18092-16-5

Upstream product

• 541-59-3 maleiimide 
• 603-35-0 triphenylphosphine 

Downstream Products

• 99885-61-7 3(Z)-(4-hydroxypentylidene)-2,5-pyrrolidinedione 
• 92013-82-6 3(E)-(4-hydroxypentylidene)-2,5-pyrrolidinedione 
• 14063-01-5 3-benzylidenepyrrolidin-2,5-dione 
• 191800-48-3 3-(2-methoxybenzylidene)pyrrolidin-2,5-dione 
• 911129-02-7 3-(4-fluorobenzylidene)pyrrolidine-2,5-dione 
• 1198098-05-3 (E)-3-(4-chlorobenzylidene)pyrrolidine-2,5-dione 
• 14063-01-5 (E)-3-benzylidenepyrrolidine-2,5-dione 
• 1198098-07-5 (E)-3-(4-methoxybenzylidene)pyrrolidine-2,5-dione 
• 1198098-09-7 (E)-3-(4-hydroxy-3-methoxybenzylidene)pyrrolidine-2,5-dione 
• 1198098-04-2 (E)-3-(3-hydroxybenzylidene)pyrrolidine-2,5-dione 
• 1198098-06-4 (E)-3-(4-bromobenzylidene)pyrrolidine-2,5-dione 
• 1198098-08-6 (E)-3-(4-(dimethylamino)benzylidene)pyrrolidine-2,5-dione 

Relevant academic research and scientific papers

Using T-Hg-T and C-Ag-T: A four-input dual-core molecular logic gate and its new application in cryptography

A simple four-input dual-core (thymine & cytosine) logic gate was successfully developed that utilized a succinic imide labelled pyrene probe as the signal responser. Moreover, this molecular logic gate could be made into fluorescent paper and applied in the field of cryptography.

Synthesis of a naphthalocyanine-like dye: The first report on Zn(II)-1,6-methano[10]annulenecyanine

The synthesis of the new dye 1,6-methano[10]annulenecyanine is described. For this purpose, the 3,4-dicyano-1,6-methano[10]annulene and 3,4-carboxyimide-1,6-methano[10]annulene buildings blocks were synthesized in six to eight steps. In both cases, these

Identification of a Pyrrole Intermediate Which Undergoes C-Glycosidation and Autoxidation to Yield the Final Product in Showdomycin Biosynthesis

Showdomycin is a C-nucleoside bearing an electrophilic maleimide base. Herein, the biosynthetic pathway of showdomycin is presented. The initial stages of the pathway involve non-ribosomal peptide synthetase (NRPS) mediated assembly of a 2-amino-1H-pyrrole-5-carboxylic acid intermediate. This intermediate is prone to air oxidation whereupon it undergoes oxidative decarboxylation to yield an imine of maleimide, which in turn yields the maleimide upon acidification. It is also shown that this pyrrole intermediate serves as the substrate for the C-glycosidase SdmA in the pathway. After coupling with ribose 5-phosphate, the resulting C-nucleoside undergoes a similar sequence of oxidation, decarboxylation and deamination to afford showdomcyin after exposure to air. These results suggest that showdomycin could be an artifact due to aerobic isolation; however, the autoxidation may also serve to convert an otherwise inert product of the biosynthetic pathway to an electrophilic C-nucleotide thereby endowing showdomycin with its observed bioactivities.

Synthesis and biological evaluation of thiazole derivatives as GPR119 agonists

A series of 4-(phenoxymethyl)thiazole derivatives was synthesized and evaluated for their GPR119 agonistic effect. Several 4-(phenoxymethyl)thiazoles with pyrrolidine-2,5-dione moieties showed potent GPR119 agonistic activities. Among them, compound 27 and 32d showed good in vitro activity with an EC50 value of 49 nM and 18 nM, respectively with improved human and rat liver microsomal stability compare with MBX-2982. Compound 27 & 32d did not exhibit significant CYP inhibition, hERG binding, and cytotoxicity. Moreover, these compounds lowered the glucose excursion in mice in an oral glucose-tolerance test.

Heterocyclic substituted styrene compound and use thereof

The invention relates to a heterocyclic substituted styrene compound and its use. The invention discloses a heterocyclic radical, alkoxy and halogen modified styrene compound. Results of inhibition activity of the compound against Syk (spleen tyrosine kinase) show that the compound has inhibition activity against the Syk (spleen tyrosine kinase), and part of the compound has stronger inhibition activity against the Syk, and a structure foundation for further design and development of new Syk inhibitor-class rheumatoid arthritis (RA) therapy drugs is laid.

New compounds having skin whitening, antioxidant and PPAR activity, and medical use thereof

PURPOSE: A novel compound with skin whitening, antioxidation, and PPAR activation effects, and a medical use thereof are provided to be used for a pharmaceutical composition or a cosmetic product. CONSTITUTION: A compound is denoted by chemical formula 1. A skin whitening composition contains the compound as an active ingredient. An antioxidative composition for preventing or treating oxidative diseases contains the compound of chemical formula 1 as an active ingredient. The oxidative diseases are selected among skin aging, pigmentation, wrinkling, psoriasis, or eczema. The composition prevents or treats diseases which are regulated by PPAR(peroxisome proliferator-activated receptor) activity. The PPAR includes PPAR alpha or PPAR gamma.

INHIBITORS OF THE NOTCH TRANSCRIPTIONAL ACTIVATION COMPLEX AND METHODS FOR USE OF THE SAME

Disclosed herein are inhibitors of the Notch transcriptional activation complex, and methods for their use in treating or preventing diseases, such as cancer. The inhibitors described herein can include compounds of Formula (I) and pharmaceutically acceptable salts thereof: Formula (I), wherein the substituents are as described.

COMPOSITIONS FOR THE TREATMENT OF FIBROSIS AND FIBROSIS-RELATED CONDITIONS

The present invention relates to novel compounds and their use in the prophylactic and/or therapeutic treatment of fibrosis and fibrosis-related conditions.

Discovery of Benzylidene Derivatives as Potent Syk Inhibitors: Synthesis, SAR Analysis, and Biological Evaluation

Four scaffolds of varied benzylidene derivatives were synthesized and evaluated as Syk inhibitors for the treatment of rheumatoid arthritis (RA). Among these 31 compounds, 3-benzylidene pyrrolidine-2,5-dione derivatives (including 12k) universally showed good Syk inhibitory activities in the low micromolar to submicromolar range. In the cellular profiling, compound 12k, the most efficient compound, showed excellent antiproliferative activity against fibroblast-like synoviocytes (FLS)-RA, and demonstrated potencies for suppression of IL-6 and MMP-3 secretion almost equal to R406 (positive control). The oral efficacy of 12k in the murine collagen-induced arthritis model was significant, despite being weaker than R406. Taken together, all preliminary pharmacological results supported 12k as a potential small-molecule inhibitor targeting Syk for the treatment of RA.

Structural exploration, synthesis and pharmacological evaluation of novel 5-benzylidenethiazolidine-2,4-dione derivatives as iNOS inhibitors against inflammatory diseases

In our previous work, 3I inhibited the LPS-induced iNOS activity and NO production in RAW 264.7 cells and improved joint inflammation and cartilage destruction in inflammatory model. In this study, we synthesized 59 derivatives and bioisosteres on the bas