ABSTRACTThe complexes of Mn(II), Co(II), Ni(II), Cu(II) and Zn(II) with 3,4,5-trimethoxybenzoic acid have been synthesizedand characterized by elemental analysis and IR spectroscopy. The carboxylate groups bind as monodentate or bidentatechelating or bridging ligands. The metal complexes have also been tested in vitro for their antibacterial and anti-fungalactivity. The experimental results suggest that metal complex is more potent in anti-bacterial and anti-fungal activities.Keywords: 3,4,5-trimethoxybenzoates of Mn(II), Co(II), Ni(II), Cu(II) and Zn(II),thermal stability, IR spectroscopy, Antibacterialand Anti-fungal activities.

ABSTRACT A widely used antihistamine drug loratadine (2) and some of its amide derivatives (3, 4 & 5) have been synthesized for the interest of studying the biological activity-specially, for cytotoxicity by brine shrimp lethality bioassay. All of the synthesized compounds were characterized by the extensive use of IR, 1H-NMR, 13C-NMR & Mass spectral analysis and LD50 values have been determined to establish SAR of the series. The synthesized antihistamine drug loratadine (2) and its amide derivatives (3-5) showed noteworthy cytotoxic activity. Among the synthesized compounds, diethylamine derivative (3) showed least cytotoxic activity, whereas ethylenediamine derivative (4) and propylenediamine derivative (5) showed more cytotoxic activity than their precursor drug loratadine (2) with the propylenediamine derivative being the most toxic of all. From this investigation we concluded that increased presence of electronegative atoms, such as Oxygen (O), Nitrogen (N) etc. in a particular compound enhances its chance of being biologically more active. Keywords: Loratadine, Amides, Cytotoxicity, Structure-Activity Relationship.

ABSTRACT The present study was intended to screen the antipyretic activity of the methanol extract of Hypnea musciformis (Wulf.) Lamouroux collected from Manapad coast, Tamil Nadu, India on albino mice. Paracetamol (10mg/kg) was used as standard drug. The antipyretic activity of Hypnea musciformis (Wulf.) Lamouroux was determined by Brewer’s yeast induced pyrexia on albino mice. The various methanol extract doses used were 200mg/kg and 400mg/kg body weight of mice. 400mg/kg methanol extract of Hypnea musciformis (Wulf.) Lamouroux showed significant decrease in body temperature while 200mg/kg methanol extract showed less effect. 400mg/kg methanol extract exhibited closely significant (p<0.05) decrease in elevated body temperature as compared to standard drug. From the study it was concluded that the methanol crude extract of Hypnea musciformis (Wulf.) Lamouroux can be used for antipyretic activity. Keywords: Red seaweed, Hypnea musciformis, Methanol extract, Antipyretic

ABSTRACT Andrographis paniculata (King of bitters) is a plant that is native to south Asian countries such as India and Shrilanka. It is also known as Kalmegh. The leaf and underground stem are used to make medicine. Andrographis is frequently used to preventing and treating the common cold and flu (Influenza). Some people claim Andrographis stopped the 1919 flu epidemic in India, although this has not been proven. Andrographis is also used for a wide assortment of other conditions. It is used for digestive complaints including diarrhea, constipation, intestinal gas, colic and stomach pain. It also used for liver complaints including an enlargement of liver, jaundice and liver damage due to medications, for infections including leprosy, pneumonia, tuberculosis, gonorrhea, syphilis, malaria, cholera leptospirosis, rabies sinusitis and HIV/AIDS, and for skin complaints like wounds, ulcers and itchiness. Coleus forskohlii herb extract is derived from roots. Coleus is used in India folk medicines and is a traditional digestive remedy. Coleus forskohlii has been traditionally used to treat high blood pressure. Other benefits include help in losing weight by improving the breakdown of fats, improving digestion and nutrient absorption, lowering cholesterol and immune system support. It is also effective in skin problems as eczema and psoriasis. Lowers hypertensions, heart failure and angina. The active photochemical in Coleus forskohlii forskohlin, was discovered in 1974. So both the plants are very important and used in the treatment of various diseases. Keywords: Andrographis paniculata, Coleus forskohlii, Andrographolide, Medicinal potential.

ABSTRACT

More than half of all therapeutic agents consists of heterocyclic compounds. The heterocyclic ring system in many cases comprises the very core of the active moiety or pharmacophore. Hundreds of thousands of new heterocyclic compounds are prepared annually throughout the world, and many of them are entering into pharmacological screenings to determine if they have useful biological activity. This process of random screening is inefficient, but it has resulted in identification of new compounds not produced naturally or imagined by chemists. Such lead compounds form the basis of a series of analogues intended to optimize the therapeutic activity. The antitubercular drug, Ethambutol, was developed in this way. More recently emphasis has been placed on rational design of new pharmaceuticals.

Keywords: Heterocyclic compounds, Therapeutic activity, Biological activity.

ABSTRACT New pyrazolines were synthesized through cyclocondensation between chalcones derived from acetophenone and substituted benzaldehydes with furan-2-carboxylicacid hydrazide. Cyclocondensation reactions were carried out by refluxing glacial acetic acid solution of reactants with catalytic amount of PPA or subjecting the same reaction mixture to MWI. Both conditions yielded the same product with a similar yield of 65-70%. But refluxing conditions required 18 hours for the completion of the reaction whereas MWI required 1-2 min for the completion of reaction. Keywords: Pyrazoline, MWI (Microwave irradiation), PPA (Polyphosphoric acid)), Furan-2-carboxylicacid hydrazide.

