Crystal and molecular structures of 2 conformational polymorphs (forms I and II) of olopatadine hydrochloride, an antiallergic agent, are presented. Both crystal modifications crystallize in the monoclinic crystal system with 1 olopatadine hydrochloride molecule in the Z configuration in the asy...

The structure and stereochemistry of a new piperazinedione, isolated from the cells of Streptomyces albus, are assigned on the basis of spectroscopic data, including comparison with related 2,5-piperazinediones.

An efficient stereodivergent total synthesis of anti-Alzheimer agent (R)-(−) and (S)-(+)-arundic acid has been achieved from both chiral and nonchiral materials. This strategy features an efficient approach to separable diastereomeric C-2 chiral 4-pentenol intermediates employing proline catalys...

An experimentally simple, mild and straightforward synthetic route towards diversely functionalized (E)-3-acylacrylic acids is described, with Horner–Wadsworth–Emmons (HWE) reaction as the key step. The substrate scope and limitations of the HWE reaction were investigated with a range of β-ke...

Publisher SummaryThis chapter discusses the roles of vasopressin (VP) and oxytocin (OT) in rodent olfactory-based social recognition memory (SRM). The conventional paradigm used to test SRM in rats and mice is the social recognition test (SRT). A significant reduction in the duration of social i...

The synthetic 1-β,β-disubstituted analogues of [1-deamino]-oxytocin, [1′-(1′-thio-4′-methylcyclohexane)-acetic acid1]-oxytocin (MeCAOT) a peripheral oxytocin antagonist, and [1′-(1′-methyl-4′-thiopiperidine)-acetic acid1]-oxytocin (MePAOT), devoid of peripheral antioxytocin activity, wer...

Application of halophiles can decrease the cost of polyhydroxyalkanoate (PHA) production or bioplastic which are an alternative to the petroleum-derived plastic. Extremely halophilic archaeon, Natrinema ajinwuensis RM-G10 accumulated 61.02 ± 0.68% PHA of its cell dry mass at 72 h in repeated ba...

Rapidly mutating Y-STRs (RM Y-STRs) have been paid much attention in recent years. The 13 RM Y-STRs have been proved to have substantially higher haplotype diversity and discrimination capacity than conventionally used Y-STRs, indicating the considerable power in paternal lineage differentiation...

A comparison of the synthesis of wax esters by transesterification of jatropha oil and oleyl alcohol using the immobilized lipase EQ3 (Burkholderia sp. EQ3) and Lipozyme RM IM (Rhizomucor miehei) was carried out. The predominant fatty acids in jatropha oil were palmitic acid (14%), stearic acid ...

The highly polymorphic human leukocyte antigen (HLA) genes, located in the human major histocompatibility complex, encode the class I and II antigen-presenting molecules, which are centrally involved in the immune response. HLA typing is used for several clinical applications, such as transplant...

ResumenObjetivoEl objetivo de esta revisión fue evaluar la capacidad diagnóstica de la PET/RM simultánea en oncología, comparándola con la de la PET/TC, basándonos en la evidencia disponible.

Recently introduced rapidly mutating Y-chromosomal short tandem repeat (RM Y-STR) loci, displaying a multiple-fold higher mutation rate relative to any other Y-STRs, including those conventionally used in forensic casework, have been demonstrated to improve the resolution of male lineage differe...

RM-133 is a key representative of a new family of aminosteroids reported as potent anticancer agents. Although RM-133 produced interesting results in 4 mouse xenograft cancer models when injected subcutaneously, it needs to be improved to increase its in vivo potency. Thus, to obtain an analog o...

Y-chromosomal short tandem repeat (Y-STR) markers are commonly used in forensic genetics. Male-specific haplotypes provided by commercial Y-STR kits allow discriminating between many – but not all – unrelated men, while they mostly fail to separate related ones. Aiming to improve male relative...

The aminosteroid derivative RM-133 is an effective anticancer molecule for which proof of concept has been achieved in several mouse xenograph models (HL-60, MCF-7, PANC-1 and OVCAR-3). To promote this new family of molecules toward a clinical phase 1 trial, the mechanism of action governing the...

The RM-wrap (RM = Refractory Metal) is a pressure-less, versatile and tailorable joining process: it consists of wrapping Si foils inside a refractory metal wrap (i.e., Mo, Nb, Ta) in order to prevent molten silicon from leaking outside the joined region and infiltrating the facing materials dur...

An inherently regiospecific synthesis of isatins (1H-indole-2,3-diones) starting from 1-halo-2-nitrobenzenes is described. The isatins are formed by an intramolecular palladium-catalyzed annulation of 2-(2-haloethynyl)-1-nitrobenzenes via the formation of 2-haloisatogens.

A series of enantioenriched long chain 2-fluoroalk-1-en-3-ols 1 has been prepared by lipase-catalyzed resolution of the racemic compounds synthesized from terminal alkenes. The lipase of Candida antarctica was shown to be the most efficient one in terms of enantioselectivity. Transesterification...

Evidence for an enamine mechanism of inactivation of pig brain γ-aminobutyric acid (GABA) aminotransferase by (S,E)-4-amino-5-fluoropent-2-enoic acid is presented. apo-GABA aminotransferase reconstituted with [3H]pyridoxal 5′-phosphate is inactivated by (S,E)-4-amino-5-fluoropent-2-enoic acid ...

Compounds 1–4 were previously reported as potent antimitotic and antitumor agents with Pgp modulatory effects. Compounds 5–18 have been synthesized in an attempt to optimize the various activities of 1–4. Compounds 5–10 explored the influence of methoxy substitutions on the 7-benzyl moiety i...