Synthesis, Spectral, Bio Assay, Chromatographic - Studying of New Imidazole Reagents Via Three Components Reaction

2021 ◽  
Vol 19 (7) ◽  
pp. 115-122
Author(s):  
Mohammed Nawfal Abdul Maged Alkhafaji ◽  
Hutham Abd Ali Abd Al Hussain ◽  
Dr. Nagham Mahmood Aljamali
Keyword(s):  
Nervous System ◽  
Drug Targets ◽  
Biological Activities ◽  
Drug Carrier ◽  
Chemical Properties ◽  
Cancer Drug ◽  
Condensation Process ◽  
Chromatographic Study ◽  
The Central Nervous System ◽  
Physical And Chemical

Imidazoles are part of the theophylline Reagent, found in tea leaves and coffee beans, which stimulates the central nervous system. It is found in the anti-cancer drug mercaptopurine, which fights leukemia by interfering with DNA systems. A number of prepared imidazoles, including clotrimazole, are selective inhibitors of nitric oxide synthase, which makes them interesting drug targets in inflammation, respiratory diseases and tumors of the nervous system. Other biological activities of the drug carrier imidazole relate to deregulation of the intracellular fluxes of (Ca and K) ions. Novel imidazole –heterocyclic reagents were created via cyclization process then condensation process., followed by investigation of all created new reagents via a number of spectral performances (FT.IR, H.NMR)–spectrophotometric, other physical and chemical properties, and chromatographic study with microbial studying for all new created imidazole reagents.

scholarly journals Breaking Barriers: Bioinspired Strategies for Targeted Neuronal Delivery to the Central Nervous System

Pharmaceutics ◽  
2020 ◽  
Vol 12 (2) ◽  
pp. 192 ◽  
Author(s):  
Ana P. Spencer ◽  
Marília Torrado ◽  
Beatriz Custódio ◽  
Sara C. Silva-Reis ◽  
Sofia D. Santos ◽  
...  
Keyword(s):  
Central Nervous System ◽  
Nervous System ◽  
Chemical Properties ◽  
Neurologic Diseases ◽  
Physiological Processes ◽  
Specific Accumulation ◽  
The Central Nervous System ◽  
Clinical Interest ◽  
Physical And Chemical ◽  
Neuronal Delivery

Central nervous system (CNS) disorders encompass a vast spectrum of pathological conditions and represent a growing concern worldwide. Despite the high social and clinical interest in trying to solve these pathologies, there are many challenges to bridge in order to achieve an effective therapy. One of the main obstacles to advancements in this field that has hampered many of the therapeutic strategies proposed to date is the presence of the CNS barriers that restrict the access to the brain. However, adequate brain biodistribution and neuronal cells specific accumulation in the targeted site also represent major hurdles to the attainment of a successful CNS treatment. Over the last few years, nanotechnology has taken a step forward towards the development of therapeutics in neurologic diseases and different approaches have been developed to surpass these obstacles. The versatility of the designed nanocarriers in terms of physical and chemical properties, and the possibility to functionalize them with specific moieties, have resulted in improved neurotargeted delivery profiles. With the concomitant progress in biology research, many of these strategies have been inspired by nature and have taken advantage of physiological processes to achieve brain delivery. Here, the different nanosystems and targeting moieties used to achieve a neuronal delivery reported in the open literature are comprehensively reviewed and critically discussed, with emphasis on the most recent bioinspired advances in the field. Finally, we express our view on the paramount challenges in targeted neuronal delivery that need to be overcome for these promising therapeutics to move from the bench to the bedside.

scholarly journals Green Silver and Gold Nanoparticles: Biological Synthesis Approaches and Potentials for Biomedical Applications

Molecules ◽  
2021 ◽  
Vol 26 (4) ◽  
pp. 844 ◽  
Author(s):  
Andrea Rónavári ◽  
Nóra Igaz ◽  
Dóra I. Adamecz ◽  
Bettina Szerencsés ◽  
Csaba Molnar ◽  
...  
Keyword(s):  
Gold Nanoparticles ◽  
Biomedical Applications ◽  
Biological Activities ◽  
Large Body ◽  
Chemical Properties ◽  
Biological Synthesis ◽  
Silver And Gold Nanoparticles ◽  
Comprehensive Collection ◽  
Synthetic Approaches ◽  
Physical And Chemical

The nanomaterial industry generates gigantic quantities of metal-based nanomaterials for various technological and biomedical applications; however, concomitantly, it places a massive burden on the environment by utilizing toxic chemicals for the production process and leaving hazardous waste materials behind. Moreover, the employed, often unpleasant chemicals can affect the biocompatibility of the generated particles and severely restrict their application possibilities. On these grounds, green synthetic approaches have emerged, offering eco-friendly, sustainable, nature-derived alternative production methods, thus attenuating the ecological footprint of the nanomaterial industry. In the last decade, a plethora of biological materials has been tested to probe their suitability for nanomaterial synthesis. Although most of these approaches were successful, a large body of evidence indicates that the green material or entity used for the production would substantially define the physical and chemical properties and as a consequence, the biological activities of the obtained nanomaterials. The present review provides a comprehensive collection of the most recent green methodologies, surveys the major nanoparticle characterization techniques and screens the effects triggered by the obtained nanomaterials in various living systems to give an impression on the biomedical potential of green synthesized silver and gold nanoparticles.

