Synthesis of ACE tricyclic systems of daphnicyclidin A and dehy-droxymacropodumine A

The synthesis of the ACE tricyclic system of daphnicyclidin A and dehydroxymacropodumine A are developed.The key reactions include an efficient aldol reaction to introduce chiral fragment 33 for further construction of piperidine ring B and seven-membered ring C, a nucleophilic addition of lithium pentene to aldehyde for installation of ring E,and a photocatalytic decarboxylation conjugate addition to construct ring C.

Asymmetric synthesis of ABC tricyclic systems in Daphniphyllum alkaloid

Efficient synthetic routs for the direct and rapid construction of[5-6-6]ABC tricyclic systems of daphmanidin A-type and calyciphylline A-type alkaloids have been successfully developed.For the daphmanidin A-type,the synthesis of[5-6-6]tricyclic framework utilize a HCl-mediated intramolecular Aldol reaction to construct the bicyclo[2.2.2]octane core and a thermal condensation to afford the ABC ring system.In addition,for the calyciphylline A-type,an improved synthesis of ABC[5-6-6]tricyclic system was developed,featuring an introduction of methyl ester group at C2 before the Pd-catalyzed intramolecular oxidative alkylation to construct the desired bowl-shape tricyclic core with stereochemical control.

Effi cacy of tricyclic antidepressants in irritable bowel syndrome:A meta-analysis

We aimed to evaluate the efficacy of tricyclic antidepressants(TCAs) as a therapeutic option for irritable bowel syndrome(IBS) through meta-analysis of randomized controlled trials.For the years 1966 until September 2008,PubMed,Scopus,Web of Science,and Cochrane Central Register of Controlled Trials were searched for double-blind,placebo-controlled trials investigating the effi cacy of TCAs in the management of IBS.Seven randomized,placebo-controlled clinical trials met our criteria and were included in the metaanalysis.TCAs used in the treatment arm of these trials included amitriptyline,imipramine,desipramine,doxepin and trimipramine.The pooled relative risk for clinical improvement with TCA therapy was 1.93(95% CI:1.44 to 2.6,P<0.0001).Effect size of TCAs versus placebo for mean change in abdominal pain score among the two studies was -44.15(95% CI:-53.27 to -35.04,P<0.0001).It is concluded that low dose TCAs exhibit clinically and statistically signifi cant control of IBS symptoms.

Geochemical significance of tricyclic and tetracyclic terpanes in source rock extracts from the Offshore Niger Delta Basin,Nigeria

Tricyclic and tetracyclic terpanes are important constituents of crude oil and source rock extracts.However,they have not been reported in the Offshore Niger Delta Basin,Nigeria.Thus,the present study investigated the geochemical significance of tricyclic and tetracyclic terpanes in source rock extracts from the Offshore Niger Delta Bain,Nigeria with gas chromatography-mass spectrometry(GC-MS).The total relative abundances of tricyclic terpanes,C_(19)TT-C_(21)TT,and C_(23) TT in the rock samples ranged from 82.50 to 96.37%,50.08 to 74.17%,and 25.83 to 49.92%,respectively.These values showed the source rocks were formed from a mixed origin(terrestrial and marine).Among the tricyclic and tetracyclic terpanes identified in the rock extracts,the conventional(C_(20)TT,C_(23)TT,C_(24)TT,C_(24)TeT)and recent(Y1,X1,Z1)were more prominent than all others,indicating mixed input of terrigenous and marine organic matter.The C_(24)TT/C_(23)TT,C_(24)TeT/(C_(24)TeT+C_(26)TT),C_(19)TT/C_(23)TT,C_(20)TT/C_(23)TT,C_(25)TT/C_(24)TeT,C_(25)TT/C_(26)TT,C_(19)TT/C_(20)TT,C_(24)TeT/C_(26)TT,Z1/(Z1+C_(24)TT),and Y1/(Y1+C_(24)TT)in the rock samples range from 0.33 to 1.30,0.76 to 0.90,0.18 to 0.73,0.34 to 1.05,0.33 to 1.74,0.30 to 1.39,0.31 to0.89,1.66 to 4.33,0.36 to 0.83,and 0.34 to 0.79,respectively.These values further showed that the rock samples were formed from mixed input of terrigenous and marine organic matter and deposited under oxic to suboxic conditions in lacustrine-fluvial/deltaic environments.Also,the C_(24)TeT/C_(20)-26TT,C_(24)TeT/C_(30)HOP,and C_(23)TT/C_(30)HOP ranged from 0.16 to 0.45,0.02 to 0.42,and 0.01 to 0.48,respectively.This range of values suggests that source rocks were within immature to early mature stage.Thus,this study showed that tricyclic and tetracyclic terpanes were effective in determining the origin,depositional environments,and thermal maturity of source rocks in the Niger Delta Basin,Nigeria.

