Design, Synthesis and Pharmacological Evaluation of Novel C,C-Quinoxaline Derivatives as Promising Anxiolytic Agents.

A new series of quinoxaline derivatives, -, were synthesized and their anxiolytic potential was evaluated in vivo using elevated plus maze (EPM), open field (OF) and light-dark box (LDB) techniques. According to the results of the EPM, four active compounds were found in , , , . Their anxiolytic properties were confirmed in terms of LDB and the most active was compound .

Guanidine Derivatives of Quinazoline-2,4(1,3)-Dione as NHE-1 Inhibitors and Anti-Inflammatory Agents.

Quinazolines are a rich source of bioactive compounds. Previously, we showed NHE-1 inhibitory, anti-inflammatory, antiplatelet, intraocular pressure lowering, and antiglycating activity for a series of quinazoline-2,4(1,3)-diones and quinazoline-4(3)-one guanidine derivatives. In the present work, novel N1,N3-bis-substituted quinazoline-2,4(1,3)-dione derivatives bearing two guanidine moieties were synthesized and pharmacologically profiled.

Discovery of Nitro-azolo[1,5-]pyrimidines with Anti-Inflammatory and Protective Activity against LPS-Induced Acute Lung Injury.

Acute lung injury remains a challenging clinical condition, necessitating the development of novel, safe and efficient treatments. The prevention of macrophage M1-polarization is a viable venue to tackle excessive inflammation. We performed a phenotypic screening campaign to identify azolopyrimidine compounds that effectively inhibit LPS-induced NO synthesis and interleukin 6 (IL-6) secretion.

Synthesis and multifaceted pharmacological activity of novel quinazoline NHE-1 inhibitors.

The Na/H exchanger isoform 1 (NHE-1) attracts ongoing attention as a validated drug target for the management of cardiovascular and ocular diseases owing to cytoprotective, anti-ischemic and anti-inflammatory properties of NHE-1 inhibitors. Herein we report novel NHE-1 inhibitors realized via functionalization of N-alkyl quinazoline-2,4(1H,3H)-dione and quinazoline-4(3H)-one with N-acylguanidine or 3-acyl(5-amino-1,2,4-triazole) side chain. Lead compounds show activity in a nanomolar range.

Synthesis and Pharmacological Evaluation of Novel 2,3,4,5-tetrahydro[1,3]diazepino[1,2-]benzimidazole Derivatives as Promising Anxiolytic and Analgesic Agents.

A number of novel 2,3,4,5-tetrahydro[1,3]diazepino[1,2-]benzimidazole derivatives were obtained by alkylation mainly in the 1-tautomeric form of 2,3,4,5-tetrahydro[1,3]diazepino[1,2-]benzimidazole or its 8,9-dimethyl-substituted analog 4-chlorobenzyl bromide, 4-chloroacetic acid fluoroanilide, and 4-tert-butylphenacyl bromide in neutral medium. Compounds 3 were cyclized and synthesized earlier with 11-phenacyl-substituted diazepino[1,2-]benzimidazoles upon heating in conc. HBr.

Searching for new anxiolytic agents among derivatives of 11-dialkylaminoethyl-2,3,4,5-tetrahydrodiazepino[1,2-a]benzimidazole.

A study on the anxiolytic activity of the new derivatives of 11-dialkylaminoethyl-2,3,4,5-tetrahydrodiazepino[1,2-a]benzimidazole, containing privileged scaffolds of benzodiazepine and benzimidazole in their structure, was conducted. The cytotoxic properties of low levels of six compounds were preliminary determined in vitro using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide test. The screening of these substances for anxiolytic activity was conducted using elevated plus maze (EPM) test in vivo, and DAB-21 was found to be the most active compound.

Light-Assisted Rechargeable Lithium Batteries: Organic Molecules for Simultaneous Energy Harvesting and Storage.

Lithium batteries that could be charged on exposure to sunlight will bring exciting new energy storage technologies. Here, we report a photorechargeable lithium battery employing nature-derived organic molecules as a photoactive and lithium storage electrode material. By absorbing sunlight of a desired frequency, lithiated tetrakislawsone electrodes generate electron-hole pairs.

Bioderived Molecular Electrodes for Next-Generation Energy-Storage Materials.

Invited for this month's cover are the groups of George John at the City College of New York-CUNY, Leela R. Arava at Wayne State University, and Pulickel Ajayan at Rice University. The image portraits future prospects of bioderived molecular electrodes for next-generation energy-storage materials.

Bioderived Molecular Electrodes for Next-Generation Energy-Storage Materials.

Nature-derived organic small molecules, as energy-storage materials, provide low-cost, recyclable, and non-toxic alternatives to inorganic and polymer electrodes for lithium-/sodium-ion batteries and beyond. Some organic carbonyl compounds have met or exceeded the voltages and gravimetric storage capacities achieved by traditional transition metal oxide-based compounds due to the metal-ion coupled redox and facile electron-transport capability of functional groups. Stability issues that previously limited the capacity of small organic molecules can be remediated with reactions to form insoluble salts, noncovalent interactions (hydrogen bonding and π stacking), loading onto substrates, and careful electrolyte selection.

A common tattoo chemical for energy storage: henna plant-derived naphthoquinone dimer as a green and sustainable cathode material for Li-ion batteries.

The burgeoning energy demands of an increasingly eco-conscious population have spurred the need for sustainable energy storage devices, and have called into question the viability of the popular lithium ion battery. A series of natural polyaromatic compounds have previously displayed the capability to bind lithium polar oxygen-containing functional groups that act as redox centers in potential electrodes. Lawsone, a widely renowned dye molecule extracted from the henna leaf, can be dimerized to bislawsone to yield up to six carbonyl/hydroxyl groups for potential lithium coordination.

In Situ Synthesis of Metal Nanoparticle Embedded Hybrid Soft Nanomaterials.

The allure of integrating the tunable properties of soft nanomaterials with the unique optical and electronic properties of metal nanoparticles has led to the development of organic-inorganic hybrid nanomaterials. A promising method for the synthesis of such organic-inorganic hybrid nanomaterials is afforded by the in situ generation of metal nanoparticles within a host organic template. Due to their tunable surface morphology and porosity, soft organic materials such as gels, liquid crystals, and polymers that are derived from various synthetic or natural compounds can act as templates for the synthesis of metal nanoparticles of different shapes and sizes.