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Fluorescence Spectrometric Determination of Drugs Containing -Methylene Sulfone/Sulfonamide Functional Groups Using N1-Methylnicotinamide Chloride as a Fluorogenic Agent  [PDF]
Khaled M. Elokely,Mohamed A. Eldawy,Mohamed A. Elkersh,Tarek F. El-Moselhy
International Journal of Analytical Chemistry , 2011, DOI: 10.1155/2011/840178
Abstract: A simple spectrofluorometric method has been developed, adapted, and validated for the quantitative estimation of drugs containing -methylene sulfone/sulfonamide functional groups using N1-methylnicotinamide chloride (NMNCl) as fluorogenic agent. The proposed method has been applied successfully to the determination of methyl sulfonyl methane (MSM) (1), tinidazole (2), rofecoxib (3), and nimesulide (4) in pure forms, laboratory-prepared mixtures, pharmaceutical dosage forms, spiked human plasma samples, and in volunteer's blood. The method showed linearity over concentration ranging from 1 to 150? g/mL, 10 to 1000?ng/mL, 1 to 1800?ng/mL, and 30 to 2100?ng/mL for standard solutions of 1, 2, 3, and 4, respectively, and over concentration ranging from 5 to 150? g/mL, 10 to 1000?ng/mL, 10 to 1700?ng/mL, and 30 to 2350?ng/mL in spiked human plasma samples of 1, 2, 3, and 4, respectively. The method showed good accuracy, specificity, and precision in both laboratory-prepared mixtures and in spiked human plasma samples. The proposed method is simple, does not need sophisticated instruments, and is suitable for quality control application, bioavailability, and bioequivalency studies. Besides, its detection limits are comparable to other sophisticated chromatographic methods. 1. Introduction Encouraged by the successful application of the NMNCl methodology to the determination of a similar α-methylene carbonyl functional group containing drugs, namely, warfarin [1], pentoxifylline, propafenone hydrochloride and acebutolol hydrochloride [2], the almost isosteric α-methylene sulfoxide group, such as proton pump inhibitors (PPIs) and the cyclic α-methylene carbonyl group, such as ketamine hydrochloride, griseofulvin, and levonorgestrel (unpublished results), we decided to investigate the possibility of extending the application of such methodology to drugs containing the isosteric α-methylene sulfone/sulfonamide functional groups, namely, methyl sulfonyl methane (MSM) (1), tinidazole (2), rofecoxib (3), and nimesulide (4). Methyl sulfonyl methane (MSM) (1) is a relatively new dietary supplement form of sulfur that is found in our living tissues. MSM supports healthy connective tissues like tendons, ligaments, and muscle. Thus, it is important in conditions such as arthritis, muscle pains, and bursitis. MSM should be considered an integral part of any health care practice because of its physiological action, indirect importance, and current/future uses [3–5]. In this report, MSM was used as a model compound and was found to react successfully with NMNCl
INVESTIGATION OF THE ROLE OF PLACENTA IN TRANSFER OF BROMINE CONTAINING DRUGS TO INFANTS
Z. Abedinzadeh,Z.Khalkhali
Acta Medica Iranica , 1980,
Abstract: A study was undertaken to investigate the role of placenta in transferring drugs containing bromine to the infant. 20 pregnant subjects were given bromine as KBr (500 mg/50 Kg weight) 10h before the delivery the bromine content of the serum in the mother and the child was estimated by neutron.. 13 lrradlated at 2xlO activation analysis. Samples were -2 -1 n em 5 for a period of one hour. A Ge (Li) detector connected to an 800 channel analyser 82 was used for measuring Br photopeaks. In 72% of the cases the distribution of bromine in both mother and child was equal, revealing a transfer across the placenta of the intaken drug.