Tricyclic Sesquiterpene from Laurencia Majuscula

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Study on the Total Synthesis of Et 743 and its Analogues: Synthesis of a Tricyclic Intermediate and its 11-Epimer

The tricyclic compound 1, a key intermediate of the pentacyclic core of Et 743 and its analogues, was synthesized. Its 11-epimer was found as the product of racemization when BOP was used as the coupling agent, but not when BOP-C1 used in the same reaction. The stereochemistry of both isomers was confirmed on basis of the 1H NMR and NOE-difference spectra.

An Efficient Synthesis of Ethyl 7-Chloro-6-fluoro-l-methyl-4-oxo-1, 4-dihydro-[1, 3]thiazeto[3, 2-a]quinoline-3-carboxylate as Intermediate of the Prulifloxacin Containing Tricyclic Fluoroquinolone

Novel ethyl 7-chloro-6-fluoro-l-methyl-4-oxo-1, 4-dihydro-[1, 3]thiazeto[3, 2-a]quino- line-3-carboxylate 2 was prepared from 3-chloro-4-fluoroaniline in eight steps. It can be used as a new intermediate for the synthesis of tricyclic fluoroquinolones.

Study on the Total Synthesis of Hainanolide－Construction of Tricyclic Intermediate（I）

Tricyclic compounds (4b-endo) and (4b-exo) are synthesized as the plausible intermediates of the total synhthesis of hainanolide by Lewis acid catalyzed intramolecular DielsAlder (IMDA) reaction.

Crystal Structure of a Tricyclic Compound C_(20)H)(28)O_6 Obtained through IMDA Reaction

The tricyclic compoun d (2) C20H28O6 has been synthesized through thereaction of IMDA. The crystals of the title compound(2A) were crystallized from etherin monoclinic space group C2 with a unit cell: a = 11. 301 (2), b=11-.863 (3 ), c =29. 59 (1) , β= 101. 02(5)°, V=3894. 246, Dc=1.2413 g/cm3, Z=8, F(000)=1568, Mr= 364. 00 R=0.055, R2=0. 055, μ= 535 cm-1, S(GOF) =0. 571. Theconfiguration of C2a-H in the title compound was found to be contrary to what wasexpected and a possible mechanism of reaction was proposed.

Study on the Total Synthesis of Hainanolide (Ⅱ)──An Unexpected Hydroperoxide Containing Tricyclic Skeleton

An unexpected compound, hydroperoxide (4) formed from (3), the exo-cycloaddition product, which was synthesized through the Lewis acid catlyzed intramolecular Diels-Alder (IMDA) reaction. Its structure was confirmed by spectra and X-Ray diffraction analysis, An 1O2oxidation mechanism was proposed.

