Evaluation of lipophilicity and drug-likeness of donepezil-like compounds using reversed-phase thin-layer chromatography.

Fourteen donepezil-like acetylcholinesterase (AChE) inhibitors from our library were analyzed using reversed-phase thin-layer chromatography to assess their lipophilicity and blood-brain barrier permeability. Compounds possessed N-benzylpiperidine and N,N-diarylpiperazine moieties connected via a short carboxamide or amine linker. Retention parameters R , b, and C were considered as the measures of lipophilicity.

Multi-target potential of newly designed tacrine-derived cholinesterase inhibitors: Synthesis, computational and pharmacological study.

Simple and scalable synthetic approach was used for the preparation of thirteen novel tacrine derivatives consisting of tacrine and N-aryl-piperidine-4-carboxamide moiety connected by a five-methylene group linker. An anti-Alzheimer disease (AD) potential of newly designed tacrine derivatives was evaluated against two important AD targets, acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). In vitro pharmacological evaluation showed strong ChE inhibitory activity of all compounds, with IC values ranging from 117.

Determination of lipophilicity and ionization of fentanyl and its 3‑substituted analogs by reversed-phase thin-layer chromatography.

Lipophilicity and ionization constant of sixteen fentanyl analogues were investigated by reversed-phase thin-layer chromatography (RP-TLC). Fourteen compounds have nitrogen containing groups at C-3 position of the piperidine ring and two compounds are 3-carbomethoxy derivatives of fentanyl. Among them, five are diastereomeric cis/trans couples and six novel trans diastereomers.

In vitro and in vivo evaluation of fluorinated indanone derivatives as potential positron emission tomography agents for the imaging of monoamine oxidase B in the brain.

Monoamine oxidases (MAOs) play a key role in the metabolism of major monoamine neurotransmitters. In particular, the upregulation of MAO-B in Parkinson's disease, Alzheimer's disease and cancer augmented the development of selective MAO-B inhibitors for diagnostic and therapeutic purposes, such as the anti-parkinsonian MAO-B irreversible binder l-deprenyl (Selegiline®). Herein we report on the synthesis of novel fluorinated indanone derivatives for PET imaging of MAO-B in the brain.

UV-induction of photolytic and photocatalytic degradation of fumonisins in water: reaction kinetics and toxicity.

Although fumonisins are toxic and carcinogenic mold products that contaminate feed, food, and water, their photodegradation has not yet been reported. In this work, the efficiency of photolysis (UV, UV/HO, and UV/[Formula: see text]) and photocatalysis (TiO (Degussa P25/Wackherr) and ZnO) for the degradation of fumonisins in an aqueous medium were investigated. In the case of fumonisin B (FB) optimal conditions in terms of pH, the initial concentrations of HO/[Formula: see text] for UV, UV/HO, and UV/[Formula: see text] treatments were investigated.

Exploring neural mechanisms of the health benefits of gratitude in women: A randomized controlled trial.

Background: Gratitude has received growing interest as an emotion that can bring greater happiness and health. However, little is known about the effects of gratitude on objective measures of physical health or the neural mechanisms that underlie these effects. Given strong links between gratitude and giving behavior, and giving and health, it is possible that gratitude may benefit health through the same mechanisms as giving to others.

Synthesis and pharmacological evaluation of novel cis and trans 3-substituted anilidopiperidines.

Background: 4-Anilidopiperidine class of synthetic opioid analgesics, with it's representative fentanyl, are by far the most potent and clinically significant for the treatment of the severe chronic and surgical pain. However, side effects of μ-opioids are often quite serious. In order to improve the pharmacological profile of this class of opioid analgesics, a novel fentanyl analogs were designed, synthesized and evaluated in vivo for their antinociceptive activity.

Sex Differences in the Effect of Inflammation on Subjective Social Status: A Randomized Controlled Trial of Endotoxin in Healthy Young Adults.

It has been established that inflammation leads to a variety of changes in social experience, but one area of social experience that has been overlooked is subjective social status. Furthermore, given sex differences in the relationship between inflammation and social status, males may be more sensitive to inflammation-induced changes in social status. However, no previous studies in humans have examined this possibility.

Exploring the role of gratitude and support-giving on inflammatory outcomes.

Although there has been much interest in understanding the effect of gratitude on health-related outcomes, this remains an understudied area of research, particularly regarding mechanisms and measurement of biological outcomes. The present study explored whether a gratitude intervention could reduce inflammatory outcomes and whether this occurred through increased support-giving. Healthy women ( = 76) were randomly assigned to a 6-week gratitude intervention (i.

Antidiabetics: Structural Diversity of Molecules with a Common Aim.

