A Therapeutic Journey of 5-Pyrazolones as a Versatile Scaffold: A Review.

A sizeable proportion of currently marketed drugs come from heterocycles. The heterocyclic moiety 5-pyrazolone is well known five-membered ring containing nitrogen. Derivatives of this wonder nucleus have exhibited activities as diverse as antimicrobial, anti-inflammatory, analgesic, antidepressant, anticonvulsant, antidiabetic, antihyperlipidemic, antiviral, antitubercular, antioxidant, anticancer and antiviral, including action against severe acute respiratory syndrome (SARS) or 3C protease inhibitor.

1,3,5-Pyrazoline Derivatives in CNS Disorders: Synthesis, Biological Evaluation and Structural Insights through Molecular Docking.

Background: Anxiety and oxidative stress are the common disorders prevailing in the modern age. Many new pyrazoline derivatives have been synthesized and patented, but there is still continuous research in progress to explore antidepressant and antioxidant potential of pyrazoline scaffold.

Objectives: The present work was carried out to synthesize, characterize and evaluate the pharmacological potential of 1,3,5-Pyrazoline derivatives.

Synthesis, biological evaluation and molecular docking studies of novel 3,5-disubstituted 2,4-thiazolidinediones derivatives.

A series of thirteen novel 2,4-thiazolidinedione derivatives were synthesized through three step reaction procedure. The title compounds were synthesized by Knoevenagel condensation at the 5th position of the 2,4-thiazolidinedione ring. Various physicochemical and spectral studies were conducted to characterize the synthesized derivatives including- IR, Mass, H NMR, C NMR and elemental analysis.

Pectin, beta-cyclodextrin, chitosan and albumin based gastroprotective systems for piroxicam maleate: Synthesis, characterization and biological evaluation.

In order to optimize drug action, new drug formulations have been developed based upon the prodrug approach. This study was inspired by the increasing interest in the field of macromolecular prodrugs and Piroxicam maleate was used as a model drug. A total of five prodrugs were synthesized using beta cyclodextrin, chitosan, pectin, egg albumin, bovine serum albumin.

A randomized controlled clinical trial evaluating the efficacy of zoledronate gel as a local drug delivery system in the treatment of chronic periodontitis: A clinical and radiological correlation.

Background: This study aimed to evaluate the efficacy of local drug delivery system of zoledronate (ZLN) gel as an adjunct to scaling and root planing (SRP) for the treatment of human periodontal intrabony defects clinically and radiographically.

Materials And Methods: Forty intrabony defects (three walled and combined defects without involving furcation) in moderate to severely affected forty chronic periodontitis patients (range, 30-50 years) were randomly divided into two groups and treated either with 0.05% ZLN gel (ZLN = 20; 1 dropout) or placebo gel (control group [CG] = 20) after SRP.

Urate crystal degradation for treatment of gout: a nanoparticulate combination therapy approach.

The objective of the present work was to develop polymeric nanoparticles of uricase and aceclofenac (NSAID) and to incorporate them into gel, for delivering drugs to synovial joints, for effective treatment of Gout. Nanoparticles containing uricase and aceclofenac were prepared by double emulsion solvent evaporation method and emulsion solvent evaporation, using PLGA (50:50) as carrier, respectively. Process parameters were optimized using Taguchi L4 orthogonal array and L9 array, respectively.

Development of cellulosic polymer based gel of novel ternary mixture of miconazole nitrate for buccal delivery.

Aim of the present investigation was to develop cellulosic polymer based mucoadhesive antifungal gel comprising novel ternary mixture of miconazole nitrate (MN) for buccal delivery. Crosslinking of gel was made by adjusting pH with triethanolamine (TEA) and gel formulation was optimized on the basis of flux of MN (0.562-1.

Hydrogels: a journey from diapers to gene delivery.

Hydrogels are the biomaterials comprising network of natural or synthetic polymers capable of absorbing large amount of water. Hydrogels are "Smart Gels" or "Intelligent Gels" which can be made to respond to the various environmental conditions like temperature, pH, magnetic/electric field, ionic strength, inflammation, external stress etc. There are numerous potential applications of hydrogels in modern day life ranging from a diaper to gene delivery.

Bioavailability enhancers of herbal origin: an overview.

Recently, the use of herbal medicines has been increased all over the world due to their therapeutic effects and fewer adverse effects as compared to the modern medicines. However, many herbal drugs and herbal extracts despite of their impressive in-vitro findings demonstrates less or negligible in-vivo activity due to their poor lipid solubility or improper molecular size, resulting in poor absorption and hence poor bioavailability. Nowadays with the advancement in the technology, novel drug delivery systems open the door towards the development of enhancing bioavailability of herbal drug delivery systems.

Mimosa pudica L. (Laajvanti): An overview.

Mimosa pudica L. (Mimosaceae) also referred to as touch me not, live and die, shame plant and humble plant is a prostrate or semi-erect subshrub of tropical America and Australia, also found in India heavily armed with recurved thorns and having sensitive soft grey green leaflets that fold and droop at night or when touched and cooled. These unique bending movements have earned it a status of 'curiosity plant'.

Herbs-are they safe enough? an overview.

Drugs based on herbs have become a common form of therapy as well as for prophylaxis because they are often perceived as being natural and therefore harmless. Today they are one of the hottest trends and most sought after in the field of nutrition or herbal therapeutics. As the use of complementary medicine grows, so does the knowledge that many compounds in common use not only have a significant effect on the body but may also interact with pharmaceuticals and also with other alternative products.

