142650-55-3

Upstream product

• 1379325-80-0 N-aminopropyl phenylacetamide 
• 619-66-9 4-Carboxybenzaldehyde 
• 106-95-6 allyl bromide 
• 107-18-6 allyl alcohol 
• 80735-94-0 1-Phenyl-3-buten-1-ol 

Downstream Products

• 142650-66-6 4-(allyloxycarbonyl)benzoic acid 
• 142650-56-4 allyl 4-hydroxymethylbenzoate 
• 191796-97-1 C₂₅H₂₂N₄O₃ 
• 24968-12-5 bis(4-(4-allylterephthaloyloxy)butyl) terephthalate 
• 63440-94-8 butylene terephthalate cyclic trimer 

Relevant academic research and scientific papers

Macrocyclic Modalities Combining Peptide Epitopes and Natural Product Fragments

"Hot loop" protein segments have variable structure and conformation and contribute crucially to protein-protein interactions. We describe a new hot loop mimicking modality, termed PepNats, in which natural product (NP)-inspired structures are incorporated as conformation-determining and-restricting structural elements into macrocyclic hot loop-derived peptides. Macrocyclic PepNats representing hot loops of inducible nitric oxide synthase (iNOS) and human agouti-related protein (AGRP) were synthesized on solid support employing macrocyclization by imine formation and subsequent stereoselective 1,3-dipolar cycloaddition as key steps. PepNats derived from the iNOS DINNN hot loop and the AGRP RFF hot spot sequence yielded novel and potent ligands of the SPRY domain-containing SOCS box protein 2 (SPSB2) that binds to iNOS, and selective ligands for AGRP-binding melanocortin (MC) receptors. NP-inspired fragment absolute configuration determines the conformation of the peptide part responsible for binding. These results demonstrate that combination of NP-inspired scaffolds with peptidic epitopes enables identification of novel hot loop mimics with conformationally constrained and biologically relevant structure.

COMPOUNDS AND METHOD OF USE

This present disclosure relates to compounds with ferroptosis inducing activity, a method of treating a subject with cancer with the compounds, and combination treatments with a second therapeutic agent.

Synthesis of Albicidin Derivatives: Assessing the Role of N-terminal Acylation on the Antibacterial Activity

The peptide antibiotic albicidin, which is synthesized by the plant pathogenic bacterium, Xanthomonas albilineans, represents the most prominent member of a new class of antibacterial gyrase inhibitors. It shows remarkable antibacterial activities against Gram-positive and Gram-negative microorganisms. Its unique structure potentially represents a new lead structure for the development of an antibacterial drug. Here we report the synthesis of 14 albicidin derivatives with structural variations at the N-terminus, primarily investigating the effects of variation of cinnamoyl, phenylpropanoyl, and benzoyl residues. Gyrase inhibition in vitro and determination of minimal inhibitory concentrations were assessed in parallel. Activities in a nanomolar range and the importance of N-acylation were demonstrated.

Palladium-catalyzed allylic esterification via C-C bond cleavage of a secondary homoallyl alcohol

Palladium-catalyzed allylic esterifications of secondary homoallyl alcohols with acids via sequential retro-allylation and esterification are demonstrated, affording the corresponding allyl ester in up to 99% yield. The electron effect of the substituent of the secondary alcohol was found to be crucial to the selective C-C bond cleavage.

Development of a new nonpeptidic self-immolative spacer. application to the design of protease sensing fluorogenic probes

The design and synthesis of novel self-immolative spacer systems aiming at the release of phenol-containing compounds are described. The newly designed traceless linkers proved to be conveniently stable under physiological conditions and operate through spontaneous decomposition of an hemithioaminal intermediate under neutral aqueous conditions. Their utility was then illustrated by the preparation of original fluorogenic substrates of penicillin amidase whose strong fluorescence is unveiled through enzyme-initiated domino reactions.

Solid phase organic synthesis

A method of synthesis of a material corresponding to the general formula:R3—X—Hcharacterized in that it comprises a material corresponding to the following general formula: being cleaved as indicated enzymatically or non-enzymatically using aci

Bi-aromatic compounds, compositions containing them and uses

The invention relates to novel biaromatic compounds having general formula I and their use in pharmaceutical compositions for use in human and veterinary medicine, in particular for treating dermatological, rheumatic, respiratory, cardiovascular, and ophthalmological disorders, and for use in cosmetic compositions.

Di(aromatic) compounds and their use in human and veterinary medicine and in cosmetics

Di(aromatic) compounds corresponding to the following formula: STR1 in which: Ar represents either STR2 n=1 or 2 or: STR3 X represents a divalent radical, Z represents O, S or a divalent radical, and R1, R2, R3, R4 and R5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R1 is a carboxylic acid function. Use in human and veterinary medicine and in cosmetics.