We describes in this chapter, the assignment of the 1,4- and 1,5-regioisomer structures of N-protected 2-(1H-1,2,3-triazol-1-yl)-glycine derivatives on the basis of 1H NMR, IR and chemical pathway. A subsequent assignment of 1,4- and 1,5-regioisomer structures of biheterocyclic glycine derivatives and their phosphonic analogues were based on spectroscopic study in 1H NMR and 13C NMR.
Author(s) Details :
Saïd Achamlale Laboratory of Scientific Research and Pedagogic Development (LSRPD) CRMEF Fez-Meknes, Morocco.
Anouar Alami Organic Chemistry Laboratory (LCO), Faculty of Sciences Dhar El Mahraz, Sidi Mohammed Ben Abdellah University, P.B. 2626, Fez 30000, Morocco.
Younas Aouine Organic Chemistry Laboratory (LCO), Faculty of Sciences Dhar El Mahraz, Sidi Mohammed Ben Abdellah University, P.B. 2626, Fez 30000, Morocco.
Department of Chemistry, Faculty of Sciences, Ibn Zohr University, P.B. 8106, Cité Dakhla, Agadir 80060, Morocco
Ultrasonic velocity, density and viscosity of a binary system of acrylonitrile in 1, 4-Dioxane have been measured at 298 K and 2 MHz. Experimental data of the ultrasonic sound velocity, density and viscosity have been used to calculate various acoustical parameters, such as adiabatic compressibility (βa), intermolecular free length (Lf), free volume (Vf), excess values of adiabatic compressibility (βaE), excess values of free length (LfE) and excess values of free volume (VfE). It is observed from these acoustical parameters that, weak intermolecular interactions are confirmed in this system. Dipole inducement in the system is found to be more predominant. The nonlinear behavior of all these parameters throws more light on the various interactions among the molecules.
Dr. G. R. Bedare Department of Physics, N. S. Science and Arts College, Bhadrawati, Dist – Chandrapur (MS), India.
The study of heterocyclic systems provides most fascinating field for exploration in view of variety of interesting and intricate reactions, which lead to synthesis of unusual systems having diversities in their skeletal pattern. In this context, various new heterocycles and derivatives are synthesized with increased biological activities and less toxicity. Benzo-fused azoles containing three heteroatoms, specially, benzo[d][1,2,3]triazole, has received great attention, these days, for their chemical and biological properties and many of them are used as medicines for various diseases. Many researches have also shown that when heterocyclic and aliphatic secondary amines are introduced in a variety of heterocyclic compounds, the resulting compounds have been found to possess enhanced biological activities. Therefore aim of our research was to hook benzotriazole scaffold with these amines with a help of suitable linker in thirst of obtaining the resulting synthesized molecules possessing high and varied biological activities which can be useful to mankind in future. We have synthesized N-aminoalkylated derivatives of benzo[d][1,2,3]triazole. All the synthesized compounds were fully characterized on the basis of their detailed spectral studies and were evaluated for their antimicrobial activities in vitro.
Bharti Bhardwaj Department of Chemistry, University of Delhi, Delhi-110 007, India.
Sunita Bhagat Department of Chemistry, ARSD College, University of Delhi, India.
This study was designed to evaluate the phytochemical profile and the antimicrobial potential of the essential oil of Salvia brachyodon Vandas growing wild in Croatia. The emergence of multidrug resistant bacteria has become a serious threat to public health that has prompted research to the discovery and development of new active agents capable of partly or completely suppressing bacterial growth. Recently, a class of biological active compounds that has been attracting increased attention in drug discovery is the plant based derivatives. Many plants produce special biomolecules to protect themselves according to a stress or infection caused by microorganisms. Plants produce a broad assortment of secondary metabolites, including tannins, terpenoids, alkaloids, polyphenols and favonoids, which have been found in vitro to have antimicrobial properties against both Gram- positive and Gram- negative bacteria. Essential oils (EOs) are secondary metabolites, and are important for plant defense mechanism hence, they have various medicinal properties including antimicrobial activity. Natural products isolated from Salvia spp. have long been used in traditional medicine to treat several microbial afflictions, but considering the high number of species of this genus, the antimicrobial properties of all of them is not well known. Short tooth sage (S. brachyodon Vandas), an endemic species that grows in the south east areas of the Adriatic coast in Croatia, Bosnia and Herzegovina, and Montenegro. It is a perennial plant that grows up to 70-80 cm in height and flowers from July to September. The phytochemical components of the essential oil were identified by gas chromatography-mass spectrometry (GC-MS) analysis. The