Synthesis and biological evaluation of coumarin-thiazole hybrids as selective carbonic anhydrase IX and XII inhibitors.

A series of coumarin-linked thiazoles (6a-p) was synthesized and the synthesized compounds were evaluated against human carbonic anhydrases (hCAs) IX and XII, which have been implicated in cancer. All the compounds exhibited selective inhibition of both isoforms. The designed compounds inhibited hCA IX in a moderate nanomolar to submicromolar range.

Discovery of newer pyrazole derivatives with potential anti-tubercular activity via 3D-QSAR based pharmacophore modelling, virtual screening, molecular docking and molecular dynamics simulation studies.

Tuberculosis is one of the leading causes of death of at least one million people annually. The deadliest infectious disease has caused more than 120 million deaths in humans since 1882. The cell wall structure of Mycobacterium tuberculosis is important for survival in the host environment.

Preparation and Optimization of Leuprolide Acetate Nanoparticles Using Response Surface Methodology: and Evaluation.

This study aims to develop optimized leuprolide acetate (LA) nanoparticles (NPs) for intranasal delivery in the treatment of Alzheimer's disease. Box-Behnken Design was used to optimize LA polylactide--glycolic acid (PLGA) NPs. The independent variables chosen were PLGA concentration, surfactant concentration, and the ratio of water to oil phase, whereas the dependent variables were particle size and % entrapment efficiency.

New Drug Delivery Systems Developed for Brain Targeting.

The blood-brain barrier (BBB) and the blood-cerebrospinal fluid barrier (B) are two of the most complex and sophisticated concierges that defend the central nervous system (CNS) by numerous mechanisms. While they maintain the neuro-ecological homeostasis through the regulated entry of essential biomolecules, their conservative nature challenges the entry of most of the drugs intended for CNS delivery. Targeted delivery challenges for a diverse spectrum of therapeutic agents/drugs (non-small molecules, small molecules, gene-based therapeutics, protein and peptides, antibodies) are diverse and demand specialized delivery and disease-targeting strategies.

Solid dispersion technology as a formulation strategy for the fabrication of modified release dosage forms: A comprehensive review.

Solubility limited bioavailability is one of the crucial parameters that affect the formulation development of the new chemical entities. Thus the major constraint in the pharmaceutical product development is the suitable solubility enhancement technique for Active Pharmaceutical Ingredient. Solid dispersion (SD) is an established and preferred method for improving the solubility which ultimately may be helpful to enhance bioavailability.

Insights into the structural requirements of triazole derivatives as promising DPP IV inhibitors: computational investigations.

Diabetes is one of the leading causes of death globally as per World Health Organization 2019. To cope up with side effects of current diabetes therapy, researchers have found several novel targets for the treatment of diabetes. Currently, dipeptidyl peptidase IV (DPP IV) has emerged as a target in modulating the diabetes physiology.

Bacterial Nanocellulose based Wound Dressings: Current and Future Prospects.

Although there are many treatment options available for wound and burns dressings, improvements in technology are still required. Bacterial cellulose is a polymer derived from the microbiological world and has shown some promising properties that recommend it as a wound healing therapeutic. Moreover, bacterial cellulose can be nanosized to form Bacterial Nanocellulose (BNC), enhancing its properties.

Ayurveda botanicals in COVID-19 management: An in silico multi-target approach.

The Coronavirus disease (COVID-19) caused by the virus SARS-CoV-2 has become a global pandemic in a very short time span. Currently, there is no specific treatment or vaccine to counter this highly contagious disease. There is an urgent need to find a specific cure for the disease and global efforts are directed at developing SARS-CoV-2 specific antivirals and immunomodulators.

In silico studies on therapeutic agents for COVID-19: Drug repurposing approach.

Aims: The severe acute respiratory syndrome coronavirus 2, better known as COVID-19 has become the current health concern to the entire world. Initially appeared in Wuhan, China around December 2019, it had spread to almost 187 countries due to its high contagious nature. Precautionary measures remain the sole obliging tactic to cease the person to person transmissions till any effective method of treatment or vaccine is developed.

Structure-based design, synthesis and biological evaluation of a newer series of pyrazolo[1,5-a]pyrimidine analogues as potential anti-tubercular agents.

In-depth study of structure-based drug designing can provide vital leads for the development of novel, clinically active molecules. In this present study, twenty six novel pyrazolo[1,5-a]pyrimidine analogues (6a-6z) were designed using molecular docking studies. The designed molecules were synthesized in good yields.

Anti-anaphylactic and antiasthmatic activity of L. on experimental animals.

In Ayurveda, L. (Euphorbiaceae) prescribed in the treatment of various ailments like bronchial asthma, cough, diarrhea and bleeding piles. The present study was investigated to evaluate antianaphylactic, mast cell stabilizing and antiasthmatic activity of methanol and aqueous extract of (ET) on experimental animals.

