Synthesis, Trans-Cis Photoisomerization, Fluorescence Decay Studies of Methoxy Ester Functionalized Alkoxy Side Chain Azobenzene Compounds and Their Photoluminescence Dynamics.

In this study, a series of new methoxy ester functionalized core fluorinated, chloro-fluorinated azobenzene derivatives were synthesized. The molecular structures of the azobenzene derivatives (3a-3c and 4a-4c) were confirmed through various analytical methods, with variations in the alkoxy chain length on one end of the aromatic ring. Optical absorption studies of 3a, 3b revealed π-π* transitions around 368-392 nm.

Polymeric Nanodiscs Comprising 5-Fluorouracil for Inhibition of Protein Aggregation and Their Anti-Alzheimer's Activity in the Model.

Nanoconjugates are promising for therapeutic drug delivery and targeted applications due to the numerous opportunities to functionalize their surface. The present study reports the synthesis of 5-fluorouracil (5-FU)-entrapped polyvinylpyrrolidone (PVP) nanoconjugates, precisely 5-FU-PVP and 5-FU-PVP-Au, and the evaluation of protein aggregation inhibition efficiency. The 5-FU-loaded polymer nanoconjugates were functionalized with gold nanoparticles and analyzed using characterization techniques like dynamic light scattering, UV-visible spectroscopy, Fourier-transform infrared spectroscopy, and zeta potential analysis.

Quinoline hybrid derivatives as effective structural motifs in the treatment of tuberculosis: Emphasis on structure-activity relationships.

Mycobacterium tuberculosis (MTB/Mtb) is the causative agent of tuberculosis (TB), a highly infectious serious airborne illness. TB usually affects the lungs, in 25 % of patients (children or immune impaired adults), mycobacteria can enter the blood stream and infect other bodily areas such the meninges, pleura, lymphatic system, genitourinary system, bones, and joints. Currently, the most challenging aspect of treating this illness is the ineffectiveness of the most potent first-line anti-TB medications, isoniazid, rifampin, pyrazinamide, and ethambutol, which can result in multidrug-resistant TB (MDR-TB), extensively drug-resistant TB (XDR-TB), and in rare instances, completely drug-resistant TB (TDR-TB).

Engineering the Coordination Environment in the Silver(I)- and Ruthenium(II)--Heterocyclic Carbene Complexes in Instigating the Electrocatalytic Hydrogen Evolution Reaction.

The quest for cost-efficient and high-performance electrocatalysts towards electrocatalytic water splitting is a key and an interdisciplinary area of study. Considerable progress is being driven by developments in the field of energy research. In a fundamental study, we have synthesized NHC precursors ( and ) and corresponding metal-NHC complexes of silver(I)- ( and ) and ruthenium(II)- ( and ) of a N-heterocyclic carbene-based ligand type incorporating coumarins.

Quinoline Synthesis: Nanocatalyzed Green Protocols-An Overview.

Heterocyclic compounds are of great interest in our daily lives. They are widely distributed in nature and are synthesized in laboratories. Heterocycles play an important role in the metabolism of all living cells, including vitamins and coenzyme precursors like thiamine and riboflavin.

Polymeric curcumin nanospheres for lysozyme aggregation inhibition, antibacterial, and wound healing applications.

The present study reports highly stable polymeric nanoparticles comprising curcumin and polyvinylpyrrolidone, and then conjugated with gold nanoparticles, resulting in C-PVP and C-PVP-Au, respectively. The synthesized conjugates C-PVP and C-PVP-Au were investigated for amyloid aggregation inhibition activity, antimicrobial activity, and wound healing applications. The anti-amyloidogenic capacity of nanoconjugates were studied for model protein, hen egg-white lysozyme (HEWL).

Wound healing efficacy of curcumin-loaded sandalwood bark-derived carbon nanosphere/PVA nanofiber matrix.

The present investigation deals with the evaluation of the wound healing efficacy of sandalwood bark-derived carbon nanospheres loaded with curcumin-embedded polyvinyl alcohol (PVA) nanofiber membranes (NF). Carbon nanospheres (CNS) were prepared by pyrolyzing sandal wood bark powder at 750 °C. The morphology was confirmed by field emission scanning electron micrographs and a rich amount of carbon was confirmed by the energy dispersive X-ray technique.

