An Alternative Approach to Isoganciclovir: A Prominent Impurity in the Antiviral Drug Ganciclovir.

A simple and efficient process for the preparation of (±)-9-[(2,3-dihydroxypropoxy)methyl]guanine (isoganciclovir) is described. The synthesis features the preparation of a kinetically and thermodynamically controlled acyclic side chain using masked glycerol and methoxymethyl acetate. The unwanted regioisomers were separated through selective crystallization, which upon deprotection yielded isoganciclovir in good yield.

Synthesis and Characterization of Impurities in the Production Process of Lopinavir.

Lopinavir is an antiretroviral drug used for the inhibition of HIV protease. Four related substances of lopinavir were observed during the manufacturing process of lopinavir in the laboratory and they were identified. The present work describes the origin, synthesis, characterization, and control of these related substances.

Prediabetes and Alzheimer's Disease.

Aging patients with diabetes are at higher risk of developing Alzheimer's disease. Emerging evidences demonstrate the role of brain insulin resistance, which is a key mediator in prediabetes and diabetes mellitus that may lead to Alzheimer's disease. Insulin and insulin-like growth factors regulate many biological processes such as axonal growth, protein synthesis, cell growth, gene expression, proliferation, differentiation, and development.

Toxicity and tolerance of aluminum in plants: tailoring plants to suit to acid soils.

Aluminum (Al) stress is one of the serious limiting factors in plant productivity in acidic soils, which constitute about 50 % of the world's potentially arable lands and causes anywhere between 25 and 80 % of yield losses depending upon the species. The mechanism of Al toxicity and tolerance has been examined in plants, which is vital for crop improvement and enhanced food production in the future. Two mechanisms that facilitate Al tolerance in plants are Al exclusion from the roots and the ability to tolerate Al in the symplast or both.

Redescription and morphometric analysis of Paramazocraes thrissocles Tripathi, 1959 and P. setipinna Zhang & Ding in Zhang, Yang & Liu, 2001 (Monogenea: Mazocraeidae) infecting clupeoid fishes off Visakhapatnam coast, Bay of Bengal.

Two species of the mazocraeid monogenean genus Paramazocraes Tripathi, 1959 are redescribed based on specimens collected from the gills of clupeoid fishes off the Visakhapatnam coast, Bay Bengal: Paramazocraes thrissocles Tripathi, 1959 from Thryssa mystax (Bloch & Schneider), T. setirostris (Broussonet), T. malabarica (Bloch) and Paramazocraes setipinna Zhang & Ding in Zhang, Yang & Liu, 2001 from Setipinna taty (Valenciennes).

Molecular docking based screening of G6PS with 1, 5 Benzothiazepine derivates for a potential inhibitor.

Glucosamine-6-phosphate synthase (G6PS) (EC 2.6.1.

Nutrient composition and antioxidant activity of gonads of sea urchin Stomopneustes variolaris.

The study investigated, for the first time, proximate nutritional composition and antioxidant activity of gonads from the sea urchin, Stomopneustes variolaris, inhabiting the coastal area of Visakhapatnam (India). Moisture, ash, proteins, lipids and carbohydrate content were 77.53%±0.

MicroBlaze implementation of GPS/INS integrated system on Virtex-6 FPGA.

The emphasis of this paper is on MicroBlaze implementation of GPS/INS integrated system on Virtex-6 field programmable gate array (FPGA). Issues related to accuracy of position, resource usage of FPGA in terms of slices, DSP48, block random access memory, computation time, latency and power consumption are presented. An improved design of a loosely coupled GPS/INS integrated system is described in this paper.

New Validated Stability-Indicating Rp-HPLC Method for Simultaneous Estimation of Atorvastatin and Ezetimibe in Human Plasma by Using PDA Detector.

Purpose: This paper describes a simple, precise and accurate RP-HPLC method for simultaneous estimation of atorvastatin and ezetimibe in plasma.

Methods: The chromatographic separation of the drugs were performed on an X-Terra C8 (4.6 x 150 mm, 3.

Synthesis, Characterization, and Biological Activities of Pendant Arm-Pyridyltetrazole Copper(II) Complexes: DNA Binding/Cleavage Activity and Cytotoxic Studies.

