Inherited genetic modifiers and pharmacologic agents that enhance fetal hemoglobin (HbF) expression reverse the clinical severity of sickle cell disease (SCD). Recent efforts to develop novel strategies of HbF induction include discovery of molecular targets that regulate γ-globin gene transcri...

The synthesis of two new dopamine transporter ligands, 3β-(4-fluoromethylphenyl)tropane-2β-carboxylic acid methyl ester and 3β-(2-fluoromethylphenyl)tropane-2β-carboxylic acid methyl ester, and their spectral characterization are described. The precursors for these ligands were prepared by T...

The carbocyclic nucleoside 3-deazaaristeromycin has shown biological promise but a library of its derivatives upon which to expand this property is lacking. To address this situation, the synthesis of the two diastereomers of 2′-fluoro-3-deazaaristeromycin is described in a multistep convergent...

The synthesis of an advanced intermediate is described that could secure the polyoxygenated core of zaragozic acids and related natural products. The key strategy employs a two-step synthesis of the 3(2H)-furanone ring system by catalytic dihydroxylation-mercury(II)/acid-catalysed cyclisation wi...

An efficient method for asymmetric synthesis of epohelmins A (3), B (4) and their isomer 24 is detailed in this report. The key feature in this divergent synthesis includes the SmI2-induced cross-coupling of N-tert-butanesulfinyl imine 10 with chiral aldehyde 9 derived from d-malic acid. A casca...

The absolute configuration of two novel αvβ6 integrin inhibitors was established via degradation to the corresponding C3-aryl substituted butyrolactone. The configuration of the resulting lactones was established by asymmetric synthesis using 1,4-addition of arylboronic acids to butenolide, ca...

A new synthetic strategy for (R)- and (S)-3-hydroxy-4-(2,4,5-trifluorophenyl)butanoic acid, a building block in the preparation of sitagliptin and its derivatives, was developed. Pd(OAc)2 catalyzed coupling of 2,4,5-trifluoro-1-iodobenzene with allyl alcohol gave 3-(2,4,5-trifluorophenyl)propana...

The structures and absolute stereochemistry of restricticin (1), its N,N-dimethyl derivative (4) and desglycyl hydrolysis product (3), isolated from Penicillium restrictum, have been determined on the basis of spectroscopic evidence. They belong to a new class of broad spectrum antifungal agents...

The antifungal agent (+)-restricticin (1) was prepared in 12 steps from ketone (S)-8. The key steps are (i) the boron-mediated anti aldol reaction of (S)-8 with 9 to give 13 and (ii) the cyclisation reaction 4 → 15.

Synthesis of cyclohexyl analogs of restricticin, a novel type of antifungal agent from ⊂-) R-carvone and their in vitro antifungal activity are described.

The novel antifungal antibiotic restriction was synthesized from l-mannose

Final effluent from wastewater treatment plants may contain bacteria that can pose a range of environmental and health threats. A microbubble-gas plasma reactor capable of producing a number of both reactive oxygen species and reactive nitrogen species has been developed for inactivating bacteri...

AimsThis randomized controlled trial (RCT) study was carried out to assess effects of omega-3 supplementation alone and in combination with vitamin E on gene expressions of SIRT1, SIRT3, SIRT6, FOXO1, FOXO3 and UCP-2 in patients with coronary artery disease (CAD).

Dicarboxylic acids, such as the phthalic acids and their derivatives, are monomeric components in several important polyesters and polyamides. In most cases, these compounds are derived from fossil fuels and are not easily biodegradable. Dipicolinic acid (DPA) is a biologically derived aromatic ...

Highly potent and brain-penetrant phosphodiesterase 10A (PDE10A) inhibitors based on the 2-oxindole scaffold were designed and synthesized. (2-Oxo-1,3-oxazolidin-3-yl)phenyl derivative 1 showed the high P-glycoprotein (P-gp) efflux (efflux ratio (ER) = 6.2) despite the potent PDE10A inhibitory a...

A series of novel conjugates of cobalt bis(1,2-dicarbollide)(-I) with 5-ethynyl-2′-deoxyuridine and its cyclic derivatives were synthesized. Conjugates with 5-ethynyl-2-deoxyuridine were prepared by the direct Sonogashira coupling of a series of cobalt bis(1,2-dicarbollide)(-I) terminal alkynes...

The extension of the deprotection procedure using HNO3 in CH2Cl2 to a number of appropriately selected N-BOC-masked amines and derivatives of natural amino acids was investigated. The method was found to work effectively with almost all tested substrates, with the exception of activated aromatic...

One gene encoding a protein has been shown to have two entirely different functions. Such a phenomenon, which has been called “gene sharing,” was first known in crystallins. We found two multifunctional proteins in the ciliated protozoan Tetrahymena: 14-nm filament protein and protein translat...

SummaryThe Tetrahymena 14-nm filament protein (designated as 49K protein) is a cytoskeletal protein involved in oral morphogenesis and in pronuclear behavior during fertilization. From the previous gene analysis, the 49K protein was shown to share a high sequence identity with porcine heart citr...

Tetrahymena 14-nm filament-forming protein has dual functions as a citrate synthase in mitochondria and as a cytoskeletal protein involved in oral morphogenesis and in pronuclear behavior during conjugation. By immunoblotting using monoclonal and polyclonal antibodies following two-dimensional g...