Trichosanthes dioica Roxb.: An overview.

Trichosanthes, a genus of family Cucurbitaceae, is an annual or perennial herb distributed in tropical Asia and Australia. Pointed gourd (Trichosanthes dioica Roxb.) is known by a common name of parwal and is cultivated mainly as a vegetable.

Heavy metals and living systems: An overview.

Heavy metals are natural constituents of the earth's crust, but indiscriminate human activities have drastically altered their geochemical cycles and biochemical balance. This results in accumulation of metals in plant parts having secondary metabolites, which is responsible for a particular pharmacological activity. Prolonged exposure to heavy metals such as cadmium, copper, lead, nickel, and zinc can cause deleterious health effects in humans.

Parenteral drug delivery: a review.

The parenteral route of administration is the most effective route for the delivery of the active pharmaceutical substances with narrow therapeutic index, poor bioavailability especially for those drugs, prescribed to unconscious patients. To maintain a therapeutic effective concentration of the drug, it requires frequent injections which ultimately lead to patient discomfort. In parenteral drug delivery, major progress has been done in the field of formulation technologies so as to provide a targeted and sustained release of drug in predictable manner.

Soyabean powder as a novel diluent in tablet formulation of simvastatin.

The present research paper introduces soyabean nuggets powder, as a novel excipient with nutraceutical value for tablets containing cholesterol lowering drug, simvastatin. Experiments were carried out to evaluate the suitability of soyabean nuggets powder as a diluent by incorporating in tablet formulation of simvastatin. The formulation was compared with the marketed product to determine its relative efficacy.

Preparation and evaluation of sustained release microballoons of propranolol.

Background And The Purpose Of The Study: The purpose of the present investigation was to characterize, optimize and evaluate microballoons of Propranolol hydrochloride and to increase its boioavailability by increasing the retention time of the drug in the gastrointestinal tract.

Methods: Propranolol hydrochloride-loaded microballoons were prepared by the non-aqueous O/O emulsion solvent diffusion evaporation method using Eudragit RSPO as polymer. It was found that preparation temperature determined the formation of cavity inside the microballoon and this in turn determined the buoyancy.

Crocus sativus L.: A comprehensive review.

Crocus sativus L. belonging to the family Iridaceae (syn - kesar) comprises the dried red stigma and is widely cultivated in Iran and other countries such as India and Greece. Saffron contains more than 150 volatile and aroma-yielding compounds mainly terpenes, terpene alcohol, and their esters.

Pistia stratiotes (Jalkumbhi).

Pistia stratiotes (Family: Araceae) is commonly used in Ayurvedic medicine. This review article is a compilation of all the updated information on its phytochemical and pharmacological activities, which were performed by different methods. Studies indicate that P.

Fullerenes: from carbon to nanomedicine.

Fullerenes, the third carbon allotrope, have emerged as agents which could revolutionize the treatment of many diseases. Fullerenes possess different biological applications like neuroprotective agents, antioxidants, anti-HIV activity, enzyme inhibition, antiapoptotic activity and the list is ever increasing. Moreover, they are being utilized as drug carrier systems and also for many non-biological applications like superconductors, catalysis and so on.

Proton HR-MAS NMR spectroscopic characterization of metabolites in various human organ tissues: pancreas, brain and liver from trauma cases.

High-Resolution Magic Angle Spinning (HR-MAS) NMR has been employed to characterize various metabolites of human pancreas, liver and brain tissues from trauma cases. The potential usefulness of NMR in identifying the metabolites in human tissues has been explored using a combination of one- and two-dimensional experiments. The complete resonance assignments of pancreas tissue have been carried out for the first time.

QSAR study on pyridinone derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitor: a mixed approach.

HIV-1 reverse transcriptase inhibitory activity of a series of substituted pyridinone derivatives (non-nucleoside) was subjected to classical QSAR study by using mixed approach (Hansch and Free-Wilson). The study was carried out with indicator parameter encoding different group contributions and some physico chemical parameters namely hydrophobic (phi), electronic (sigma), steric (MR) and STERIMOL values of aromatic substitutents. The best generated models were validated by leave-one- out technique (LOO-internal validation) and predicting the activity of the test (external validation).

Influence of thermodynamic parameter in Lanosterol 14alpha-demethylase inhibitory activity as antifungal agents: a QSAR approach.

A quantitative structure activity relationship, Hansch approach was applied on twenty compounds of chromene derivatives as Lanosterol 14alpha-demethylase inhibitory activity against eight fungal organisms. Various physicochemical descriptors and reported minimum inhibitory concentration values of different fungal organisms were used as independent variables and dependent variable respectively. The best models for eight different fungal organisms were first validated by leave-one-out cross validation procedure.

QSAR study of 3-phenyl-5-acyloxymethyl-2H,5H-furan-2-ones as antifungal agents: the dominant role of electronic parameter.

To explore physicochemical properties of 3-phenyl-5-acyloxymethyl-2H,5H-furan-2-ones derivatives responsible for their antifungal activity, a quantitative structure activity relationship, Hansch approach was applied on sixteen compounds of above mentioned derivatives. Various physicochemical descriptors and reported minimum inhibitory concentration values of different fungal organisms were used as independent variables and dependent variable respectively. The best models for twelve different fungal organisms were first validated by leave-one-out cross validation procedure.