2-(1H-Tetrazol-5-yl)pyridine (L) has been reacted separately with Me2NCH2CH2Cl⋅HCl and ClCH2CH2OH to yield two regioisomers in each case, N,N-dimethyl-2-[5-(pyridin-2-yl)-1H-tetrazol-1-yl]ethanamine (L1)/N,N-dimethyl-2-[5-(pyridin-2-yl)-2H-tetrazol-2-yl]ethanamine (L2) and 2-[5-(pyridin-2-yl)-1H-tetrazol-1-yl]ethanol (L3)/2-[5-(pyridin-2-yl)-2H-tetrazol-2-yl]ethanol (L4), respectively. These ligands, L1-L4, have been coordinated with CuCl2 ⋅H2O in 1 : 1 composition to furnish the corresponding complexes 1-4. EPR Spectra of Cu complexes 1 and 3 were characteristic of square planar geometry, with nuclear hyperfine spin 3/2.

Assessment of phytochemicals and antioxidant activities of raw and germinating Ceiba pentandra (kapok) seeds.

To determine the significance of germination on phytochemical constituents and non-enzymatic antioxidant activities of Ceiba pentandra seed extracts. Phytochemicals and antioxidant activities of raw and germinating seeds of Ceiba pentandra were estimated by different methods. The levels of phytochemical constituents were influenced by germination and increased except alkaloids and tannins, which were decreased significantly during germination.

A pH-triggered delayed-release chronotherapeutic drug delivery system of aceclofenac for effective management of early morning symptoms of rheumatoid arthritis.

Context: Rheumatoid arthritis (RA) is differentiated as an early morning exacerbation of the core arthritis condition associated with increase in pain and stiffness in joints and necessitate for medication.

Objective: The aim of the present work was to develop and optimise a pH-triggered delayed-release colon-specific aceclofenac microspheres and to accomplish chronotherapy of RA.

Methods: A 3-factor, 3-level Box-Behnken design (BBD) was used to optimise selected variables.

Should Governments engage health insurance intermediaries? A comparison of benefits with and without insurance intermediary in a large tax funded community health insurance scheme in the Indian state of Andhra Pradesh.

Background: A peculiar phenomenon of engaging insurance intermediaries for government funded health insurance schemes for the poor, not usually found globally, is gaining ground in India. Rajiv Aarogyasri Scheme launched in the Indian state of Andhra Pradesh, is first largest tax funded community health insurance scheme in the country covering more than 20 million poor families. Aarogyasri Health Care Trust (trust), the scheme administrator, transfers funds to hospitals through two routes one, directly and the other through an insurance intermediary.

Molecular docking based screening of novel designed chalcone series of compounds for their anti-cancer activity targeting EGFR kinase domain.

Epidermal growth factor receptors (EGFR) are critical for the growth of many tumors and expressed at high levels in about one third of epithelial cancers. Hence, blockade of the binding sites for EGFR has been hypothesized as an effective anti-cancer therapy. Chalcone derivative compounds have been shown to be highly effective anti-cancer agents, however there are still so many novel derivatives possible, one of which might get us the best targeted EGFR inhibitor.

Re-engineering nalidixic acid's chemical scaffold: A step towards the development of novel anti-tubercular and anti-bacterial leads for resistant pathogens.

Occurrence of antibacterial and antimycobacterial resistance stimulated a thrust to discover new drugs for infectious diseases. Herein we report the work on re-engineering nalidixic acid's chemical scaffold for newer leads. Stepwise clubbing of quinoxaline, 1,2,4-triazole/1,3,4-oxadiazole with nalidixic acid yielded better compounds.

Quality-by-design-based ultra high performance liquid chromatography related substances method development by establishing the proficient design space for sumatriptan and naproxen combination.

Quality-by-design-based methods hold greater level of confidence for variations and greater success in method transfer. A quality-by-design-based ultra high performance liquid chromatography method was developed for the simultaneous assay of sumatriptan and naproxen along with their related substances. The first screening was performed by fractional factorial design comprising 44 experiments for reversed-phase stationary phases, pH, and organic modifiers.

Oral administration of geraniol ameliorates acute experimental murine colitis by inhibiting pro-inflammatory cytokines and NF-κB signaling.

Ulcerative colitis is associated with a considerable reduction in the quality of life of patients. The use of phyto-ingredients is becoming an increasingly attractive approach for the management of colitis. Geraniol is a monoterpene with anti-inflammatory and antioxidative properties.