Development and Validation of a High-Performance Thin-Layer Chromatographic (HPTLC) Method for Simultaneous Quantification of Reserpine, Atropine, and Piperine in , a Classical Ayurvedic Preparation.

Anxiety disorders are the most common of emotional disorders, affecting more than 20 million people annually. is a classical Ayurvedic polyherbal formulation prescribed in conditions of insomnia, hysteria, and is used as an anxiolytic agent. Standardization and quality control are the two major issues that need to be addressed for herbal formulations, especially those containing multiple herbal ingredients.

Direct and enhanced delivery of nanoliposomes of anti schizophrenic agent to the brain through nasal route.

The problem of inadequate oral bioavailability of Quetiapine Fumarate, a lipophilic drug used for schizophrenia, due to hepatic metabolism and repulsion by brain barrier was attempted in this study. Combination of two approaches, viz. Quetiapine inclusion into the liposomal carrier for better diffusion and administration through nasal route to avoid hepatic metabolism and barrier elimination was applied.

Comparison of three acute stress models for simulating the pathophysiology of stress-related mucosal disease.

Stress-related mucosal disease (SRMD) is highly prevalent in intensive care patients leading to increasing treatment cost and mortality. SRMD is a disease elusive of ideal treatment. Evaluation of drugs is very pertinent for the efficient and safe treatment of SRMD.

Anti-arthritic activity of a classical Ayurvedic formulation in rats.

In India, has been traditionally used in the Ayurvedic system of medicine to treat rheumatoid arthritis (RA). The current study was undertaken to evaluate anti-arthritic activity of alcoholic extract of in rats. Arthritis was induced by administration of formaldehyde (2%v/v) or Complete Freund's Adjuvant (CFA) into the sub-plantar surface of left hind paw of the animals.

Anti-inflammatory activity of fenugreek ( Linn) seed petroleum ether extract.

Objectives: The aim of the present work was to study the anti-inflammatory and anti-arthritic activities of petroleum ether extract of fenugreek seeds.

Materials And Methods: Fenugreek seed powder was extracted in petroleum ether by cold maceration. This fenugreek seed petroleum ether extract (FSPEE) was analyzed by gas-liquid chromatography (GLC) and tested on rats against carrageenan and formaldehyde-induced paw edema, complete Freund's adjuvant (CFA)-induced arthritis and cotton pellet-induced granuloma.

Beneficial effect of aspirin against interferon-α-2b-induced depressive behavior in Sprague Dawley rats.

Accumulating data advocates that inflammatory mediators may contribute to depression in experimental models as well as in humans. Nonetheless, whether anti-inflammatory treatments can prevent depression still remains controversial. To substantiate our hypothesis, we used an interferon-α-2b model of depression using Sprague Dawley rats.

Effect of ethanol extract of an ayurvedic preparation (Pathyadya Churna) on arthritis in rats.

Objectives: To study the anti-arthritic activity of Pathyadya Churna ethanol extract (PCE) in rats.

Materials And Methods: Formaldehyde (2% v/v) or complete Freund's adjuvant (CFA 0.l mL) was injected in the left hind paw of male Wistar rats to develop arthritis.

Design, Development and Rationalization of Sarpagandha Ghanvati.

Sarpagandha ghanvati is a classical Ayurvedic formulation widely prescribed for anxiety and insomnia. It contains Sarpagandha (roots of Rauwolfia serpentina L. (Benth.

Role of Aspirin and Dexamethasone against Experimentally Induced Depression in Rats.

A large number of current studies indicate that inflammatory mediators may contribute to depression in experimental models as well as in human beings. Nevertheless, the subject, whether anti-inflammatory treatments can prevent depression still remains controversial. In the present study, a chronic mild stress (CMS) model of male Sprague Dawley rats was used to investigate the role of anti-inflammatory drugs in the treatment of depression.

Comparative study between simple and optimized liposomal dispersion of quetiapine fumarate for diffusion through nasal route.

Context: Nasal route of drug administration is preferred more and more for the targeted delivery to the brain in current drug development scenario due to its ease of use, reliability, quick action, and lesser side effects. Those CNS drugs which have limited oral bioavailability due to pharmacokinetic consequences and brain barrier repulsion are getting onto this direction.

Objective: Quetiapine fumarate, an analogous to above and an antischizophrenic agent, is tested for its diffusion property with and without lipophilic carrier through sheep nasal membrane.

Wound healing activity of extracts derived from Shorea robusta resin.

Context: Shorea robusta Gaertn.f. (Dipterocarpaceae) resin is used for treating infected wounds and burns by tribals in India.

Formulation development, optimization, and evaluation of sustained release tablet of valacyclovir hydrochloride by combined approach of floating and swelling for better gastric retention.

The present study is intended to enhance gastric retention of sustained release tablet of valacyclovir hydrochloride by combined approach of floating and swelling. The tablets are prepared by direct compression method. Polyethylene oxide (Polyox WSR 303) is selected as the swelling matrix agent.