Synthesis, preclinical evaluation and antidepressant activity of 5-substituted phenyl-3-(thiophen-2-yl)-4, 5-dihydro-1H-pyrazole-1-carbothioamides

A series of phenyl-3-(thiophen-2-yl)-4, 5-dihydro-1H-pyrazole-1-carbothioamides (TTa-TTg) were synthesized by the ring closure reaction of phenyl-1-(thiophen-2-yl) prop-2-en-1-ones with thiosemicarbazide in alcoholic basic medium. All the final derivatives were evaluated for their antidepressant and neurotoxicity screening. The structures of the compounds were characterized by IR, 1H NMR, 13C NMR, Mass and elemental analyses. Preclinical evaluation of the compounds were ascertained by in silico toxicity, blood-brain barrier and human oral absorption prediction. In this series, 5-(4-hydroxyphenyl)-3-(thiophen- 2-yl)-4,5-dihydro-1H-pyrazole-1 carbothioamide (TTg) reduced immobility time 61.17 and 62.05 % in both force swimming and tail suspension test respectively at 10 mg/kg dose level when compared to the standard Imipramine without influencing the baseline locomotion. Moreover it was observed that the titled scaffold possessing electron withdrawing chlorine atom in the 4th position of aromatic ring of the scaffold also showed good the antidepressant activity. In conclusion, the behavioural investigation revealed that thiophene based pyrazolines having a carbothioamide tail unit in the N1 position may be therapeutically useful as potential antidepressant medications

A checking method for probabilistic seismic-hazard assessment: case studies on three cities

The conventional Cornell's source-based approach of probabilistic seismic-hazard assessment (PSHA) has been employed all around the world, whilst many studies often rely on the use of computer packages such as FRISK (McGuire FRISK-a computer program for seismic risk analysis. Open-File Report 78-1007, United States Geological Survey, Department of Interior, Washington 1978) and SEISRISK III (Bender and Perkins SEISRISK III-a computer program for seismic hazard estimation, Bulletin 1772. United States Geological Survey, Department of Interior, Washington 1987). A "black-box" syndrome may be resulted if the user of the software does not have another simple and robust PSHA method that can be used to make comparisons. An alternative method for PSHA, namely direct amplitude-based (DAB) approach, has been developed as a heuristic and efficient method enabling users to undertake their own sanity checks on outputs from computer packages. This paper experiments the application of the DAB approach for three cities in China, Iran, and India, respectively, and compares with documented results computed by the source-based approach. Several insights regarding the procedure of conducting PSHA have also been obtained, which could be useful for future seismic-hazard studies. © 2010 The Author(s).published_or_final_versionSpringer Open Choice, 21 Feb 201

A statistical analysis of corpus based approach on learning sentence patterns

This research paper examines the adverse effect of theoretical explanation of the grammatical rules among the learners. Exploration of the methods and materials taught inductively or deductively is the panacea to achieve the required goal. The study throws light on the pedagogical implication of adopting appropriate methods and materials for building the learners’ grammar and language. It primarily intends to explore a new teaching method using language corpora that can be employed in the English grammar classes in colleges at the undergraduate level. It strives to evaluate the effectiveness of teaching sentence patterns through corpus based activities comparing with the traditional based teaching. Thus the methodology aims to encourage students to become independent corpus users

Landslide Inventory along newly Constructed Ghat road secetion at Vathalmalai Hills, Tamil Nadu, India

The study aims to conduct landslide inventory and calculate the area and volume of landslide material from the geometrical measurements of landslides occurred at Vathalmalai hills, Dharmapuri district, Tamil Nadu, The study area located in a semi tropical region, India. Empirical relationship was derived between volume estimation and other parameters through the Person correlation coefficient model. Field data were collected through extensive field surveys and using the satellite data. The correlation between the area under landslide and volume of landslide material was studied using different curve estimation models. Various statistical parameters were calculated to relate the models with each other. Among various results, the power of law matches the records better. While, next to power law fit compound, growth and Exponential show high R2 value and low F statistic and less RMSE value. The correlation between area and volume of landslides determined V=0.492A1.224 for 10 landslide locations of the slide area in Vathalmalai. The landslide modeling shows that high R2 value in power law from 0.90, while it decreased as 0.83 in compound, growth and exponential. It significantly low in inverse model (0.48). According to the suggested relation, the mean of the average depth of landslides was assessed as 1.839 m which was near to mean of actual depth of 2.0 m

COMBINED EFFECT OF SELECTIVE BIOACTIVE COMPOUNDS FROM PLANT ORIGIN IN AN ANIMAL MODEL OF ANXIETY

Objective: Evidence is emerging that specific combinations of bioactive compounds may be far more effective in protecting against several diseases as compared to the effect of a single compound. The present study was aimed to investigate the interactive effect of Diosgenin and Silymarin, the bioactive compounds from plant origin in an animal model of anxiety. Methods: Albino wistar rats of either sex were divided into five groups and treated for 5 d. Group I and II served as control and standard and test groups were treated with Diosgenin (100 mg/kg, p. o.), Silymarin (100 mg/kg, p. o.) and combination of Diosgenin (50 mg/kg, p. o.)+Silymarin (50 mg/kg, p. o.), respectively. Diazepam (1 mg/kg, i. p.) was used as a standard for the study. Anxiolytic effects were studied in the Elevated plus-maze, Hole-board test and Light/Dark model. Results: The results suggested that Diosgenin when given alone at a dose of 100 mg/kg, does not shown significant anxiolytic effect when as compared with control. Whereas, the compound Silymarin (100 mg/kg) shown significant anti-anxiety effect (P<0.01), independently. The same two bioactive compounds, given in combination at a dose of 50 mg/kg, (each), exhibited significant anxiolytic-like effect, potentially. Conclusion: It can be concluded that Diosgenin has got a synergistic effect on anti-anxiety action when given in combination with Silymarin

