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Sciensage

2013-Vol 4-Issue 2

Research Articles

SYNTHESIS AND EVALUTION OF ANTIBACTERIAL ACTIVITY OF SOME 2-AMINO/SUBSTITUTED AMINO-4-(PHENYL/p-CHLOROPHENYL) THIAZOLES

One of the first commercial synthetic drugs containing thiazole ring was sulphathiazole, a simple sulfamide antibiotic derived from 2-amino thiazole. Moreover, a large number of thiazole derivatives have been found to exhibit pharmacological activities. More specifically, thiabendazole is widely used as anthelmintic and fungicide. Dcngolinc is used as ingredient of herbicide. 3- substituted-4-amino thiazole-2-thione possesses antifugal activity. Moreover, ever large number of functional derivatives of thiazole exhibit interesting biological properties. These reports substantiated the importance of 2-amino -4- (phenyl/p-chlorophenyl) thaizole moiety. In the view of the above facts and wide spectrum of activity associated with thiosemicarbazide, thiadiazole, thiazolidinones, and pyrimidine diones, it was thought worthwhile to synthesize a series of 2-amino/substituted amino-4- (phenyl/p-chlorophenyl) thiazoles and their derivatives (Scheme-1) as possible anti bacterial agents. A series of 2-amino/substituted [thiosemicarbazide/2-(N-2’mercapto-1’,3’,4’-thiadiazol-5’-yl] amino-4- (phenyl/p-chlorophenyl) thaizole moieties were prepared. The structures of compounds have been established on the basis of their IR and ¹H NMR spectral data. All the synthesized compounds were evaluated for their antibacterial activity using gram (+) ve and gram (-) ve organisms. The following tests compounds 2a, 2b, 3a, 3b, 4b and 5b shows moderately active against gram +ve bacteria like SA and LB. Remaining compounds like 1a, 2a and 5b which are highly active against gram (+) ve organisms. The following compounds 1a, 1b, 2a, 2b, 3a, 3b, 4a, 4b, 5a and 5b shows moderately active against gram - ve organisms like EC, ST, PA and PB. Remaining compounds like 1a, 3b, 4a, 4b, 5a and 5b which are highly active gram - ve organisms. In the present study, we concluded that some of the synthesized compounds possessed highly antibacterial activity.

Chigarambatla Kistayya, N. G. Raghavendra Rao, B. Sanjeev Nayak, V.N.Sonar

Jyothishmathi Institute of Pharmaceutical Science, Thimmapur, Karimnagar , AP. India

CLINICALLY SIGNIFICANT DRUG-DRUG INTERACTIONS AND THEIR ASSOCIATION WITH POLYPHARMACY IN ELDERLY PATIENTS

To identify the potential drug drug interactions of clinical significance and assess its relation with polypharmacy, the prospective observational study was conducted to identify drug-drug interactions according to severity and to show the relation between number of prescribed medications and actual DDIs in elderly patients in a tertiary care teaching hospital. Micromedex Healthcare Series 2.0. was used to identify actual and potential DDIs. Drug therapy details by medication chart review and clinical review of 120 elderly inpatients (52% male and 48% female) was carried out and analyzed for incidence of any actual and potential drug-drug interactions. Polypharmacy was observed in almost all cases, wherein 45% were prescribed 11-15 drugs and 32% patients were with 6-10 drugs per prescription. 256 no. of DDIs were encountered in the study, comprising of 32 actual and 224 potential DDIs. As per severity, 34.37% were major and 65.62% were moderate. Multiple object drug and precipitant drugs were involved in actual and potential DDIs. Most common outcome of these actual DDIs was found to be increased blood pressure and blood sugar level, electrolyte and fluid imbalance, decreased diuretic effect of drugs. Elderly patients taking multiple medications concurrently because of their comorbid and multimorbid health conditions have lead to polypharmacy. The actual and potential DDIs increase as per number of drugs in prescription.The management of clinically relevant DDIs can be improved by clinical pharmacist interventions. Advice on withdrawal or substituting the precipitant drug would be beneficial.