The Inertia Indexes of One Special Kind of Tricyclic Graphs

Let G be a graph and A=(aij)n×n be the adjacency matrix of G, the eigenvalues of A are said to be the eigenvalues of the graph G, and to form the spectrum of this graph. The numbers of positive, negative and zero eigenvalues in the spectrum of the graph G are called positive and negative inertia indexes and nullity of the graph G, are denoted by p(G), n(G), η(G), respectively, and are collectively called inertia indexes of the graph G. The inertia indexes have many important applications in chemistry and mathematics. The purpose of the research of this paper is to calculate the inertia indexes of one special kind of tricyclic graphs. A new calculation method of the inertia indexes of this tricyclic graphs with large vertices is given, and the inertia indexes of this tricyclic graphs with fewer vertices can be calculated by Matlab.

Sustainability of E-Trike as Alternative Mode of Public Transportation System: The Case of Cabanatuan City, Philippines

The City of Cabanatuan is dubbed as the “Tricycle Capital of the Philippines”. Tricycle is a three wheeled vehicle used to transport people. Cabanatuan has about 30,000 registered gas-fed four-stroke motorized tricycles. Tricycle operation in this City has become the source of livelihood for around 10,000 families. Its number has tremendously increased despite growing competition and declining net daily income and the adverse effects it brings to the environment. The study analyzed the different aspects in the adoption of E-trikes (electric tricycles) as a mode of public transport system replacing motorized tricycles in the city. The conceptual framework of sustainable development was used to analyze the data. Basic accounting method in determining return on investment and payback period were used to compare the cost and return from among the current mode of transportation as against the adoption of E-trike. Data gathering employed the interviews, survey questionnaires and focus group discussion. The three areas of sustainability measured in the study were economic, socio-political and environmental. The study showed that from among 412 tricycle driver-operators randomly selected, majority were amenable to the shift from engine propelled tricycle to E-trike. However, cost of E-trike deters adoption and full implementation by the City Government. Political issue is also?the?utmost consideration since work displacement is imminent among the stakeholders once adoption of this mode takes place. On the other side, E-trike was found to be sustainable in the long run both on the point of view of operators and the riding public. The paper recommended that policy regulation be laid down, adopted, and implemented by the local government unit in response to the Philippines Cleaner Air Act.

严重生物降解原油GC-MS特征及油源对比

图牧吉油砂位于松辽盆地边缘,搞清它的油源对于该地区的油气勘探有着十分重要的意义.气相色谱-质谱分析表明,该样品受到了严重的生物降解,部分用于对比的甾、萜烷生标标志物受到了降解,使与之有关的参数值发生了变化,给油源对比带来了困难.……

A randomized controlled trial of imipramine in patients with irritable bowel syndrome

AIM: To study the efficacy of low-dose imipramine in relieving symptoms associated with the irritable bowel syndrome (IBS). METHODS: A randomized, double-blind trial of 25 mg imipramine vs matched placebo for 12 wk was performed. Doubling the dose was allowed once at week 2 in case of an unsatisfactory early response. Primary efficacy variables were subjective global symptom relief and quality of life (QoL) using SF-36 at week 12. RESULTS: One hundred and seven patients were enrolled by advertisement or referral by general practitioners and 56 (31 imipramine: 25 placebo) completed the 16-wk study. Baseline characteristics were comparable. A high overall dropout rate was noted in the imipramine and placebo arms (47.5% vs 47.9%, P > 0.05), a mean of 25.0 and 37.4 d from enrollment, respectively (P < 0.05). At the end of 12 wk, there was a significant difference in global symptom relief with imipramine over placebo (per-protocol: 80.6% vs48.0%, P = 0.01) and a trend on intent-to-treat (ITT) analysis (42.4% vs 25.0%, P = 0.06). This improvement was evident early and persisted to week 16 (P = 0.024 and 0.053 by per-protocol and ITT analyses, respectively). Mean cumulative and componentspecific SF-36 scores improved in the imipramine group only (per-protocol, P < 0.01). Drug-related adverse events leading to patient dropout were more common in the imipramine group (25.4% vs 12.5%, P > 0.05). CONCLUSION: Imipramine may be effective in the treatment of IBS patients and is associated with improved QoL. Careful patient selection, initiation of a low dose with gradual escalation and monitoring for side effects may result in an improved therapeutic response.