SOLID DISPERSION TECHNIQUE TO ENHANCE THE SOLUBILITY AND DISSOLUTION OF FEBUXOSTAT AN BCS CLASS II DRUG

Objective: The present study was aimed to enhance the solubility of poorly water-soluble drug (BCS Class II) Febuxostat using water-soluble polymers.Methods: Pre-formulation studies like drug excipient compatibility studies by Fourier-transform infrared spectroscopyDifferential scanning calorimetry and determination of saturation solubility of drug individually in various media like distilled water and pH 7.4 phosphate buffer. Solid dispersions of Febuxostat was prepared using Polyethylene glycol (PEG 6000) (fusion method) and Polyvinyl pyrrolidone (PVP K30) (solvent evaporation method) in various ratios like 1:1, 1:2, 1:3 and 1:4 separately. The formulated solid dispersions were evaluated for percentage yield, drug content and in vitro dissolution studies.Results: From the results of pre-formulation studies it was revealed that there was no interaction between drug and excipients and the pure drug was poorly soluble in water. The percentage yield of all formulations was in the range of 54-78 %, and drug content was in the range of 43-78 mg. The solid dispersion containing polyvinylpyrrolidone K 30 in 1:4 ratio showed the highest amount of drug release at the end of 30 min than other formulations.Conclusion: Finally it was concluded that solid dispersion prepared with PVP K-30 in 1:4 ratio by solvent evaporation method was more soluble than by fusion method

Principles and Practices of Seismic Microzonation: Case Studies in India

This paper presents an overview of the principles and practices of seismic microzonation with some case studies in India. India has experienced major damages and loss of life due to earthquakes. Macrozonation map in Indian seismic code IS-1893 is frequently revised soon after a major earthquake in the country. New revision which was published in 2002 after Bhuj earthquake in 2001 contains four macro zones. These zones are based on geology and limited seismology input without considering geotechnical aspects such as site effects and liquefaction. In order to understand the earthquake vulnerability of major urban centers and prepare new zonation map, the Govt. of India has initiated microzonation of 63 cities in India after 2001 earthquake. Many microzonation studies are under progress and few of them have been completed. This paper presents an overview of these studies. Seismic microzonation of Jabalpur urban area is the first work in India towards seismic microzonation of Indian cities. Jabalpur study has provided many learning lessons to other studies. Preliminary microzonation of Delhi has been completed and detailed one is under progress. Seismic Hazard and Microzonation Atlas of the Sikkim Himalaya has been published with geological and seismological background. Microzonation of Guwahati was done based on geology, geomorphology, seismotectonics, soil characteristics, pre-dominant frequencies, peak ground acceleration, seismic hazard and demography. Seismic Microzonation of Dehradun has been prepared based on shear wave velocity with site response. First order Microzonation of Haldia has been developed based on peak ground acceleration, predominant frequency and elevation map. Different maps and results were presented for Gujarat microzonation based on noise survey and after shock data. None of these studies included the geotechnical aspects. The geotechnical aspects were fully incorporated in the recently completed Microzonation work of Bangalore and the ongoing study of Chennai microzonation. An overview of seismic microzonation studies in India is presented in this paper

Comparative study on the antimicrobial activities of three Indian medicinal plants

Aqueous, methanol and chloroform extracts from the leaves of Ficus religiosa, Thespesia populnea and Hibiscus tiliaceus were completely screened for antibacterial and antifungal activity. The chloroform extract of F. religiosa possessed a broad spectrum of antibacterial activity with a zone of inhibition of 10 to 21 mm at very low MIC values. The methanolicextracts possessed moderate antibacterial activity against a few bacterial strains. There was less antibacterial activity or none at all using aqueous extracts. The extracts of F. religiosa were found to be active against Aspergillus niger and Penicillium notatum. The extracts from theleaves exhibited considerable and variable inhibitory effects against most of the microorganisms tested

A REVIEW ON SUPRAMOLECULAR CHEMISTRY IN DRUG DESIGN AND FORMULATION RESEARCH

Supramolecular chemistry, other way called as intermolecular chemistry disclose the relationship of molecules with environment. It exploits while exposing the physicochemical phenomina that happens when two like or unlike molecules/ions/systems contact each other. Drug action involve the target recognition process and response triggered by the intermolecular complex of drug and target. Drug design therefore require in depth study of intermolecular forces that exist between drug and target. Formulation of the drug or Active Pharmaceutical Ingredient (API) is also regulated by these forces. Compatibility and incompatibility in formulations are nothing but of the effect of the intermolecular forces on physical behavior of systems. Therefore review of intermolecular chemistry in general and its role particularly in pharmaceutical research is presented here for the benefit of the students and research scholars who aspire to work on interdisciplinary projects in the field of pharmacy. Key words: intermolecular forces, hydrogen bond, drug design, active pharmaceutical ingredient (API), crystal