antimicrobial activity was assessed against a panel of representative Gram-positive and Gram-negative bacteria as well as fungi. The antimicrobial activities of the oil against pathogenic microorganisms were determined by using agar disc diffusion and broth microdilution methods. From the thirty-eight identified constituents representing 95.7% of the oil, 1,8-cineole (16.7%), β-pinene (19.7%) and α-pinene (7.6%), were the major components. The levels of oxygenated monoterpenes such as camphor (5.6%), borneol (4.2%), myrtenol (2.4 %) and terpinen-4-ol were significant. Other important compounds were sesquiterpenes hydrocarbons β-caryophyllene (6.6%), α-humulene (4.9%), viridiflorol (3.0%), spathulenol (2.9%) and aromadendrene. Preliminary antimicrobial screening revealed that the oil exhibited a very interesting antimicrobial profile. The oil exhibited moderate in vitro antibacterial activity after it was tested against twenty pathogenic bacteria and fungal strains, but high antimicrobial activity observed against medically important pathogens such as E. coli O157:H7, Listeria monocytogenes and Candida albicans. Results presented here may suggest that the essential oil of S. brachyodon possess antimicrobial properties, and is, therefore, a potential source of antimicrobial ingredient in food and pharmaceutical industry. The obtained results are preliminary and a further research is needed in order to obtain information regarding the practical effectiveness of essential oil to prevent the growth of foodborne and spoilage microbes under specific application conditions.
Dr. M. Skočibušić Faculty of Science, University of Split, Croatia.
Mrs. S. Lacić Faculty of Science, University of Split, Croatia.
Background: Malaria is one of the most common parasitic disease in tropical and subtropical regions. Plasmodium falciparum, one of the causative agent of malaria is resistant to many type of antimalarial drugs. This study present in vitro assessment of the antiplasmodial activity of substituted phénanthrolinone compounds.
A series of 7 substituents were used to substitute the chlorine on the 5
position in the 5-chloro-3,4-dihydro-1H-pyrano[3,4-b]-1,10-phenanthrolinone
ring. In vitro antiplasmodial activities were evaluated on
chloroquine-sensitive and resistant strains of P. falciparum.
The results showed that compounds 7 and 8 possessing N,N-diethylamino side
chain had the best antiplasmodial activities. In addition, the cytotoxic
activities were evaluated on HeLa cells and compound 8 was the least cytotoxic
of all studied compounds.
The synthesis and antimalarial activity of substituents of compound 2 were
carried out. This study has shown that compounds with basic and lipophilic
substituents exhibited the best antiplasmodial activity. Drug resistance of parasites and anopheles
remains a major problem in the malaria burden. At present, the best chemically
solution to eradicate definitely this disease is establishment of new
antimalarial drug which is exempt of any resistance. The 1,10-phenanthroline
skeleton was synthesized and studied for it potential new antimalarial
activity. Its pharmacomodulation led to several compounds among which compound
8 showed higher activity as compared to the parent compound 2. This compound
should be used for future pharmacomodulation particularly to open the lactone
ring in basic medium.
Pr. Cheikh Sall Laboratoire de Chimie, UFR des Sciences de la Santé, Université de Thiès, BP 967 Thiès, Sénégal.
It is estimated that there will be an increase in the incidence of chronic obstructive pulmonary disease (COPD) in the coming decades. Thus, the pharmacological attributes of products of plant origin should be considered as an important economic and scientific strategy in the investigation of therapeutic alternatives, since their experimental validations are indispensable to substantiate the reliability of these products in the treatment of chronic diseases. Like biologically active compounds, Eucalyptol, also known as 1,8- cineole, is the major constituent of the leaf oil of eucalyptus species, such as Eucalyptus globulus and Eucalyptus tereticornis. It is a terpenoid oxide, free of steroid-like side effects. This study is based on a review of the specialised literature with purpose to discuss the biological effects of Eucalyptol in the respiratory system and its interaction with some of the most promising targets in the treatment of COPD, such as: receivers and membrane channels, oxidative stress, transcription and expression of cytokines, cell adhesion molecules and neutrophil chemotaxis, proteases and remodeling.
Fladimir de Lima Gondim Postgraduate Program in Physiological Sciences, State University of Ceará, Ceará, Brazil.
Gilvan Ribeiro dos Santos Center of Technological Sciences, State University of Ceará, Ceará, Brazil.
Daniel Silveira Serra Center of Technological Sciences, State University of Ceará, Ceará, Brazil.
Francisco Sales Ávila Cavalcante Center of Technological Sciences, State University of Ceará, Ceará, Brazil.