Prevalence, clinical features and treatment of depression in Parkinson's disease: An update

Parkinson's disease(PD) is one of the most prevalent neurodegenerative diseases which typically affects individuals over 65 years. Although the symptomatology is predominantly motor, neuropsychiatric manifestations, e.g., depression, apathy, anxiety, and cognitive impairment occur in the course of the illness and can have a great impact on the quality of life in these patients. Parkinson's disease is commonly comorbid with depression with prevalence rates of depression, generally higher than those reported in general population. Depression in PD is frequently underestimated andconsequently undertreated, which have significant effects on the quality of life in these patients. The neurobiology of depression in PD is complex and involves alterations in dopaminergic, serotonergic, noradrenergic and possibly other neurotransmitter systems which are affected in the course of the disease. The tricyclic antidepressants and the selective serotonin reuptake inhibitors are the two classes of antidepressant drugs used for depressive symptoms in PD. Several published studies suggested that both classes are of comparable efficacy. Other serotonergic antidepressants, e.g., nefazodone and trazodone have also been of benefit. Meanwhile, there are limited data available on other drugs but these suggest a benefit from the serotonin and noradrenaline reuptake inhibitors such as mirtazapine, venlafaxine, atomoxetine and duloxetine. Some of the drugs used in symptomatic treatment of PD, e.g., the irreversible selective inhibitors of the enzyme monoamine oxidase-B, rasagiline and selegiline as well as the dopamine receptor agonist pramipexole are likely to have direct antidepressant activity independent of their motor improving action. This would make these drugs an attractive option in depressed subjects with PD. The aim of this review is to provide an updated data on the prevalence, clinical features of depression in subjects with PD. The effects of antiparkinsonian and antidepressant drugs on depressive symptoms in these patients are also discussed.

Navigating the Nomenclature of a Purported “Dietary Supplement”: A Cautionary Tale for Consumers and Practitioners Regarding Tianeptine or “Gas Station Heroin”

Dietary supplement sales have surpassed $30 billion per year with their use becoming and remaining extremely popular amongst the general public. There are numerous bioactive components, both nutritive and non-nutritive, in dietary supplements with considerable efficacy in promoting health. However, there are many ways disallowed ingredients may enter the supplement pipeline with potentially toxic effects. Dietary supplements can be regulated (either pre- or post-market) as a drug, dietary supplement, a nutraceutical, new dietary ingredient (NDI), generally recognized as safe (GRAS) food ingredient, a food additive, or a food. A pharmaceutical drug (medication) is used to treat, cure, prevent, or diagnose a disease and is regulated by the FDA pre-market only and allowed by medical prescription, whereas the other labeling designations are largely regulated post-market. One such molecule with a labeling problem is tianeptine, which has global use as an efficacious, prescribed drug, while at the same time being considered a non-drug and potentially dangerous adulterant often referred to as gas station heroin. In this paper, we critically evaluate the use and labeling of this compound and attempt to clarify the conundrum surrounding its legal or illegal use. Tianeptine is effective and efficacious as an antidepressant in those responding poorly to selective serotonin reuptake inhibitors (SSRIs) and exhibits many medicinal characteristics of tricyclic antidepressants with fewer opioid-like side effects. As a result, sixty-six countries permit use of tianeptine as a prescription drug. At higher doses, tianeptine has recently been shown to exhibit significant potential for abuse and dependency along with toxicity. As such, the US does not recognize tianeptine as an FDA-approved drug or as a dietary supplement, nutraceutical, new dietary ingredient (NDI), GRAS ingredient, or a food. Instead, tianeptine is a synthetic adulterant of a dietary supplement and considered technically an unapproved food additive. In conclusion, tianeptine, although viewed as a safe dietary supplement by many, is illegal in the US despite benefits to many but toxicity to others that make it vital that consumers and healthcare providers learn to critically evaluate and navigate the often confusing nomenclature of a purported dietary supplement to convey to the public whether it is efficacious, safe, and legal.