A simple, accurate, economical and precise reverse phase high performance liquid chromatographic (RP-HPLC) method has been developed for the simultaneous determination of Fexofenadine and Montelukast. The separation was achieved on Intersil C 18 column (250 x 4.6 mm, 5 μm) as stationary phase with a mobile phase comprising of Orthophosphoric acid buffer pH(6.0):Acetonitrile: Methanol (30:50:20) in an isocratic mode, at a flow rate of 1 ml/min. The detection was monitored at 244 nm. The retention time of Fexofenadine and Montelukast were 2.65 min and 3.65 min respectively. The linearity was found to be in the range of 72-168 μg/ml and 6-14 μg/ml for Fexofenadine and Montelukast respectively with correlation coefficient of 0.999. The proposed method was validated according to ICH guidelines for parameters like linearity, accuracy, precision and specificity. All validation parameters were within the acceptable range. The developed method was successfully applied for the estimation of Fexofenadine and Montelukast in pure and pharmaceutical dosage form.

Keywords: Fexofenadine, Montelukast, RP-HPLC, Validation, Simultaneous estimation, ICH guidelines.

ABSTRACT Thiadiazole nucleus is found in natural and synthetic products of biological interest. A wide variety of biological and pharmacological properties are associated with thiadiazole nucleus. Various substituted thiadiazole have been reported to have a very wide range of biological activities, such as anti-inflammatory, anticonvulsant, antibacterial, antifilarial, antihelmintic activities etc. In view of proven potentiality of thiadiazole, it has been felt worthwhile to get then incorporated with the suitable pharmacophores by molecular conjunction method. Accordingly it has been planned to synthesize substituted thiadiazoles.2-cyano-3-phenyl-N-(5-phenyl-1,3,4-thiadiazol-2-yl)acryl amides with thiadiazole pharmacophore group is planned to be synthesized as they incorporate many interesting structural features associated with antibacterial activity. As physico-chemical properties influence the biological activity to a great extent, various ring substituted derivatives have been synthesized. Keywords: Thiadiazole, Biological activities, Anti-inflammatory, Anticonvulsant, Antibacterial.

ABSTRACT The present investigation regarding the viscometric measurements of 3-(2-hydroxy-3-nitro-5-methyl) phenyl-6-amino-1,2,5-thioxazine in 60% ethanol water mixture at various temperatures (240C, 280C, 320C and 360C)by keeping constant molar concentration 0.1 M . This investigation also includes the study of the solute –solvent interaction and effect of dilution of the solvent. The results obtained during this investigation gave detail information regarding to pharmocokinetics and pharmocodynamics of these drug. Keywords: Viscometric Measurements, 3-(2-hydroxy-3-nitro-5-methyl) phenyl-6-amino-1,2,5-thioxazine, ethanol-water mixture etc.

ABSTRACT To investigate the anti-inflammatory and antioxidant activity of 1,3- Dimethyl 2,6-Diphenyl piperidine 4-One Oxime. Anti-inflammatory activity was evaluated using the carrageenan induced rat paw oedema. After 12hrs fast rats were divided into five groups of six each. Each animal was marked for identification and regularly monitoring. Group I served as control group received carrageenan only. Group II, III and IV animals received 1,3- Dimethyl 2,6-Diphenyl piperidine 4-One Oxime at a dose of 100, 250 and 500 mg/kg orally. Group V was orally administered 2mg/kg (ip) Dexamethasone as a standard drug. In vitro Antioxidant activity like DPPH and superoxide radical scavenging activity were investigated by standard methods. Results of the present study indicates that higher dose of 1,3- Dimethyl 2,6-Diphenyl piperidine 4-One Oxime has potent anti-inflammatory activity close to standard drug. The above results confirmed that 1,3- Dimethyl 2,6-Diphenyl piperidine 4-One Oxime possess significant anti-inflammatory activity as compared to standard drug dexamethasone. The antioxidant activity of 1,3- Dimethyl 2,6-Diphenyl piperidine 4-One Oxime was concentration dependent and approximately comparable to commercial synthetic antioxidants as ascorbic acid. On the basis of the results of this study, it clearly indicates that 1,3- Dimethyl 2,6-Diphenyl piperidine 4-One Oxime had powerful anti-inflammatory and in vitro antioxidant activity. Keywords: Anti-inflammation, In vitro Antioxidant, 1,3- Dimethyl 2,6-Diphenyl piperidine 4-One Oxime.

A sensitive, robust and selective liquid chromatographic – tandem mass spectrometric method (LC-MS/MS) was
developed & validated for Efavirenz and Emtricitabine quantification in human EDTA plasma. Sample preparation was based
on solid phase extraction using mixture of methanol/ammonium acetate 5mM (80/20v/v) to extract the drug and internal
standard from plasma. Chromatography was performed on c18 analytical column, retention time were for Efavirenz,
Emtricitabine and IS was around 2.34min, 1.52min and 1.76min respectively. The ionization was optimized using ESI(+)
selectivity was achieved by tandem mass spectrometric analysis using MRM functions for Efavirenz, Emtricitabine &
Atenolol. Analytical curve ranged from 25 - 5000 ng/mL for Efavirenz and 20 - 4000 ng/mL for Emtricitabine. Inter day
precision and accuracy of the quality control samples were <15 % relative standard deviation (RSD), analyte stability during
sampling processing and storage were established. The developed and validated bioanalytical method for Efavirenz and
Emtricitabine drugs shows satisfactory linearity, precision, accuracy and stability. The practical extraction procedure based on
solid phase extraction technique for the specific drug used in the study provides a high and precise recovery from plasma. The
method can be particular useful for pharmacokinetics and pharmacodynamics.