SYNTHESIS AND CHARACTERIZATION OF THERMALLY STABLE NOVEL POLYMERS CONTAINING PHENYLTHIOUREA, AZO AND SULFONE GROUPS IN THE BACKBONE
SIVADHAYANITHY,MYLSAMY; RAVIKUMAR,LINGAM; RAMACHANDRAN,T;
Journal of the Chilean Chemical Society , 2007, DOI: 10.4067/S0717-97072007000300007
Abstract: the present work deals with the synthesis of thermally stable polymers that contain phenylthiourea, sulfone and azo group in the backbone from bisphenol and diacid chlorides. the bisphenol containing phenylthiourea and azo groups was synthesized via three steps. in the first step, 4,4'-bis(thiourea) diphenyl sulfone (btds) was obtained from 4,4'- diaminodiphenyl sulfone and ammonium thiocyanate. the second step involved the diazodisation reaction of 4-aminophenol. the third step in the preparation of the monomer was the coupling of bisthiourea (btds) with the diazonium chloride in the presence of an alkali which resulted in 4,4'-bis(p-hydroxyphenyl azo thiourea)diphenyl sulfone (hp-atds). the final step was the synthesis of polyesters by polycondensation reaction of this monomer with various acid chlorides (both aromatic and aliphatic). the polymers were characterized by solution viscosity, uv-vis, ft-ir,'h-nmr and tga. solubility of the polymers was also tested with different solvents, which is an important parameter for the processablity of the polymer. the synthesis and characterization of the monomer and polymers is discussed herein
SYNTHESIS AND CHARACTERIZATION OF THERMALLY STABLE NOVEL POLYMERS CONTAINING PHENYLTHIOUREA, AZO AND SULFONE GROUPS IN THE BACKBONE  [cached]
MYLSAMY SIVADHAYANITHY,LINGAM RAVIKUMAR,T RAMACHANDRAN
Journal of the Chilean Chemical Society , 2007,
Abstract: The present work deals with the synthesis of thermally stable polymers that contain phenylthiourea, sulfone and azo group in the backbone from bisphenol and diacid chlorides. The bisphenol containing phenylthiourea and azo groups was synthesized via three steps. In the first step, 4,4'-bis(thiourea) diphenyl sulfone (BTDS) was obtained from 4,4'- diaminodiphenyl sulfone and ammonium thiocyanate. The second step involved the diazodisation reaction of 4-aminophenol. The third step in the preparation of the monomer was the coupling of bisthiourea (BTDS) with the diazonium chloride in the presence of an alkali which resulted in 4,4'-bis(p-hydroxyphenyl azo thiourea)diphenyl sulfone (HP-ATDS). The final step was the synthesis of polyesters by polycondensation reaction of this monomer with various acid chlorides (both aromatic and aliphatic). The polymers were characterized by solution viscosity, UV-Vis, FT-IR,'H-NMR and TGA. Solubility of the polymers was also tested with different solvents, which is an important parameter for the processablity of the polymer. The synthesis and characterization of the monomer and polymers is discussed herein
Synthesis and Antifungal Activity of Novel Sulfone Derivatives Containing 1,3,4-Oxadiazole Moieties  [PDF]
Weiming Xu,Jiang He,Ming He,Feifei Han,Xuehai Chen,Zhaoxi Pan,Jian Wang,Maoguo Tong
Molecules , 2011, DOI: 10.3390/molecules16119129
Abstract: A series of new sulfone compounds containing 1,3,4-oxadiazole moieties were synthesized. The structures of these compounds were confirmed by spectroscopic data (IR, 1H- and 13C-NMR) and elemental analyses. Antifungal tests indicated that all the title compounds exhibited good antifungal activities against eight kinds of plant pathogenic fungi, and some showed superiority over the commercial fungicide hymexazol. Among them, compounds 5d, 5e, 5f, and 5i showed prominent activity against B. cinerea, with determined EC50 values of 5.21 μg/mL, 8.25 μg/mL, 8.03 μg/mL, and 21.00 μg/mL, respectively. The present work demonstrates that sulfone derivatives such as 5d containing a 1,3,4-oxadiazole moiety can be used as possible lead compounds for the development of potential agrochemicals.
Magnesium-containing drugs in cardiovascular diseases  [cached]
A.V. Govorin,A.P. Filev
Rational Pharmacotherapy in Cardiology , 2012,
Abstract: At present experimental and clinical data confirming efficacy of magnesium-containing drugs in different cardiovascular diseases are obtained. Physiological significance of magnesium is determined by its intracellular fraction. That is why it is desirable to use magnesium with the components contributing to its intracellular penetration. Magnerot deserves attention as a complex drug consisting of magnesium and orotic acid that contributes to intracellular penetration. Data of some studies on magnesium-containing drugs application in different cardiovascular diseases are presented.
