110830-17-6

Upstream product

• 120-57-0 piperonal 
• 32085-04-4 3-acetyl-2-thioxoimidazolidin-4-one 
• 503-87-7 2-thiohydantoin 
• 495-76-1 piperonol 

Downstream Products

• 1402230-96-9 (5Z)-2-[4-[2-[2-(2-azidoethoxy)ethoxy]ethoxy]phenylamino]-5-(benzo[1,3]dioxol-5-ylmethylene)-3,5-dihydroimidazol-4-one 
• 1430324-81-4 (5Z)-2-[4-[2-[2-[2-(2-aminoethoxy)ethoxy]ethoxy]ethoxy]phenylamino]-5-(benzo[1,3]dioxol-5-ylmethylene)-3,5-dihydroimidazol-4-one 
• 1402230-97-0 (5Z)-2-[4-[2-[2-(2-aminoethoxy)ethoxy]ethoxy]phenylamino]-5-(benzo[1,3]dioxol-5-ylmethylene)-3,5-dihydroimidazol-4-one 
• 1112978-28-5 (5Z)-5-(1,3-benzodioxol-5-ylmethylidene)-2-methylsulfanyl-3,5-dihydro-4H-imidazol-4-one 

Relevant academic research and scientific papers

Leucettamine B analogs and their carborane derivative as potential anti-cancer agents: Design, synthesis, and biological evaluation

Leucettamine B is a natural product found in marine sponge Leucetta microraphis. Several of analogs of its family, such as aplysinopsine and clathridine, are medicinally active molecules which have applications in many pharmaceuticals and healthcare products; however, thus far, leucettamine B has not been studied. In this report, we describe the synthesis of a new class of analogs of leucettamine B obtained by Knoevenagel condensation using a microwave reactor. The 25 newly synthesized compounds were tested against MDA-MB-468, SW480, and Mahlavu cell lines for anticancer activity. Among them, the carborane-based compound (Z)-5-(benzo[d][1,3]dioxol-5-ylmethylene)-3-(1-closo-carboranyl)-2-thioxo -thiazolidin-4-one (49) and (Z)-5-(benzo[d][1,3]dioxol-5-ylmethylene)-3-(2-(pyrrolidin-1-yl)ethyl)-2-thioxothiazolidin-4-one (31) derivatives were found to have the most potential for use against tumor cells. The carborane derivative 49 had the lowest IC50 value against the SW480 cell line (4.7 μM) and the Mahlavu (6.6 μM) cell line. Furthermore, compound 31 also had a low IC50 value against SW480 (7.5 μM). Our research shows that leucettamine B analogs might have potential for use in cancer chemotherapy.

Antimycobacterial activity of 5-arylidene derivatives of hydantoin

The synthesis of various 5-arylidene-2-thiohydantoins and results of the primary assay in vitro for their antimycobacterial activity is reported. Eight of those compounds exhibited >90% inhibition of Mycobacterium tuberculosis growth and for them the minimum inhibitory concentrations, cytotoxicity (IC50) and the selectivity index values were determined. The most active structure, (5Z)-5-(1,1′-biphenyl-4-ylmethylene)-2-thioxoimidazolidin-4-one, showed MIC=0.78 μg/ml. For all compounds logP and logD (pH 6.5) values were calculated.

USE OF HETEROCYCLIC DERIVATIVES WITH CARDIOMYOCYTE PROLIFERATION ACTIVITY FOR TREATMENT OF HEART DISEASES

Provided herein is the use of heterocyclic derivatives with cardiomyocyte proliferation activity for treatment of heart diseases. Specifically, disclosed is the use of compounds of formula (I) or a pharmaceutically acceptable salt, a solvate, a stereoisomer or a prodrug thereof; and application thereof. Definition of each group in the formula can be found in the specification for details.

NOVEL HETEROCYCLIC DERIVATIVES WITH CARDIOMYOCYTE PROLIFERATION ACTIVITY FOR TREATMENT OF HEART DISEASES

Provided are novel heterocyclic derivatives with cardiomyocyte proliferation activity for treatment of heart diseases. Specifically, provided are the compounds of formula (I) or pharmaceutically acceptable salts, stereoisomers, solvates or prodrugs, prepa

Microwave-Assisted condensation reactions of acetophenone derivatives and activated methylene compounds with aldehydes catalyzed by boric acid under solvent-free conditions

We here disclosed a new protocol for the condensation of acetophenone derivatives and active methylene compounds with aldehydes in the presence of boric acid under microwave conditions. Implementation of the reaction is simple, healthy and environmentally

Chemical synthesis and biological validation of immobilized protein kinase inhibitory Leucettines

Leucettines, a family of marine sponge-derived 2-aminoimidazolone alkaloids, are potent inhibitors of DYRKs (dual-specificity, tyrosine phosphorylation regulated kinases) and CLKs (cdc2-like kinases). They constitute promising pharmacological leads for the treatment of several diseases, including Alzheimer's disease and Down syndrome. In order to investigate the scope of potential targets of Leucettine L41, a representative member of the chemical class, we designed an affinity chromatography strategy based on agarose-immobilized leucettines. A synthesis protocol for the attachment of a polyethylene (3 or 4 units) linker to L41 was first established. The linker attachment site on L41 was selected on the basis of the co-crystal structure of L41 with several kinases. L41 was then covalently bound to agarose beads through the primary amine located at the end of the linker. Control, kinase inactive Leucettine was also immobilized, as well as free linker devoid of ligand. Extracts of several mouse tissues revealed a complex pattern of interacting proteins, some of which probably resulting from non-specific, hydrophobic binding, while others representing bona fide Leucettine-interacting proteins. DYRK1A and GSK-3 (glycogen synthase kinase-3) were confirmed as interacting targets by Western blotting in various mouse tissues. The Leucettine affinity chromatography resin constitutes a powerful tool to purify and identify the targets of this new promising therapeutic class of molecules.

CONDENSATION ON ALUMINA: III - SYNTHESIS OF 5-ALKYLIDENE, 2-THIOHYDANTOIN FROM 3-ACETYL, 2-THIOHYDANTOIN

A convenient procedure for the synthesis of 5-alkylidene, 2-thiohydantoin is described.