16536-95-1

Usage

InChI:InChI=1/C5H11NS/c1-4(2)3-5(6)7/h4H,3H2,1-2H3,(H2,6,7)

Upstream product

• 625-28-5 Isovaleronitrile 
• 66365-41-1 triphenylphosphine-thiocyanogen 
• 5674-02-2 2-methylpropylmagnesium chloride 
• 70017-64-0 N_.N-Diethyl-isovaleramidin 
• 541-46-8 isobutylamide 
• 108-12-3 isopentanoyl chloride 

Downstream Products

• 882305-14-8 ethyl 2-isobutyl-1,3-thiazole-4-carboxylate 

Relevant academic research and scientific papers

MODIFIED PEPTIDES AND THEIR USE

The invention relates to a compound of formula (A) wherein n is an integer from 1 to 6, and R1, R1', R2, R2', R3, R3' are cationic or hydrophobic residues.

Tailoring the Physicochemical Properties of Antimicrobial Peptides onto a Thiazole-Based γ-Peptide Foldamer

Antimicrobial peptides (AMPs) are amphipathic molecules displaying broad-spectrum bactericidal activity, providing opportunities to develop a new generation of antibiotics. However, their use is limited either by poor metabolic stability or by high hemolytic activity. We herein addressed the potential of thiazole-based γ-peptide oligomers named ATCs as tunable scaffolds to design polycationic AMP mimetics. Knowing the side chain distribution along the backbone, we rationally designed facially amphiphilic sequences with bactericidal effect in the micromolar range. Since no hemolytic activity was detected up to 100 μM, this class of compounds has shown the potential for therapeutic development.

Common origins of RNA, protein and lipid precursors in a cyanosulfidic protometabolism

A minimal cell can be thought of as comprising informational, compartment-forming and metabolic subsystems. To imagine the abiotic assembly of such an overall system, however, places great demands on hypothetical prebiotic chemistry. The perceived differences and incompatibilities between these subsystems have led to the widely held assumption that one or other subsystem must have preceded the others. Here we experimentally investigate the validity of this assumption by examining the assembly of various biomolecular building blocks from prebiotically plausible intermediates and one-carbon feedstock molecules. We show that precursors of ribonucleotides, amino acids and lipids can all be derived by the reductive homologation of hydrogen cyanide and some of its derivatives, and thus that all the cellular subsystems could have arisen simultaneously through common chemistry. The key reaction steps are driven by ultraviolet light, use hydrogen sulfide as the reductant and can be accelerated by Cu(I)-Cu(II) photoredox cycling.

COMPOUNDS FOR USE IN THE TREATMENT OF MYCOBACTERIAL INFECTIONS

The present invention concerns compounds of general formula (I): in which Y and Z are chosen from CH and N; T is chosen from CO or SO2; n is 1 to 3; R1 represents a group chosen, for example, from C1-C3 alkyl chains unsubstituted or substituted by fluorine, the unsubstituted or substituted cyclic, cyano, azido, alkoxy and phenyl groups; and R is chosen from the azido, cyano, alkinyl and 2-benzothiazolyl groups and an optionally substituted aromatic heterocycle with five vertices; and the use thereof in the treatment of bacterial and mycobacterial infections such as, for example, tuberculosis, leprosy and atypical mycobacterial infections. The present invention also concerns pharmaceutical compositions comprising, as the active ingredient, at least one of the abovementioned compounds and optionally an antibiotic activatable via the EthA pathway

Microwave-assisted synthesis of potent PDE7 inhibitors containing a thienopyrimidin-4-amine scaffold

A series of novel thienopyrimidin-4-amines have been synthesized and evaluated as phosphodiesterase (PDE) inhibitors. A rationale for the observed selectivity against PDE7 has been obtained from molecular modelling studies on the most active compounds. This journal is the Partner Organisations 2014.

Analogs of isovaleramide, a pharmaceutical composition including the same, and a method of treating central nervous system conditions or diseases

An isovaleramide analog having at least one of an increased potency, an increased half-life, and an increased stability compared to isovaleramide. The isovaleramide analog is a cyclic analog or a noncyclic analog. The isovaleramide analog is formulated into a pharmaceutical composition. A method of treating a central nervous system condition or disease is also disclosed. The method comprises administering an isovaleramide analog to a patient suffering from the central nervous system condition or disease.

Synthesis of (4R,5S)-melithiazols F and I

Palladium-catalyzed cyclization-methoxycarbonylation of (2R,3S)-3-methylpenta-4-yne-1,2-diol (8) derived from the (2R,3S)-epoxybutanoate 7 followed by methylation gave the tetrahydro-2-furylidene acetate (-)-9, which was converted into the left-half aldehyde (+)-4. A Wittig reaction between (+)-4 and the phosphoranylide derived from the bithiazole-type phosphonium iodide 5 using lithium bis(trimethylsilyl)-amide afforded (+)-(4R,5S)- melithiazol F (1), whose spectroscopic data were identical with those of the natural product 1. Moreover, the synthesis of (+)-(4R,5S)-melithiazol I (2), was achieved by the same synthetic strategy as that of (+)-(4R,5S)-melithiazol F (1). The antifungal activity of the synthetic melithiazols F (1) and I (2) against the phytopathogenic fungus, Phytophthora capsici, was evaluated by using a paper disc assay method. Wiley-VCH Verlag GmbH & Co. KGaA, 2006.

Methods of treatment of amyloidosis using bi-aryl aspartyl protease inhibitors

The invention relates to novel compounds and methods of treating diseases, disorders, and conditions associated with amyloidosis. Amyloidosis refers to a collection of diseases, disorders, and conditions associated with abnormal deposition of A-beta protein.