Asawari Raut, Atmaram Pawar*, Arundhati Diwan, Govind Naruka, Chetan Sonar

Dept. of Clinical Pharmacy, Bharati Vidyapeeth Deemed University, Poona College of Pharmacy, Pune, Maharashtra, India

RESPONSE SURFACE METHODOLOGICAL OPTIMIZATION OF THE MEDIUM COMPONENTS FOR PRODUCTION OF XYLANASE UNDER SSF BY ASPERGILLUS FUMIGATUS

Response surface methodology was employed for the optimization of various medium components for the production of xylanase by Aspergillus fumigatus in solid state fermentation. The medium components influencing the enzyme production were screeened using Plackett-Burman design. Among the twelve independent variables screened by using Plackett-Burman design, only four variables FeSO4.7H2O, Yeast extract, KH2PO4 and CoSO4 were found to be significantly affecting variable for xylanase production. For obtaining the mutual interaction between the four variables and optimizing these variables, a 23 factorial central composite design (CCD) using response surface methodology was employed. The optimal values of four variables obtained for maximal production of xylanase were: FeSO4.7H2O - 8.0817 mg/gds, yeast extract - 35.057 mg/gds, KH2PO4 - 21.700 mg/gds and CoSO4 – 3.1717 mg/gds with a predicted xylanase activity of 354.33 IU/gds. These predicted optimal parameters were tested by carrying out the three repeated batch experiments in the laboratory and the maximum xylanase activity (355 IU/gds) obtained was close to the predicted value. A poor quantity of carboxy methyl cellulase activity was also obtained in all the experimental runs.

Vimalashanmugam Kanagasabai*, Viruthagiri Thangavelu

Bio-Process Laboratory, Department of Chemical Engineering, Annamalai University, Annamalai Nagar, TamilNadu, India

IMPACT OF REGIONAL VARIATION ON LUPEOL CONTENT IN CARISSA CARANDAS LINN. FRUITS: EVALUATION USING VALIDATED HIGH PERFORMANCE THIN LAYER CHROMATOGRAPHY

The present work is an attempt to evaluate the impact of regional variation on lupeol content in Carissa carandas Linn. fruits collected from different geographical regions of India using a validated HPTLC method. Chromatographic separation was achieved on TLC plates pre-coated with silica gel 60 F254 using toluene: methanol (8:1, v/v) as a mobile phase. Detection of lupeol was carried out by derivatizing the plates with 10 % methanolic sulphuric acid reagent followed by its densitometric scanning using CAMAG TLC scanner 4 at 366 nm. The method was validated as per ICH guidelines. Statistical analysis reveals that, the content of lupeol in different geographical region varied significantly.

Sunita Shailajan*, Neelam Sayed, Bhavesh Tiwari

Herbal Research Lab, Ramnarain Ruia College, Matunga, Mumbai, India

β-CYCLODEXTRIN MODIFIED CARBON PASTE ELECTRODE FOR THE DETERMINATION OF GEMIFLOXACIN AND NADIFLOXACIN

The electrochemical behavior of Gemifloxacin and Nadifloxacin at β-Cyclodextrin modified carbon paste electrode has been studied. Compared with carbon paste electrode, the β-Cyclodextrin modified carbon paste electrode exhibited a marked enhancement of current response of Gemifloxacin and Nadifloxacin. A simple, precise, inexpensive and sensitive voltammetric method has been developed for the determination of the cited drugs. Cyclic Voltametry studies in Britton Robinson buffer indicate that the process was irreversible and diffusion controlled with some adsorption character. Differential pulse voltammetry (DPV) was used to determine Gemifloxacin and Nadifloxacin in the pure form. The adsorptive stripping response was evaluated as a function of some variables such as pH, the scan rate and accumulation time. The peak current varied linearly for GF and NF in the following range: 5.0x10-8 to 2.0x10-7 mol l-1. The limits of detection (LOD) were 1.2x10-8, 1.0x10-8 mol l-1, while the limits of quantification (LOQ) were 4.3x10-8, 3.3x10-8 mol l-1 for Gemifloxacin and Nadifloxacin, respectively. The percentage recoveries were found in the following ranges: 99.57-100.36% and 99.85-100.64% for normal and differential pulse voltammetry, respectively. The relative standard deviations were found in the following ranges: 0.426-0.828% and 0.316-0.937% in case of GF and NF, respectively.

Manal A. El-Shal*, Ali K. Attia and Shabaan A. Abdulla

National Organization for Drug Control and Research (NODCAR), P. O. B 29 Cairo, Egypt