Phytochemical Evaluation of Roots of Polygonum viscosum Buch-ham.

Phytochemical evaluation of the chloroform extract of roots of Polygonum viscosum has yielded six compounds, stigmasterol, 7,4-dimethylquercetin, kaempferol, quercetin, myricetin and scutellarein. Among the six compounds isolated and characterized by chemical and spectral (UV, NMR and Mass) analysis in the present phytochemical evaluation, stigmasterol was not reported earlier from P. viscosum.

Formulation and Evaluation of Cefixime Trihydrate Matrix Tablets Using HPMC, Sodium CMC, Ethyl Cellulose.

The objective of the present work is to design sustained release matrix tablets of cefixime trihydrate by incorporating drug in a matrix made up of release retardant polymers, which prolong drug release leading to minimization of the peak and valley effect in the plasma and provide patient convenience. The effect of combination of polymers on parameters like release pattern, release mechanism of the drug were studied. Total nine formulations each containing 200 mg of drug were prepared by direct compression method.

Formulation and Characterization of Pyrazinamide Polymeric Nanoparticles for Pulmonary Tuberculosis: Efficiency for Alveolar Macrophage Targeting.

Pyrazinamide, a highly specific agent against Mycobacterium tuberculosis is used as first-line drug to treat tuberculosis. The current work aims to formulate polymeric nanoparticles based drug delivery system to sustain the release profile and reduce the dosing frequency of pyrazinamide. Further aim was to target the macrophages within body fluid.

Spectroscopic studies (FT-IR, FT-Raman, UV-Visible), normal co-ordinate analysis, first-order hyperpolarizability and HOMO, LUMO studies of 3,4-dichlorobenzophenone by using Density Functional Methods.

The vibrational frequencies of 3,4-dichlorobenzophenone (DCLBP) were obtained from the FT-IR and Raman spectral data, and evaluated based on the Density Functional Theory using the standard method B3LYP with 6-311+G(d,p) as the basis set. On the basis of potential energy distribution together with the normal-co-ordinate analysis and following the scaled quantum mechanical force methodology, the assignments for the various frequencies were described. The values of the electric dipole moment (μ) and the first-order hyperpolarizability (β) of the molecule were computed.

Formulation and optimization of gastric floating drug delivery system using Central composite design and its biopharmaceutical evaluation.

The present work investigates the formulation and biopharmaceutical estimation of gastric floating drug delivery system (GFDDS) of propranolol HCl using semi-synthetic polymer carboxymethyl ethyl cellulose (CMEC) and a synthetic polymer polyethylene oxide (PEO). A central composite design was applied for optimization of polymer quantity (CMEC or PEO) and sodium bicarbonate concentration as independent variables. The dependent variables evaluated were: % of drug release at 1 hr (D1hr), % drug release at 3 hr (D3hr) and time taken for 95% of drug release (t95).

Formulation development and systematic optimization of stabilized ziprasidone hydrochloride capsules devoid of any food effect.

Context And Objective: The objective of the study was to develop a stable capsule formulation of ziprasidone hydrochloride which can be administered without regards to food intake.

Materials And Methods: The unstable anhydrous form of ziprasidone hydrochloride was stabilized employing hot-melt extrusion and further optimized by 3 central composite design. The formulation was optimized after establishing acceptable ranges for response variables like disintegration time, dissolution and impurity profile.

Association of Climatic Variability, Vector Population and Malarial Disease in District of Visakhapatnam, India: A Modeling and Prediction Analysis.

Background: Malarial incidence, severity, dynamics and distribution of malaria are strongly determined by climatic factors, i.e., temperature, precipitation, and relative humidity.

Novel LC- ESI-MS/MS method for desvenlafaxine estimation human plasma: application to pharmacokinetic study.

A simple, sensitive and specific liquid chromatography tandem mass spectrometry (LC-ESI-MS/MS) method was developed for the quantification of desvenlafaxine in human plasma using desvenlafaxine d6 as an internal standard (IS). Chromatographic separation was performed using a Thermo-BDS hypersil C8 column (50 × 4.6 mm, 3 µm) with an isocratic mobile phase composed of 5 mM ammonium acetate buffer: methanol (20:80, v/v), at a flow rate of 0.