Thermoanalytical Investigation of Terazosin Hydrochloride
Ali Kamal Attia,Mona Mohamed Abdel-Moety
Advanced Pharmaceutical Bulletin , 2013, DOI: 10.5681/apb.2013.025
Abstract: Purpose: Thermal analysis (TGA, DTG and DTA) and differential scanning calorimetry (DSC) have been used to study the thermal behavior of terazosin hydrochloride (TER). Methods: Thermogravimetric analysis (TGA/DTG), differential thermal analysis (DTA) and differential scanning calorimetry (DSC) were used to determine the thermal behavior and purity of the used drug. Thermodynamic parameters such as activation energy (E*), enthalpy ( H*), entropy ( S*) and Gibbs free energy change of the decomposition ( G*) were calculated using different kinetic models. Results: The purity of the used drug was determined by differential scanning calorimetry (99.97%) and specialized official method (99.85%) indicating to satisfactory values of the degree of purity. Thermal analysis technique gave satisfactory results to obtain quality control parameters such as melting point (273 oC), water content (7.49%) and ash content (zero) in comparison to what were obtained using official method: (272 oC), (8.0%) and (0.02%) for melting point, water content and ash content, respectively. Conclusion: Thermal analysis justifies its application in quality control of pharmaceutical compounds due to its simplicity, sensitivity and low operational costs. DSC data indicated that the degree of purity of terazosin hydrochloride is similar to that found by official method.
Lithium difluoro(oxalato)borate tetramethylene sulfone disolvate  [cached]
Joshua L. Allen,Paul D. Boyle,Wesley A. Henderson
Acta Crystallographica Section E , 2011, DOI: 10.1107/s1600536811011743
Abstract: The title compound, Li+·C2BF2O4 ·2C4H8O2S, is a dimeric species, which resides across a crystallographic inversion center. The dimers form eight-membered rings containing two Li+ cations, which are joined by O2S sulfone linkages. The Li+ cations are ligated by four O atoms from the anions and solvent molecules, forming a pseudo-tetrahedral geometry. The exocyclic coordination sites are occupied by O atoms from the oxalate group of the difluoro(oxalato)borate anion and an additional tetramethylene sulfone ligand.
Investigation of Frequency of Leftover Drugs at Home and Related Factors
Ercan Gocgeldi,Muharrem Ucar,Cengiz Han Acikel,Turker Turker
TAF Preventive Medicine Bulletin , 2009,
Abstract: AIM: The purpose of this survey was to investigate the frequency of leftover drugs at homes and related factors regarding this problem. METHOD: This descriptive study was performed among 692 non-medical personnel servicing at two military bases in December 2006. Data were collected by using a questionnaire, which had been developed by the investigators. Frequencies and percents were used as descriptive statistics. Chi-square test was used to compare the frequencies of leftover drugs according to certain variables. RESULTS: Of the total participants 78,8% were males, 72,8% aged between 18 to 39, and 29,6% were unmarried. The findings revealed that 61,3% of the participants had leftover drugs at their homes. Participants living with together 2 to 4 family members had higher frequencies of leftover drugs at homes. When we looked at the frequencies of leftover drugs according to drug use behaviors; the frequency of leftover drug was determined higher among those who stated; the recipe was not explained sufficiently, he did not use drugs as directed, he kept drugs until due time when did not use all of the drugs, he kept drugs in a box or bag, he visited a health center in order to have a recipe (p<0,05). CONCLUSION: It was determined leftover drugs were kept at nearly two third of the participants homes. Regarding incompleteness of treatment, the intoxication risk for children, and drug waste, this frequency of drug leftover was high, and all responsible professions in the chain of rationale drug use particularly physicians should be awaked on this issue. The use of drugs in a recipe should be explained to patients clearly. [TAF Prev Med Bull. 2009; 8(2): 113-118]
Thermoanalytical and Kinetic Study of Lubricating Lithium Greases
L.M.R. Lima,J.C.O. Santos,A.G. Souza
Journal of Engineering and Applied Sciences , 2012,
Abstract: The study of thermoanalytical and kinetic properties of lubricating lithium greases is of great importance to understand its behavior when submitted to different temperatures and atmospheres and as those conditions affect its performance. In the present research, thermal analyses and infrared spectroscopy of lubricating greases were accomplished to the lithium base. The lubricating greases were submitted to Thermogravimetry (TG) and Differencial Scanning Calorimetry (DSC) analysis.
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