Pharmacological management of neuropathic pain in patients with vestibular schwannomas:Experience of the Atlantic Lateral Skull Base Clinic

Neuropathic pain is chronic pain generated by disorders of the peripheral and central nervous system, including skull base tumours. A skull base tumour can be any type of tumour that forms in the skull base, and this includes vestibular schwannomas which arise from the sheath of the inner ear vestibulocochlear nerve(eighth cranial nerve). Growth of the tumour, surgical resection, and/or stereotactic radiotherapy may result incompression and/or irritation of the fifth cranial nerve(trigeminal nerve) resulting in facial pain and/or numbness. Non-trigeminal afferent input may contribute to the wide constellation of symptoms seen in orofacial pain patients. The purpose of this report was to develop a decision tool to guide the recognition and treatment of neuropathic pain in this specialized population. Recommendations for treatment are based on evidence presented in Canadian and international neuropathic treatment guidelines. Algorithms are included for assessment and treatment of adult patients with agents that are recognized to have analgesic efficacy within the broad context of neuropathic pain.

Paediatric amitriptyline overdose

We report a near fatal case of paediatric amitriptyline overdose including a series of ECGs demonstrating the effects of sodium bicarbonate therapy on cardio-toxicity. We briefly discuss the role of sodium to counteract the sodium channel blockade of tricyclic antidepressants and discuss the possible utility of lipid emulsion therapy in such cases.

Model-Based Approach to Investigate the Influences of Different Load States to the Vehicle Dynamics of Light Electric Vehicles

The need to find alternative urban mobility solutions for delivery and transport has led mobility companies to devote enormous resources for research-based solutions to increase vehicle safety. This paper documents a virtual approach to investigate the influences of different load states to the vehicle dynamic of light electric vehicle. A model basing on a three-dimensional multibody system was used, which consists of five bodies. By applying methods of multibody modelling the generalized equations of motion were generated. To include the behavior within the contact point between road and vehicle a simplified tire models was added. The implementation of the equations allowed a first validation of the model via simulations. In a final modeling step the simulation results were interpreted in respect of plausibility. Afterwards, the model was simulated numerically to investigate different load states of the vehicle, by applying constant steering stimuli and variable velocities. In sum, the investigated model approach is useful to identify safety relevant parameters and shows the effects of load states to the vehicle dynamics. Furthermore, it behaves plausibly regarding general vehicle dynamics. These results prove the general usability of the model for the development controllers and estimators in driver assistances systems.

Road traffic accidents, near-misses and their associated factors among commercial tricycle drivers in a Nigerian city

Tricycles form an important part of the intra-city transport system, following the ban placed on motorcycles in Maiduguri, Nigeria. However, no previous studies have been conducted to assess the occurrence of accidents among them. The objective of this study was to determine the prevalence of road accidents, near-misses, and their associated factors among commercial tricycle drivers in Maiduguri. A cross-sectional study was conducted among registered commercial tricycle drivers in Maiduguri who had been in the business for at least a year. Data was collected through face-to-face interviews, using a structured questionnaire, and was subjected to bivariate and multivariate analysis using SPSS. The prevalence of road accidents and near misses were 46% and 50.3% respectively. Only six (3.9%) of respondents who had experienced a near-miss mentioned that they occurred while they were fully awake;during clear weather;and on a smooth, broad, and non-congested road. All the others had experienced the near miss under an unfavourable weather, road, and/or while feeling sleepy. In the bivariate analysis, only psycho-active substance use (χ^2=3.941;df =1;p=0.047) and having experienced more than one near miss (χ^2=31.807;df =1;p<0.001) were significantly associated with having an accidents. However, in the multivariate analysis, having experienced more than one near miss was the only factor which significantly predicted having an accident (OR=2.89 95% CI: 1.64-5.09;p<0.001). There is a need to conduct further intervention studies to determine the effectiveness of intervention measures in reducing accident rates among these tricycle drivers.