Background: Diabetes mellitus type 2 (DMT2) is an endocrine disease of global proportions which is currently affecting 1 in 12 adults in the world, with still increasing prevalence. World Health Organization (WHO) declared this worldwide health problem, as an epidemic disease, to be the only non-infectious disease with such categorization. People with DMT2 are at increased risk of various complications and have shorter life expectancy.

α-Glucosidase inhibitory activity and cytotoxic effects of some cyclic urea and carbamate derivatives.

The inhibitory activities of selected cyclic urea and carbamate derivatives (1-13) toward α-glucosidase (α-Gls) in in vitro assay were examined in this study. All examined compounds showed higher inhibitory activity (IC) against α-Gls compared to standard antidiabetic drug acarbose. The most potent was benzyl (3,4,5-trimethoxyphenyl)carbamate (12) with IC = 49.

Correction: A Pilot Study Examining Physical and Social Warmth: Higher (Non-Febrile) Oral Temperature Is Associated with Greater Feelings of Social Connection.

[This corrects the article DOI: 10.1371/journal.pone.

A Pilot Study Examining Physical and Social Warmth: Higher (Non-Febrile) Oral Temperature Is Associated with Greater Feelings of Social Connection.

An emerging literature suggests that experiences of physical warmth contribute to social warmth-the experience of feeling connected to others. Thus, thermoregulatory systems, which help maintain our relatively warm internal body temperatures, may also support feelings of social connection. However, the association between internal body temperature and feelings of connection has not been examined.

Exposure to an inflammatory challenge enhances neural sensitivity to negative and positive social feedback.

Inflammation, part of the body's innate immune response, can lead to "sickness behaviors," as well as alterations in social and affective experiences. Elevated levels of pro-inflammatory cytokines have been associated with increased neural sensitivity to social rejection and social threat, but also decreased neural sensitivity to rewards. However, recent evidence suggests that inflammation may actually enhance sensitivity to certain social rewards, such as those that signal support and care.

The Neurobiology of Giving Versus Receiving Support: The Role of Stress-Related and Social Reward-Related Neural Activity.

Objectives: There is a strong association between supportive ties and health. However, most research has focused on the health benefits that come from the support one receives while largely ignoring the support giver and how giving may contribute to good health. Moreover, few studies have examined the neural mechanisms associated with support giving or how giving support compares to receiving support.

Trait sensitivity to social disconnection enhances pro-inflammatory responses to a randomized controlled trial of endotoxin.

Unlabelled: One proposed mechanism for the association between social isolation and poor health outcomes is inflammation. Lonely or socially disconnected individuals show greater inflammatory responses, including up-regulation of pro-inflammatory gene expression, and people who are sensitive to cues of social disconnection (e.g.

Yearning for connection? Loneliness is associated with increased ventral striatum activity to close others.

Loneliness is a distressing state indicating that one's basic need for social connection is not being met. In an effort to satisfy the need for social connection, loneliness may increase the processing of social cues and desire to connect with others. Yet the neural substrates that contribute to the drive for increased connection in response to loneliness are not known.

Inflammation impairs social cognitive processing: A randomized controlled trial of endotoxin.

Unlabelled: Neuropsychiatric disorders (e.g., autism, schizophrenia) are partially characterized by social cognitive deficits, including impairments in the ability to perceive others' emotional states, which is an aspect of social cognition known as theory of mind (ToM).

Sex differences in depressive and socioemotional responses to an inflammatory challenge: implications for sex differences in depression.

Substantial evidence demonstrates that inflammatory processes may underlie depression for a subset of patients, including work showing that healthy subjects exposed to an inflammatory challenge show increases in depressed mood and feelings of social disconnection. However, despite the fact that depression is two times as likely to occur in females than males, the vast majority of this work has been carried out in males. Thus, the objective of this study was to determine whether females (vs males) would show greater increases in proinflammatory cytokines, depressed mood, and social disconnection in response to an inflammatory challenge.

The role of the ventral striatum in inflammatory-induced approach toward support figures.

Although considerable research has shown that inflammation leads to social withdrawal more generally, it is also possible that inflammation leads to social approach when it comes to close others. Whereas it may be adaptive to withdraw from strangers when sick, it may be beneficial to seek out close others for assistance, protection, or care when sick. However, this possibility has never been explored in humans nor have the neural substrates of these behavioral changes.

[Truncus coeliacus compression syndrome is a rare cause of mesenteric ischaemia].

Truncus coeliacus compression syndrome (TCK) is a rare condition which causes mesenteric ischaemia. The pathogenesis is compression of truncus coeliacus, where it branches off the aorta, commonly because of an anatomical variant of the median arcuate ligament. The syndrome is characterized by the clinical triad: postprandial abdominal pain, weight loss and vomiting.