P2X receptors are a family of extracellular ATP-gated trimeric cation channels that is widely distributed in human tissues. Quite some drug candidates targeting P2X receptors have entered into preclinical or main phases of clinical trials, but many of them failed due to low subtype-selectivity o...

Taking the pyrrolopyrimidine derived IGF-1R inhibitor NVP-AEW541 as the starting point, the benzyl ether back-pocket binding moiety was replaced with a series of 2-cyclic ether methyl ethers leading to the identification of novel achiral [2.2.1]-bicyclic ether methyl ether containing analogues w...

A series of d- and l-tyrosine-chlorambucil analogs was synthesized as anticancer drugs for chemotherapy of breast cancer. The novel compounds were synthesized in good yields through efficient modifications of d- and l-tyrosine. The newly synthesized compounds were evaluated for their anticancer ...

Rosmarinic acid methyl ester (Ov-8) was isolated form Origanum vulgare. The antioxidant activities of Ov-8 were evaluated by measuring radical-scavenging activities, reducing power, and inhibition of lipid peroxidation, using liposomes and mice tissue. The percentage inhibition, by Ov-8, of the ...

Novel quaternary ammonium compounds (QUATS) derived from l-Tyrosine and L-3,4-dihydroxyphenylalanine (l-DOPA) with chain lengths varying from C10 to C16 were synthesised and their physicochemical properties were determined. The CMCs of the QUATS were higher than their corresponding ester hydroch...

3-Ketosteroid Δ1-dehydrogenases are FAD-dependent enzymes that catalyze the introduction of a double bond between the C1 and C2 atoms of the A-ring of 3-ketosteroid substrates. These enzymes are found in a large variety of microorganisms, especially in bacteria belonging to the phylum Actinobac...

Acyclic nitrones react with dimethyl acetylenedicarboxylate (DMAD) to give stable isoxazolines, from which the ones that contain electron-donating aromatic rings at the C3 position (R1) were shown to undergo unprecedented fragmentation at room temperature, giving the R1-aldehyde and inseparable ...

Oxidation of 1,1′-methylenebis[4-tert-butyl-2-(diphenylphosphino) benzene] by H2O2 or S8 in toluene affords two new PCP-type pincer ligands. The methylene group deprotonation in the new ligands as well as in their precursor by n-BuLi or LiCH2SiMe3 failed, while the methylene group in the precur...

Reaction of (μ-SCH2CH2CH2S-μ)Fe2(CO)6 (1) with 2-(diphenylphosphino)benzaldehyde in the presence of Me3NO·2H2O yielded monosubstituted complex (μ-SCH2CH2CH2S-μ)Fe2(CO)5[Ph2P(2-C6H4CHO)] (3) and disubstituted complex (μ-SCH2CH2CH2S-μ)Fe2(CO)4[Ph2P(2-C6H4CHO)]2 (4) in 47% and 23% yields, re...

The coordinated 1-alkyl-2-(arylazo)imidazole (RaaiR/) in [Ag(μ-dppm)(RaaiR/)]2(PF6)2 (dppm, bis-(diphenylphosphino)methane) undergoes light induced trans-to-cis isomerization about NN bond. The quantum yields (ϕt→c) of trans-to-cis isomerization of coordinated RaaiR/ in the complex is lower th...

We have investigated the addition of a simple phosphinoboronate ester, Ph2PBpin (pin = 1,2-O2C2Me4), to 2-diphenylphosphinobenzaldehyde (2-Ph2PC6H4C(O)H) and related aldimine derivatives (2-Ph2PC6H4C(NR)H) as a simple and effective strategy for generating unique diphosphine ligands bearing a pen...

[M(sac)2(dppp)] (1 and 2), [M(dppp)2](sac)2 (3 and 4) and [M(sac)2(dppb)] (5 and 6) complexes, where M = PdII (1, 3 and 5) and PtII (2, 4 and 6), sac = saccharinate, dppp = 1,3-bis(diphenylphosphino)propane and dppb = 1,4-bis(diphenylphosphino)butane, were synthesized and characterized by IR, NM...

Two new uranium metallacyclopropenes, (C5Me4R)2U(η2-Ph2PCCPPh2) (R = Me, Et) were prepared by reducing the corresponding (C5Me4R)2UCl2 complexes with KC8 in the presence of 1,2-bis(diphenylphosphino)acetylene (Ph2PCCPPh2). Both compounds were fully characterized by a combination of elemental an...

1-Alkyl-2-(arylazo)imidazole (RaaiR/), a bidentate N(azo), N(imidazolyl) chelator, and bis(diphenylphosphino)methane (dppm), a P, P bridger, have been used to prepare phosphino bridged dinuclear-Cu(I) complexes, [Cu(μ-dppm)(RaaiR/)]2(ClO4)2. The structures of the complexes have been established...

Inhibition of phosphodiesterase 9 (PDE9) has been reported to enhance rodent cognitive function and may represent a potential novel approach to improving cognitive dysfunction in Alzheimer’s disease. PF-04447943, (6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyr...

A series of new 3-methyl-3-phenyl-2,5-dioxo-pyrrolidin-1-yl-acetamides (6–23) has been synthesized and evaluated for their anticonvulsant activity in the maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ) seizure tests after intraperitoneal injection in mice. The acute neuro...

A series of 3(R)-aminopyrrolidine derivatives were designed and synthesized for JAK1-selective inhibitors through the modification of tofacitinib’s core structure, (3R,4R)-3-amino-4-methylpiperidine. From the new core structures, we selected (R)-N-methyl-N-(pyrrolidin-3-yl)-7H-pyrrolo[2,3-d]pyr...

BackgroundDehydrocorydaline (DHC) and canadine (THB) are two active alkaloid compounds in Corydalis yanhusuo (Y.H. Chou & Chun C. Hsu) W.T. Wang ex Z.Y. Su & C.Y. Wu (Papaveraceae) (Rhizoma Corydalis). DHC and THC were previously shown to exert anti-platelet aggregation effect dose-dependently, ...

The substrate specificity of a purified lysyl-ribonucleic acid synthetase of Escherichia coli 9723 has been studied by determining the effects of a group of lysine analogs upon (a) the enzymic transfer of lysine-14C to soluble ribonucleic acid and (b) lysine-dependent ATP-pyrophosphate exchange....

The selective acylation of the 6-amino group of 2,6-diamino-4-hexynoic acid was obtained in high overall yield by a simple approach instead of copper complex method.