Coumarin and its derivatives are reactive compounds, suitable for many syntheses. They are used as anticoagulants, antibacterial, animistic compounds. The interest in coumarins has increased because it was found that they reduce the HIV virus activity. The synthesis of 4-arylaminocoumarin derivatives from 4-hydroxycoumarin, has been carried out, and their antimycotic effects were tested. In the QSAR (quantitative structure-activity relationship) QSPR (quantitative structure-property-activity relationship) study we have used physicochemical properties and topological indices (Balaban index J(G), Wiener index W(G), information-theoretical index I(G), and valence connectivity index (G), to predict bioactivity of the newly synthesized coumarin compounds. By using methods of molecular modelling, the relationships between structure, properties and activity of coumarin compounds have been investigated. The best QSPR models were obtained using valence connectivity index or combination indices. According Rekker's method the best correlation of calculated values log P, has been obtained with the model based on the inhibition zone (I) 4-arylaminocoumarin derivatives expressed in mm. The results obtained in this study enable further synthesis of new coumarin derivatives and predict their biological activity and properties.
Cardiovascular diseases are leading cause of morbidity in the world. Measurement of the level of biochemical markers in the serum is one of World Health Organisation (WHO) criteria in diagnosing acute myocardial infarction (AMI). Non-specific clinical state of patients and insufficiently sensitive electrocardiographic (ECG) diagnostics, at patient's hospital admission time, point out the importance of biochemical markers in acute myocardial infarction diagnosis. Technology development and new diagnostic methods lead to the invention of highly sensitive and specific marker as myocardial damage evidence. Cardiac Troponin I (cTnI) is specific marker for myocardial damage1. Its elevation in the serum within myocardial ischemia symptomatology is important in diagnosis of myocardial infarction.
Polytrauma with significant lesion of peripheral nerves is a specific war injury. It is also one of the most delicate problems in rehabilitation treatment because it requires a close cooperation with surgeon and timely surgical interventions. Based on our experience, the best results in the treatment of injured persons with lesion of peripheral nerves have been accomplished after the surgical treatment. Results in the neurolysis were better than those accomplished in neurorrhaphy. Total of 436 patients with lesion of peripheral nerves were recorded and 56 patients with plexus lesion. Out of this number, 78 patients (about 15%) had surgical treatment (41 neurorrhaphy and 37 neurolysis). Due to lack of adequate ENMG diagnostics, the objective valorisation of treatment outcome was not possible.
In this paper we present introduction and development of some new analytical methods for identification of anabolic steroids, their metabolites and certain hormones, especially determination of exogenous testosterone by means of gas chromatography-mass spectrometry. Identification of central nervous stimulants and corticosteroides has been performed by high performance liquid chromatography. In desire to achieve better results, to increase strength and endurance, to sharpen reflexes and to reduce stress and anxiety athletes as well as other people use different pharmacological substances, hormones or even illicit drugs. Use of these substances without medical supervision can lead to adverse effects to one's health or even cause a death. At the same time, use of such substances means a kind of cheat that could not be accepted. This is why International Olympic Committee started at 1968 with official doping control that is permanently carried out and continuously increasing number of banned substances. Doping control demands for discover and development of new sensitive and specific methods for detection of banned substances and their metabolites in urine and blood.
Panic disorder (PD) is an acute psychobiologic reaction manifested by intense anxiety and panic attacks, that occur unpredictably with subjective sense of intense apprehension or terror, accompanied by temporary loss of the ability to plan, think, or reason and the intense desire to escape or flee the situation. Panic attacks may last from a few seconds to an hour or longer. Symptoms typically include, among others, palpitations, tachycardia, hypertension, chest pain, dyspnoea, and fear of loosing control or going crazy and vague feeling of imminent doom or death. Since pharmacotherapy of PD includes the administration of selective serotonin reuptake inhibitors and tricyclic antidepressants, the objective of this study was to perform a pilot double blind clinical trial designed to compare the effects of two studied drugs in the treatment of PD. A total number of 40 patients with a history of panic disorder were randomly assigned into two groups of 20 patients each. Hamilton anxiety rating scale and Standard Psychiatric Interview were methods for PD assessment. One group was treated with clomipramine hydrochloride (ANAFRANIL) 75 mg/day and the other with fluoxetine (OXETIN) 60 mg/day. Both drugs were administrated by mouth (PO) two times-a-day in equally divided doses for 6 weeks. Both studied agents produced similar antipanic effectiveness. Favourable response was achieved in 95% of patients treated with fluoxetine and 90% of patients treated with clomipramine. The onset of antipanic effects was quicker in all clomipramine treated patients, while fluoxetine produced more-favourable response in male patients. The duration of treatment with both antidepressants studied should be at least 10 weeks, instead of 6 weeks.
Drugs, natural medicinal plant, animals and mineral materials, have a large and various application in official pharmacy and medicine. Carriers of multilateral pharmacological effects that those drugs shown, are chemically define as active components that are present in them. Methods of qualitative and quantitative analysis are used for the chemical investigation of components that drugs contain. Method of thin layer chromatography has been shown as very reliable. According to the chemical investigation of single drugs, it is possible to define a group of compound or single compound comparing them with standards. Relating to the usage of method of thin layer chromatography, it has been carried out investigation on presence of coumarins and flavonoids in domestic plant material that have wide everyday usage. Coumarins and flavonoids from the point of view of chemical belonging are phenol derivatives with important pharmacological effects. Applying method of thin layer chromatography, it is detected presence of coumarins and flavonoids substances in plant material that has been tested. Anethi graveolens fructus et folium (fruit and leaf of dill), Anethum graveolens L., Apiaceae, Avenae sativae fructus (fruit of oats), Avena sativa L., Poaceae and Asperulae odoratae herba (sweet woodruff), Asperula odorata L., Rubiaceae. Chromatograms are developed in systems cyclohexane-ethylacetat (13:7) and toluene-ether (1:1) saturated with 10% acetic acid, and visualisation by observing on UV lamp (254 and 366 nm), spraying with reagents KOH (10% ethanol solution) and diphenylboryloxyethylamine (1% methanol solution).
An increased understanding of the phenomenon of polymorphism should enable pharmaceutical scientists to gain control over the crystallization process in order to selectively obtain the desired polymorph or suppress the growth of an undesired one. Phase changes during processing and scale-up are a problem, which may be avoided by carefully designed initial small-scale studies. The availability of detailed structural data, combined with strategic design of substrates and additives, has led to significant advances in the control over the polymorphs obtained in a particular crystallization. With all the information available from these initial studies, it should be possible to design and to select processing conditions which would give a desired polymorph and maintain the desired form throughout the various stages of drug processing and manufacture.
The skin is an excellent barrier to the transport of charged compounds and large molecules. Many substances of present and potential therapeutic utility carry charge at physiological pH, have high molecular weights and/or are hydrophilic and, consequently, do not transport well across the skin. Pathways for the transport of small ions do appear to exist through the skin and flow along these pathways can be substantially enhanced by iontophoresis.
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