Synthesis and enantiomeric recognition studies of a novel 5,5-dioxophenothiazine-1,9 bis(thiourea) containing glucopyranosyl groups

A novel optically active 5,5-dioxophenothiazine-1,9 bis(thiourea) containing glucopyranosyl groups was synthesized and its enantiomeric recognition properties were examined towards the enantiomers of tetrabutylammonium salts of chiral α-hydroxy and N-protected α-amino acids using UV–vis spectroscopy

Investigation of the preparation of cycloalkanoindole derivative in ionic solvent

Optimization of the synthesis of carba analogs of physostigmine is described. Aza-Claisen-rearrangement, followed by aza-Alder-ene reaction of aniline derivatives gave the title product besides some byproduct. The effects of the amounts of catalyst, solvent, temperature and the method of heating were investigated

Role of physical activity and cardiorespiratory fitness in metabolically healthy obesity: a narrative review

Obesity has been associated with a multitude of metabolic disorders, often clustering with risk factors of cardiovascular disease and type 2 diabetes mellitus, hypertension, dyslipidaemia. Overall, obesity is a worldwide, growing health concern. However, a subgroup of obese individuals with a low burden of metabolic abnormalities have been identified and described as metabolically healthy obese (MHO). Whether the MHO phenotype is protective against obesity-related metabolic disorders in the long-term is presently unclear, and current research examining the potential transition has yielded inconsistent results. In this current narrative review, we aim to provide insights on the role of physical activity (PA) and cardiorespiratory fitness (CRF) in MHO. Lifestyle factors such as PA and CRF may influence the MHO phenotype. Limited studies have characterised energy expenditure and CRF in MHO and metabolically unhealthy obese. However, higher levels of PA, less sedentary behaviour and higher CRF have been observed in MHO individuals. Considering the multiple benefits of PA, it is high time to advocate this lifestyle change beyond its influence on energy balance in a weight loss programme to improve cardiovascular and metabolic risk factors irrespective of body weight and fat mass changes. Improved CRF via increased PA, especially exercise participation, while avoiding weight gain is not only a realistic goal, but should be the primary intervention for MHO populations to prevent the transition to an abnormal metabolic state

Some Questions of the Competitiveness of Hungarian Sheep-breeding

The authors did economic calculations examining the possibilities for the raise of rentability in Hungarian sheep-breeding sector. It was been counting with a flock of 300 ewes. While analysing four models were set up. The first represents the economic parameters of the present average and in a certain way traditional sheep-farming. This model, which symbolises the present situation, is able to provide maximum 47,827 HUF income for a sheperd, parallel with a loss of 843,495 HUF. The second model shows the possible production of the Hungarian merino flocks determined by its genetically limited productivity and technology. It ensures the opportunity to spend 550,000 HUF to expansion above average rental. This amount might be increased with a yearly subsidy of 450,000 HUF plus the 831,610 HUF extra EU payments. The third model is based on the results of an upgrade with prolific breeds in order to better meat performance. The possible result in this case was 1,324,412 HUF, which sum would be supplemented with the subsidies and direct EU payments. The professional management of milking stocks may raise the net income with extra 600,000 HUF. (Model number four)

Membrane-Supported Recovery of Homogeneous Organocatalysts: A Review

As catalysis plays a significant role in the development of economical and sustainable chemical processes, increased attention is paid to the recovery and reuse of high-value catalysts. Although homogeneous catalysts are usually more active and selective than the heterogeneous ones, both catalyst recycling and product separation pose a challenge for developing industrially feasible methods. In this respect, membrane-supported recovery of organocatalysts represents a particularly useful tool and a valid option for organocatalytic asymmetric synthesis. However, catalyst leaching/degradation and a subsequent decrease in selectivity/conversion are significant drawbacks. As the effectivity of the membrane separation depends mainly on the size of the catalyst in contrast to the other solutes, molecular weight enlargement of small organocatalysts is usually necessary. In the last few years, several synthetic methodologies have been developed to facilitate their recovery by nanofiltration. With the aim of extending the possibilities for the membrane-supported recovery of organocatalysts further, this contribution presents a review of the existing synthetic approaches for the molecular weight enlargement of organocatalysts

Diszubsztituált aminosavak enantioszelektív szintézise fázistranszfer katalizátorok segítségével: Enantioselective synthesis of disubstituted amino acids in the presence of phase transfer catalysts