THEORETICAL STUDY USING DFT CALCULATIONS ON INHIBITORY ACTION OF SOME PYRAZOLE DERIVATIVES ON STEEL

The inhibition activity of two pyrazole derivatives, namely 1-{[benzyl-(2-cyano-ethyl)amino]methyl}-5-methyl-1H-pyrazole-3-carboxylic acid methyl ester (P1) and 1-{[benzyl-(2-cyano-ethyl)amino] methyl}-5-methyl-1H-pyrazole-3-carboxylic acid ethyl ester (P2) has been performed using density functional theory (DFT) at the B3LYP/6-31G(d,P) basis set level in order to elucidate the different inhibition efficiencies and reactive sites of these compounds as corrosion inhibitors. The calculated structural parameters correlated to the inhibition efficiency are the frontier molecular orbital energies EHOMO (highest occupied molecular orbital energy), ELUMO (lowest unoccupied molecular orbital energy), energy gap (ΔE), dipole moment (μ), hardness (η), softness (S), the absolute electronegativity (χ), the electrophilicity index (ω) and the fractions of electrons transferred (ΔN) from pyrazole molecules to iron. The local reactivity has been analyzed through the condensed Fukui function and condensed softness indices using population analysis. The calculated % IE was found to be in agreement with experimental corrosion inhibition efficiencies.

P.Udhayakalaa*, T.V. Rajendiranb, S. Gunasekaranc

Department of Chemistry, Dr.M.G.R. Educational and Research Institute, Chennai, India

EVALUATION OF ANTI DIABETIC ACTIVITY OF CARICA PAPAYA SEEDS ON STREPTOZOTOCIN- INDUCED TYPE-II DIABETIC RATS

A crude extract of Carica papaya seeds was prepared in boiling water and the aqueous extract was dried. At a dose of 100 mg/kg, 200mg/kg the extract was given to Male Sprague- Dawley rats for 14 days to evaluate the anti hyperglycemic and anti hyperlipidaemic activity in Streptozotocin - Nicotinamide induced diabetic rats. Glibenclamide was used as a standard drug. The blood glucose levels were determined at different times by glucose oxidase method. Serum Glutamate Oxaloacetate Transaminase (SGOT), Serum Glutamate Pyruvate Transaminase (SGPT) levels and lipid profile was also determined. Dosage of 100mg/kg and 200mg/kg of the extract significantly (P<0.001, P< 0.01) decreased blood glucose levels and the decrease was found to be dose dependent. SGOT, SGPT levels were decreased (P<0.01, P<0.05). Lipid profile was also decreased significantly (P<0.01, P<0.05). In the present study the anti hyperglycemic potential of Carica papaya was demonstrated in rats. It also has beneficial effects in diabetes associated complications.

Venkateshwarlu E*, Dileep P, Rakesh Kumar Reddy P, Sandhya P

Department of Pharmacology, Vaagdevi College of Pharmacy, Hanamkonda, Andhra Pradesh, India

IONIC LIQUID ASSISTED GREEN SYNTHESIS OF 2-PHENYLIMIDIZO [4,5-F][1,10]- PHENANATHROLINE AT ROOM TEMPERATURE

A range of 2-phenylimidazo [4,5-f] [1,10]-phenanthroline have been synthesized in very good yield under solvent-free conditions by grinding 1,10,phenanthroline-5dione,aromatic aldehydes and ammonium acetate in the presence of [HBim]BF4 as catalyst. The short reaction time, clean reaction, and easy workup make this protocol practically economical attractive and efficient.

Arshia Parveen

Department of Chemistry B. Raghunath College, Parbhani, India

Short Communications

EXTRACTION OF NATURAL DYE (XANTHOPHYLL) FROM MARIGOLD FLOWER

Marigold flower [Tagetes erecta L.], a major source of carotenoids and Lutin, is grown as a cut flower and in addition being grown for its medicinal values. Marigold flowers [Tagetes], which are yellow to orange red in colour, are a rich source of lutein, a carotenoid pigment. Nowadays, Lutein is becoming an increasingly popular active ingredient used in the Food Industry and Textile coloration.This pigment has acquired greater significance because of its excellent colour value. Although marigold flower extract has been used in veterinary feeds, the potential use of marigold as a natural textile colorant has not been exploited to its full extent. This is due to the lack of information on its safety, stability, and compatibility in textile coloration. In this study, an experiment was conducted to study the use of an extract isolated from marigold as a natural dye. The dye potential of the extract was evaluated by dyeing, using the flower, in 100 % cotton fabrics under normal dyeing conditions. Studies of the dye concentration and pH were undertaken. The surface colour was not affected by washing, and the quality of the flower was maintained even washing at 60˚C for 30 minutes. Studies have indicated that the change of some of the colors have been noticed after washing with soap. These findings reveal that the extract of marigold flower can be used for coloration of 100 % cotton, silk, and wool fabrics. This article deals with the chemistry, processing, and stability of the pigment and its applications in textile coloration and medicinal values.

Kannadasan T., Gnanaprakasam A., Harikrishnan R.*, Nganyei konyak, Rajkumar A.

Department of Chemical Engineering, Coimbatore Institute of Technology, Coimbatore, India


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