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"Chemical agents"
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Bioactive Thiazine and Benzothiazine Derivatives: Green Synthesis Methods and Their Medicinal Importance
Thiazines are a group of heterocyclic organic compounds that are still largely unexplored for their pharmacological activities. There are different available methods for the synthesis of thiazine derivatives in the literature. In this review, we discuss available methods of thiazine preparation through green synthesis methods. Beside their synthesis, many thiazine derivatives are biologically active and play an important role in the treatment of various diseases and show promising results of varying degrees, where they act as antibacterial, antifungal, antitumor, antimalarial, antineoplastic, antiviral, anti-inflammatory, analgesic and anticancer agents and thus they represent an interesting class of heterocyclic medicinal compounds worthy of further exploration.
Journal Article
Novichoks: The Dangerous Fourth Generation of Chemical Weapons
“Novichoks” is the name given to the controversial chemical weapons supposedly developed in the former Soviet Union between the 1970s and the 1990s. Designed to be undetectable and untreatable, these chemicals became the most toxic of the nerve agents, being very attractive for both terrorist and chemical warfare purposes. However, very little information is available in the literature, and the Russian government did not acknowledge their development. The intent of this review is to provide the IJMS readers with a general overview on what is known about novichoks today. We briefly tell the story of the secret development of these agents, and discuss their synthesis, toxicity, physical-chemical properties, and possible ways of treatment and neutralization. In addition, we also wish to call the attention of the scientific community to the great risks still represented by nerve agents worldwide, and the need to keep constant investments in the development of antidotes and ways to protect against such deadly compounds.
Journal Article
Surfactants and interfacial phenomena
\"This book provides an easy-to-read, user-friendly resource for industrial chemists and a text for classroom use, and is an unparalleled tool for understanding and applying the latest information on surfactants. Problems are included at the end of each chapter to enhance the reader's understanding, along with many tables of data that are not compiled elsewhere. Only the minimum mathematics is used in the explanation of topics to make it easy-to-understand and very user friendly\"-- Source other than Library of Congress.
Book
Molecular Hybridization: A Useful Tool in the Design of New Drug Prototypes
Molecular hybridization is a new concept in drug design and development based on the combination of pharmacophoric moieties of different bioactive substances to produce a new hybrid compound with improved affinity and efficacy, when compared to the parent drugs. Additionally, this strategy can result in compounds presenting modified selectivity profile, different and/or dual modes of action and reduced undesired side effects. So, in this paper, we described several examples of different strategies for drug design, discovery and pharmacomodulation focused on new innovative hybrid compounds presenting analgesic, anti-inflammatory, platelet anti-aggregating, anti-infectious, anticancer, cardio- and neuroactive properties.
Journal Article
Ultrasonic synthesis, characterization, DFT and molecular docking of a biocompatible Zn-based MOF as a potential antimicrobial, anti-inflammatory and antitumor agent
Zinc metal–organic frameworks have emerged as promising candidates, demonstrating excellent biological properties stemming from the unique characteristics of MOFs and zinc. In this study, we employed a facile method to synthesize a zinc metal–organic framework
[Zn(IP)(H
2
O)]
using ultrasound irradiation, with the linker being isophthalic acid (IPA) (1,3-benzene dicarboxylic acid). The parent
Zn-MOF
and two
Ag/Zn-MOF
samples prepared via loading and encapsulation methods were comprehensively characterized using various techniques, including FT-IR, XRD, SEM, TEM, N
2
adsorption–desorption isotherm, UV–vis spectroscopy and TGA. The parent
Zn-MOF
and two
Ag/Zn-MOF
samples exhibited a broad spectrum of antibacterial effects. Remarkably, genomic DNA of
P. aeruginosa
was effectively degraded by
Zn-MOF,
further supporting its potent antibacterial results. The free radical inhibition assay demonstrated a 71.0% inhibition under the influence of
Zn-MOF
. In vitro cytotoxicity activity of
Zn-MOF
against HepG-2 and Caco-2 cell lines revealed differential cytotoxic effects, with higher cytotoxicity against Caco-2 as explored from the IC
50
values. This cytotoxicity was supported by the high binding affinity of
Zn-MOF
to CT-DNA. Importantly, the non-toxic property of
Zn-MOF
was confirmed through its lack of cytotoxic effects against normal lung cell (Wi-38). The anti-inflammatory treatment of
Zn-MOF
achieved 75.0% efficiency relative to the standard Ibuprofen drug. DFT and docking provided insights into the geometric stability of
Zn-MOF
and its interaction with active amino acids within selected proteins associated with the investigated diseases. Finally, the synthesized
Zn-MOF
shows promise for applications in cancer treatment, chemoprevention, and particularly antibacterial purposes.
Journal Article
Fibroblast Growth Factor 21 Mediates Specific Glucagon Actions
Glucagon, an essential regulator of glucose homeostasis, also modulates lipid metabolism and promotes weight loss, as reflected by the wasting observed in glucagonoma patients. Recently, coagonist peptides that include glucagon agonism have emerged as promising therapeutic candidates for the treatment of obesity and diabetes. We developed a novel stable and soluble glucagon receptor (GcgR) agonist, which allowed for in vivo dissection of glucagon action. As expected, chronic GcgR agonism in mice resulted in hyperglycemia and lower body fat and plasma cholesterol. Notably, GcgR activation also raised hepatic expression and circulating levels of fibroblast growth factor 21 (FGF21). This effect was retained in isolated primary hepatocytes from wild-type (WT) mice, but not GcgR knockout mice. We confirmed this link in healthy human volunteers, where injection of natural glucagon increased plasma FGF21 within hours. Functional relevance was evidenced in mice with genetic deletion of FGF21, where GcgR activation failed to induce the body weight loss and lipid metabolism changes observed in WT mice. Taken together, these data reveal for the first time that glucagon controls glucose, energy, and lipid metabolism at least in part via FGF21-dependent pathways.
Journal Article