Nitrite-catalyzed economic and sustainable bromocyclization of tryptamines/tryptophols to access hexahydropyrrolo[2,3-b]indoles/tetrahydrofuroindolines in batch and flow

A highly efficient and concise bromocyclization has been successfully achieved,in which tryptamine/tryptophol derivates can be transformed to valuable HPI/TFI scaffolds with economic and green manners.Moreover,a controllable cascade transformation of bromocyclization and aromatic bromination has also been smoothly achieved to form dibrominated HPIs and TFIs.Production could be successfully scaled up under both the batch process and a continuous flow fashion.The most remarkable peculiarity of our process over all previous methods is that the generated water is the major waste.Notably,successful application of this new protocol has been demonstrated by the pharmaceutical and natural products syntheses.

Research progress on the mechanism of exercise against depression

The substantial global health burden of depression encourages the development of innovative and broadly effective interventions.This paper aimed to examine recent advancements by which exercise works as an antidepressant and recommends optimal types and quantity of exercise as supplemental therapies in treating depression.Sedentary behavior and low physical activity significantly influence the onset of depression.Being an effective treatment option,exercise can significantly reduce depression risk.Exercise exerts antidepressant effects as it modulates neurotransmitters,neuroplasticity,the immune system,and hormone levels.Effective exercise forms include yoga,strength training,and walking/jogging.Tailored exercise regimens that consider individual preferences and tolerability can improve outcomes.Regular exercise enhances general well-being and reduces depressive symptoms.Additional research is needed to understand the complex basis of exercise's effects on depression.Exercise is a cost-effective and accessible intervention for depression management that needs additional exploration.Thus,customized exercise programs,as per each patient’s needs,are essential for their successful implementation clinically.

DFT-based QSAR and Action Mechanism of Phenylalkylamine and Tryptamine Hallucinogens

DFT/B3LYP/6-311G＋（d,p） basis set including solvent effect was first used to calculate a set of molecular descriptors of 55 phenylalkylamine and 20 tryptamine compounds with hallucinogenic activity. Four quantitative structure-activity relationship （QSAR） models of the hallucinogenic activity for phenylalkylamines and tryptamines were obtained by employing multiple linear regression （MLR） method. The QSAR analysis indicated that electron-related descriptors were major contributors to the hallucinogenic activities of phenylalkylamines and tryp- tamines. In addition, electron-unrelated descriptors have some impact on the hallucinogenic activities of phenylal- kylamines. Based on the results of QSAR study, a novel Conformation Complementary Judgement, Transformation and Induction （CCJTI） model had been proposed to explain different action mechanisms of phenylalkylamines and tryptamines with their target receptors. It was concluded that phenylalkylamines might combine with receptor by electronic effect, but steric factor could affect it also, whereas tryptamines could act only through the electronic effect.

Synthesis of tetrahydro-β-carbolines from phthalic anhydrides and tryptamine

Tetrahydro-b-carbolines with strictosamide skeleton have been synthesized via intermolecular condensation, selective reduction, and intramolecular cyclization starting from phthalic anhydrides and tryptamine. The reactions are carried out under mild conditions with a wide range of substrates and functional groups.

Preparation and evaluation of mixed-mode resins with tryptophan analogues as functional ligands for human serum albumin separation

Five tryptophan analogues with a hydrophobic indole ring and an amino group on each molecule were used as functional ligands of mixed-mode resins for human serum albumin(HSA) purification. Their adsorption performance was evaluated and the effects of p H and salt addition on HSA adsorption were studied. The resins prepared showed typical p H-dependent adsorption and the highest adsorption capacity and affinity were found at pH 5.0for all the resins tested. The saturated adsorption capacity was 138.02 mg·g^(-1)with the tryptaminefunctionalized resin, which significantly decreased at p H below 4.0 due to electrostatic repulsion between ligands and HSA. Moreover, the addition of Na Cl or(NH_4)_2SO_4in media reduced HSA adsorption capacity, although the two salts showed different affecting profiles. The tryptamine-functionalized resin showed the best salt-tolerant performance, and its high adsorption capacity was maintained under high salt concentrations. In addition, the five resins prepared showed good adsorption selectivity for recombinant HSA from Pichia pastoris broth. Molecular docking results between tryptamine and HSA indicated that tryptamine was favorable to bind on Site II(indole-binding site) of HSA.

First total synthesis of marine alkaloid hyrtiosulawesine

Hyrtiosulawesine was isolated from Indonesian specimens of the marine sponges Hyrtios erectus and H.reticulatu in 2002.We report here the first total synthesis of hyrtiosulawesine using an efficient and convenient synthetic strategy which could be widely used in the synthesis of otherβ-carboline compounds.All structures of new compounds were confirmed by 1H NMR,13C NMR and HRMS.