Reusable nano-catalyzed green protocols for the synthesis of quinoxalines: an overview.

Heterocyclic compounds are very widely distributed in nature and are essential for life activities. They play a vital role in the metabolism of all living cells, for example, vitamins and co-enzyme precursors thiamine, riboflavin Quinoxalines are a class of N-heterocycles that are present in a variety of natural and synthetic compounds. The distinct pharmacological activities of quinoxalines have attracted medicinal chemists considerably over the past few decades.

Anti-amyloidogenic property of gold nanoparticle decorated quercetin polymer nanorods in pH and temperature induced aggregation of lysozyme.

Quercetin is an abundant plant polyphenol effective against several diseases due to its antioxidant and anti-inflammatory activity. Herein, we report novel polymeric quercetin nanorods and the former decorated with gold nanoparticles for the first time. The prepared conjugates quercetin-polyvinylpyrrolidone (Q-PVP) and quercetin-polyvinylpyrrolidone-gold nanoparticles (Q-PVP-Au) were characterized by UV-visible spectroscopy, Fourier transform infrared, dynamic light scattering, and zeta potential measurements.

Antibacterial natural products from microbial and fungal sources: a decade of advances.

Throughout the ages the world has witnessed the outbreak of many infectious diseases. Emerging microbial diseases pose a serious threat to public health. Increasing resistance of microorganisms towards the existing drugs makes them ineffective.

Synthetic and natural coumarins as potent anticonvulsant agents: A review with structure-activity relationship.

What Is Known And Objective: The main objective of this review is to highlight the most relevant studies since 1990 (to date) in the area of medicinal chemistry aspects to provide a panoramic view to the biologists/medicinal chemists working in this area and would assist them in their efforts to design, synthesize and extract (from natural source) coumarin-based anticonvulsant agents. Also, the structure-activity relationship (SAR) studies are also discussed for further rational design of this kind of derivatives. It is hoped that this review will be helpful for new thoughts in the quest for rational designs of more active and less toxic coumarin-based antiepileptic agents.

Multi-Targeting Tacrine Conjugates with Cholinesterase and Amyloid-Beta Inhibitory Activities: New Anti-Alzheimer's Agents.

Alzheimer's disease (AD) is a severe age dependent and chronic problem with no cure so far. The available treatments are temporary, acting over short period of time. The main pathological hallmark of the disease includes cholinergic dysfunction, oxidative stress, accumulation of Aβ fibrils and tau tangles.

Nonwoven fabric supported, chitosan membrane anchored with curcumin/TiO complex: Scaffolds for MRSA infected wound skin reconstruction.

Use of biomaterial scaffolds as drug carriers for infected wounds treatment is of wide scope. A series of curcumin/TiO complex loaded chitosan scaffolds are fabricated for the same. Synthesized wound dressing material is screened for their morphology, water absorption capacity; in vitro drug release patterns, in vitro antibacterial studies against gram +ve and a gram -ve bacteria, cell viability for 3T3-L1 cell lines as well as in vivo MRSA infected wound healing capability.

Development of coumarin-benzofuran hybrids as versatile multitargeted compounds for the treatment of Alzheimer's Disease.

Alzheimer's disease (AD), the most common cause of dementia, is a neurodegenerative disorder characterized by progressive deterioration of memory and cognition. The evidenced multifactorial nature of AD has been considered the main reason for the absence of cure so far. Therefore, the development of novel hybrids to treat the disease is very much essential.

Quinoxaline and quinoxaline-1,4-di-N-oxides: An emerging class of antimycobacterials.

Tuberculosis (TB) is a highly dreaded, infectious, chronic, airborne disease affecting more than two million people all around the world, with more than eight million cases every calendar year. TB is the second leading infectious cause of death after HIV/AIDS. Over the past few decades, numerous efforts have been undertaken to develop new anti-TB agents.

Novel Tacrine-Hydroxyphenylbenzimidazole hybrids as potential multitarget drug candidates for Alzheimer's disease.