The class of enantiopure α,α-disubstituted α-amino acids has gained considerable attention in the past decades since some of them have interesting properties as antibiotics. The synthesis of such materials has been a challenging task to which enantioselective phase transfer catalysis offers an effective solution. In our work the synthesis starts from the easily available Meldrum’s acid, that is converted into the key disubstituted malonate intermediates in an asymmetric alkylation step catalyzed by cinchona-crown ether derivatives. The aim was to obtain a new type of phase transfer catalyst – cinchona derivatives of aza-crown ethers – and compare the achieved enantiomeric excess values, while also optimizing the reaction conditions. The amino acids are gained by the selective hydrolysis of the key intermediates followed by a multistep reaction.   Kivonat Az enantiomertiszta α,α-diszubsztituált α-aminosavak iránt számottevő az érdeklődés az utóbbi évtizedekben, mivel egyes képviselőik antibakteriális tulajdonságokkal bírnak. Szintézisük egy kihívást jelentő feladat, amire az enantioszelektív fázistranszfer katalízis hatékony megoldást kínál. Munkánk során az előállítás a könnyen elérhető Meldrum-savból indul, amelyből a kulcsfontosságú diszubsztituált malonát köztitermékek előállítása különböző cinkona-koronaéter származékok által katalizált, aszimmetrikus alkilezési reakcióban történik. A cél újfajta fázistranszfer katalizátorok – aza-koronaéterek cinkona származékai – előállítása és összehasonlítása volt az elérhető enantioszelektivitás szempontjából, valamint a reakciókörülmények is optimalizálásra kerültek. Az aminosavak előállítása a köztitermékekből szelektív hidrolízist követő átalakításokkal lehetséges

Potenciális bioaktivitással rendelkező cinkona alapú organokatalizátorok vizsgálata: Study of cinchona-based organocatalysts with potential bioactivity

One of the major representatives of organocatalysts is the group of  cinchona alkaloids, which, in addition to their outstanding role in organic synthesis, also have diverse biological effects. An excellent example is quinine, a long-known and generally used antimalarial agent possessing anticancer activity as well, thus the study of bioactivity and anticancer toxicity of other organocatalysts may be a question of interest. Multidrug resistance (MDR) is the main reason for the failure of chemotherapy, owing to the process in which malignant tumor cells develop resistance towards the cytotoxic agents used during the treatment. One of the most significant mechanisms of MDR is the elevated expression of P-glycoprotein (Pgp, ABCB1, MDR1), a protein belonging to the family of ABC (ATP-binding cassette) transporters, which recognizes many chemotherapeutic compounds as its substrate. We aimed to synthesize amine, thiourea, and squaramide derivatives from quinine, which, based on previous results of our research group, are presumably able to eliminate multidrug-resistant cells overexpressing Pgp. The synthesized compounds were tested and evaluated on parental and MDR cancer cell lines. Chemotypes have been successfully characterized in terms of cytotoxicity and resistance. Kivonat Az organokatalizátorok egy jelentős képviselői a cinkona alkaloidok, amelyek kémiai szerepük mellett változatos biológiai hatással is rendelkeznek. Ennek kiváló példája a kinin, amely egy régóta ismert és alkalmazott maláriaellenes szer, rákellenes hatással is rendelkezik, így érdekes kérdésként vetődhet fel további organokatalizátorok bioaktivitásának, rákellenes toxicitásának vizsgálata. A rosszindulatú tumorok kezelése során alkalmazott kemoterápia gyakran azért vall kudarcot, mert a tumorsejtek rezisztenssé válnak az alkalmazott citotoxikus szerekre, kialakul a multidrog rezisztencia (MDR). Az MDR egyik legjelentősebb mechanizmusa az ABC (ATP-binding cassette) transzporterek családjába tartozó P-glikoprotein (Pgp, ABCB1, MDR1) fehérje fokozott expressziója, amely számos kemoterápiás vegyületet szubsztrátjaként ismer fel. Célunk a kininből kiindulva olyan amin, tiokarbamid és négyzetamid származékok szintézise volt, amelyek a kutatócsoportunk korábbi eredményei alapján feltételezhetően képesek eliminálni a Pgp-t túlexpresszáló multidrog rezisztens sejteket. A szintetizált vegyületek tesztelését parentális és MDR rákos sejtvonalakon végeztük. Citotoxicitás és rezisztencia terén is sikeresen jellemeztük a kemotípusokat