describes the synthesis and in vitro biological activities of imidazolidine and hexahydropyrimidine derivatives against bacteria (Escherichia coli, Staphylococcus aureus and Mycobacterium tuberculosis) and Leishmania protozoa. Out of sixteen heterocyclic derivatives tested, none were cytotoxic against mammalian cells. The compounds showed significant bacterial effects and leishmanicidal activity. Compounds 4a and 4c were active against S. aureus and E. coli, respectively. Compounds 3a-3f, 4h and 4i presented promising results against M. tuberculosis, with MIC values ranging from 12.5 to 25.0 μg/mL, comparable to the "first and second line" drugs used to treat tuberculosis. Compounds 4a, 4c and 4e were active against L major. Three of them were structurally characterized by single-crystal X-ray diffraction.

Reversible aminal formation: Controlling the evaporation of bioactive volatiles by dynamic combinatorial/covalent chemistry

Dynamic mixtures generated by reversible aminal formation efficiently prolong the duration of evaporation of bioactive volatile aldehydes. Secondary diamines used for the generation of dynamic mixtures are obtained by treatment of primary diamines with carbonyl compounds and reduction of the diimines with NaBH4. The reversibilities of the reactions were demonstrated by NMR measurements in buffered aqueous solutions. Kinetic rate constants and equilibrium constants for the formation and hydrolysis of aminals were determined. The performance of dynamic mixtures as delivery systems for perfumery ingredients was tested after deposition onto cotton, and the long-lastingness of fragrance evaporation was investigated by dynamic headspace analysis against a reference sample. The simplicity of the concept together with its excellent performance makes this delivery system highly interesting for applied perfumery. Reversible aminal formation might also be successfully applicable to dynamic combinatorial/covalent chemistry for screening of pharmaceutically or catalytically active ligands and receptors. The evaporation of bioactive volatiles that are emitted from flowers to attract insects and that are used as fragrances in our everyday life is limited in time. Dynamic mixtures obtained by reversible aminal formation of suitably designed diamines with volatile aldehydes prolong the perception of these compounds in functional perfumery.

Synthesis of [N, N'-Bis(5-benzoyl-4-phenylthiazol-2-yl)-N, N-bisbenzyl]ethane-1, 2-diamines

Synthesis of [N,N'-bis(N-benzoylthiocarbamoyl)-N,N'-bis(benzyl)]ethane-1,2- diamines 4a-h, their cyclization to [N,N'-bis(5-benzoyl-4-phenylthiazol-2-yl)-N, N'-bisbenzyl]ethane-1,2-diamines 5a-h by reaction with phenacyl bromide and the results of antibacterial activity assay of 4a-h and 5a-h are reported.

CONTROLLED RELEASE OF ACTIVE ALDEHYDES AND KETONES FROM EQUILIBRATED DYNAMIC MIXTURES

The present invention concerns a dynamic mixture obtained by combining, in the presence of water, at least one diamine derivative, comprising at least one benzylamine moiety, with at least one active aldehyde or ketone. The invention's mixture is capable of releasing in a controlled and prolonged manner said active compound, in particular perfuming ingredients, in the surrounding environment.