Propofol exerts neurotoxic effects on the developing mammalian brains, but the underlying molecular mechanism remains unclear. MicroRNAs (miRNAs) are a class of small noncoding RNAs that modulate gene expression at the post-transcriptional level. However, in specific types of neurocytes, the det...

BackgroundDexmedetomidine (Dex) can confer cardioprotective effects against ischemia/reperfusion (I/R) injury. While there are no studies addressing cardioprotection of Dex via regulation of microRNAs. The purpose of this study was to examine the roles and mechanisms of microRNA in cardioprotect...

3,3-Diethoxy-N-sulfonyl and carbamoyl azetidin-2-ones undergo efficient ring-opening reaction with various amine nucleophiles. Subsequent acid hydrolysis of the ketal moiety generated α-keto amides in excellent overall yields. The naturally occurring serine protease inhibitor poststatin was syn...

A convergent synthesis of the pentapeptide poststatin has been developed. The key step involves oxidative cleavage of an acyl cyanophosphorane. The resulting α,β-diketo nitrile is then coupled to the free amine of a C-terminal-dipeptidyl component to generate the protected natural product. Dep...

Incubation of bradykinin with rat urine resulted in the successive degradation of bradykinin to bradykinin-(1–8), bradykinin-(1–7) and bradykinin-(1–6). In contrast, in rat plasma, bradykinin was degraded via either bradykinin-(1–8) or bradykinin-(1–7) to bradykinin-(1–5). Phosphoramidon (...

Full details are given for the syntheses of the protease inhibitors, poststatin and eurystatin by the acyl cyanophosphorane coupling procedure used for the formation of α-keto amides. We have also extended this methodology to the syntheses of the related α-hydroxy amide natural products, phebe...

The effects of nifedipine, papaverine and four benzylisoquinoline alkaloids (cularine, cularidine, celtisine and isocrasifoline) were studied in isolated rat uterus in order to clarify the mechanism of their relaxant action. All the compounds tested completely relaxed KCl-induced contractions an...

Reactions of two isomers—2-chloro-1-(oxiran-2-ylmethyl)-1H-indole-3-carbaldehyde or 2-(chloromethyl)-2,3-dihydro[1,3]oxazolo[3,2-a]indole-9-carbaldehyde with aromatic amines lead to the same products in both cases—hydrochlorides of pyrimido[1,2-a]indole derivatives containing two fragments of ...

The multistep preparation of the new 10-substituted 2-(1-piperazinyl)pyrimido[1,2-a]benzimidazol-4(10H)-ones 6a–o, and of the two isomers 10-ethyl-2-(diethylamino)pyrimido[1,2-a]benzimidazol-4(10H)-one 6p and 10-ethyl-4-(diethylamino)pyrimido[1,2-a]benzimidazol-2(10H)-one 13, as well as the in ...

Domino reactions of amidines with 2-alkylidenetetrahydrofurans, prepared by cyclization of 1,3-dicarbonyl dianions or 1,3-bis-silyl enol ethers with various dielectrophiles, provided an efficient access to 4-(3-hydroxyalkyl)pyrimidines.

Two series of thieno[2,3-d]pyrimidine derivatives bearing a dithiocarbamate side chain at the C2 position were synthesized and evaluated for cytotoxic activity in human lung cancer A549 and colon cancer HCT-116 cell lines. Compound 3n exhibited the most cytotoxic effect on A549 cells with an IC5...

Based on the deoxygenation reaction of 1-(1-tert-butyl-3-nitroazetidine-3-yl)-1H-1,2,3-triazoles a new method for the synthesis of substituted 1-(1H-imidazole-4-yl)-1H-1,2,3-triazoles has been developed. Fungicidal activity of these compounds has been investigated at a range of phytopathogenic f...

A highly efficient and practical protocol has been developed for the synthesis of 5-(hetero)arylated thiazole derivatives via an N-heterocyclic carbene palladium (Pd-NHC) complex catalyzed direct C-H arylation reaction. Utilization of this methodology, the arylation of substituted thiazoles with...

The one-pot three-component reaction of 2-formylbenzoic acid with (S)- and (R)-methylbenzylamine and dimethyl phosphite (Kabachnik–Fields reaction) proceeded in short reaction times under solvent and catalyst free-conditions to afford the corresponding (3R,1′S)- and (3S,1′R)-isoindolin-1-one-...

A series of novel N-substituted N′-(2-arylmethylthio-4-chloro-5-methylbenzenesulfonyl)guanidines 9–41 have been synthesized and investigated as inhibitors of four isoforms of zinc enzyme carbonic anhydrase (CA.EC 4.2.1.1), that is the cytosolic CA I and II, and cancer-associated isozymes CA IX...

The reaction of 4-(4-chlorophenyl)-2-mercapto-6-oxo-1,6-dihydropyrimidine-5-carbonitrile 1 with benzylidenemalononitrile and/or methyl iodide has yielded dihydropyrimido[1,2-a]pyrimidine derivative 5 and methylthio derivative 6 respectively. Thiated product 7 was cyclized with chloroacetonitrile...

The iEBE-VISHNU code package performs event-by-event simulations for relativistic heavy-ion collisions using a hybrid approach based on (2+1)-dimensional viscous hydrodynamics coupled to a hadronic cascade model. We present the detailed model implementation, accompanied by some numerical code te...

The formation of the Mojave crustal province has been a persistent enigma in models of the Proterozoic tectonic history of southwestern Laurentia. It is composed of similarly-aged 1.8–1.7 Ga rocks as the adjacent Yavapai province, yet shows evidence of much older (>2.2 Ga) lithospheric componen...

Published models for the plate tectonic evolution of the Western Indian Ocean suggest that the Southern Mascarene Basin opened by oceanic crustal accretion between the continental margins of southwestern India and southeastern Madagascar. However, with the cessation of the Mascarene Basin spread...

New experimental data on the density, viscosity and dielectric constant of HCFC-225ca (CHCl2-CF2-CF3 and HCFC-225cb (CHClF-CF2-CClF2) in the liquid phase are presented at temperatures from 293 to 323 K and pressures from 0.1 to 80 MPa. The measurements were carried out by a vibrating-tube densit...