Alzheimer's disease (AD) is a severe age-dependent neurodegenerative disorder affecting millions of people, with no cure so far. The current treatments only achieve some temporary amelioration of the cognition symptoms. The main characteristics of the patient brains include the accumulation of amyloid plaques and neurofibrillary tangles (outside and inside the neurons) but also cholinergic deficit, increased oxidative stress and dyshomeostasis of transition metal ions.

Hydroxypyridinone-benzofuran hybrids with potential protective roles for Alzheimer´s disease therapy.

A series of (3-hydroxy-4-pyridinone)-benzofuran hybrids have been developed and studied as potential multitargeting drugs for Alzheimer's disease (AD). Their design envisaged mainly to mimic the donepezil drug, a marketed inhibitor of acetylcholinesterase (AChE), and to endow the conjugate molecules with extra-properties such as metal chelation, radical scavenging and inhibition of amyloid peptide (Aβ) aggregation. Thus, a set of eleven new hybrid compounds was developed and evaluated for chemical and biological properties, in solution and in neuronal cell environment.

Cassia tora Linn.: A boon to Alzheimer's disease for its anti-amyloidogenic and cholinergic activities.

Background: Drug discovery from natural products as alternatives for Alzheimer's disease (AD) is a current trend. For which plant is an alternative for searching potential molecule for treating AD. Availability of Cassia tora as weed and abundance in nature makes it as potential source.

An overview of benzo[b]thiophene-based medicinal chemistry.

Among sulfur containing heterocycles, benzothiophene and its derivatives are at the focus as these candidates have structural similarities with active compounds to develop new potent lead molecules in drug design. Benzo[b]thiophene scaffold is one of the privileged structures in drug discovery as this core exhibits various biological activities allowing them to act as anti-microbial, anti-cancer, anti-inflammatory, anti-oxidant, anti-tubercular, anti-diabetic, anti-convulsant agents and many more. Further, numerous benzothiophene-based compounds as clinical drugs have been extensively used to treat various types of diseases with high therapeutic potency, which has led to their extensive developments.

A review on antioxidant potential of bioactive heterocycle benzofuran: Natural and synthetic derivatives.

The majority of heterocycle compounds and typically common heterocycle fragments present in most pharmaceuticals currently marketed, alongside with their intrinsic versatility and unique physicochemical properties, have poised them as true cornerstones of medicinal chemistry. In this context, oxygen heterocycles exhibit diverse biological and pharmacological activities due in part to the similarities with many natural and synthetic molecules with known biological activity. Among oxygen containing heterocycles, benzofuran (synthetic and natural isolated) and its derivatives have attracted medicinal chemists and pharmacologists due to their pronounced biological activities and their potential applications as pharmacological agents such as antioxidant, antitumor, antiplatelet, antimalarial, antiinflammatory, antidepressant and anticonvulsant properties.

Benzimidazole-core as an antimycobacterial agent.

Mycobacterium tuberculosis (Mtb) is considered as one of the precarious bacterial infections around the world. Through a projected 8.7 million new tuberculosis (TB) cases and 1.

New Tacrine Hybrids with Natural-Based Cysteine Derivatives as Multitargeted Drugs for Potential Treatment of Alzheimer's Disease.

Alzheimer's disease (AD) is a devastating age-dependent neurodegenerative disorder. The main hallmarks are impairment of cholinergic system and accumulation in brain of beta-amyloid (Aβ) aggregates, which have been associated with oxidative damage and dyshomeostasis of redox-active biometals. The absence of an efficient treatment that could delay or cure AD has been attributed to the complexity and multifactorial nature of this disease.

N-heterocyclic carbene metal complexes as bio-organometallic antimicrobial and anticancer drugs.

Late transition metal complexes that bear N-heterocyclic carbene (NHC) ligands have seen a speedy growth in their use as both, metal-based drug candidates and potentially active homogeneous catalysts in a plethora of C-C and C-N bond forming reactions. This review article focuses on the recent developments and advances in preparation and characterization of NHC-metal complexes (metal: silver, gold, copper, palladium, nickel and ruthenium) and their biomedical applications. Their design, syntheses and characterization have been reviewed and correlated to their antimicrobial and anticancer efficacies.