scholarly journals Permeability of the Blood-Brain Barrier and Transport of Nanobodies Across the Blood-Brain Barrier

2018 ◽  
Vol 62 (1) ◽  
pp. 59-66 ◽  
Author(s):  
I. Širochmanová ◽  
Ľ. Čomor ◽  
E. Káňová ◽  
I. Jiménez-Munguía ◽  
Z. Tkáčová ◽  
...  
Keyword(s):  
Central Nervous System ◽  
Nervous System ◽  
Blood Brain Barrier ◽  
Chemical Properties ◽  
Cost Effective ◽  
Central Nervous System Disease ◽  
Brain Barrier ◽  
Promising Alternative ◽  
Blood Brain ◽  
The Central Nervous System

Abstract The presence of a blood-brain barrier (BBB) and a blood-cerebrospinal fluid barrier presents animmense challenge for effective delivery of therapeutics to the central nervous system. Many potential drugs, which are effective at their site of action, have failed due to the lack of distribution in sufficient quantity to the central nervous system (CNS). In consequence, many diseases of the central nervous system remain undertreated. Antibodies, IgG for example, are difficult to deliver to the CNS due to their size (~155 kDa), physico-chemical properties and the presence of Fc receptor on the blood-brain barrier. Smaller antibodies, like the recently developed nanobodies, may overcome the obstacle of the BBB and enter into the CNS. The nanobodies are the smallest available antigen-binding fragments harbouring the full antigenbinding capacity of conventional antibodies. They represent a new generation of therapeutics with exceptional properties, such as: recognition of unique epitopes, target specificity, high affinity, high solubility, high stability and high expression yields in cost-effective recombinant production. Their ability to permeate across the BBBmakes thema promising alternative for central nervous system disease therapeutics. In this review, we have systematically presented different aspects of the BBB, drug delivery mechanisms employed to cross the BBB, and finally nanobodies — a potential therapeutic molecule against neuroinfections.

Synthesis and Kinetic Investigations for the Isomerization Process of 2–Hydroxy Chalcone Derivatives

2019 ◽  
Vol 41 (6) ◽  
pp. 1046-1046
Author(s):  
Omar A Shareef Omar A Shareef ◽  
Said A Said and Ali Y Abdulrazaq Said A Said and Ali Y Abdulrazaq
Keyword(s):  
Biological Activities ◽  
Chemical Properties ◽  
Physical And Chemical Properties ◽  
Pseudo First Order Reaction ◽  
First Order ◽  
Steric Factors ◽  
Kinetic Investigations ◽  
The Stability ◽  
Physical And Chemical ◽  
And Chemical Properties

The wide biological activities of flavanones are mainly depends on their physical and chemical properties, thus a number of substituted 2-Hydroxy chalcones have been synthesized, and their isomerization to their corresponding flavanones was studied. In order to determine the rate constant, kinetic experiments were performed using HPLC technique in (9:1) (CH3CN:H2O) medium at different temperature (298-318) K. The obtained results were interpreted by four steps mechanism, which considered the existence of phenoxide ion as the key intermediate. This study performed with a pseudo first order ( reaction in which the rate for the studied compounds follow the sequence 5 andgt; 2 andgt; 1 andgt; 4 andgt; 3, the activation energy have the same sequence for these compounds .The effect of substituents on the rate showed that electronic and steric factors play reasonable role on the stability of the product .

scholarly journals Proanthocyanidins: Oligomeric Structures with Unique Biochemical Properties and Great Therapeutic Promise

2012 ◽  
Vol 7 (3) ◽  
pp. 1934578X1200700 ◽  
Author(s):  
Zhanjie Xu ◽  
Peng Du ◽  
Peter Meiser ◽  
Claus Jacob
Keyword(s):  
Protein Interactions ◽  
Biological Activities ◽  
Antioxidant Properties ◽  
Chemical Properties ◽  
Cancer Chemoprevention ◽  
Biochemical Properties ◽  
Synthetic Methods ◽  
Practical Applications ◽  
Wide Range ◽  
Physical And Chemical

Proanthocyanidins represent a unique class of oligomeric and polymeric secondary metabolites found ubiquitously and in considerable amounts in plants and some algae. These substances exhibit a range of rather surprising physical and chemical properties which, once applied to living organisms, are translated into a multitude of biological activities. The latter include antioxidant properties, cancer chemoprevention, anti-inflammatory and anti-diabetic effects as well as some exceptional, yet highly interesting activities, such as anti-nutritional and antimicrobial activity. Despite the wide range of activities and possible medical/agricultural applications of proanthocyanidins, many questions still remain, including issues related to bioavailability, metabolism and the precise biochemical, extra- and intracellular targets and mode(s) of action of these highly potent materials. Among the various physical and chemical interactions of such substances, strong binding to proteins appears to form the basis of many of their biological activities. Once easy-to-use synthetic methods to produce appropriate quantities of pure proanthocyanidins are available, it will be possible to identify the prime biological targets of these oligomers, study oligomer-protein interactions in more detail and develop possible practical applications in medicine and agriculture.

scholarly journals Biophysical Characterization and Anticancer Activities of Photosensitive Phytoanthraquinones Represented by Hypericin and Its Model Compounds

Molecules ◽  
2020 ◽  
Vol 25 (23) ◽  
pp. 5666
Author(s):  
Valéria Verebová ◽  
Jiří Beneš ◽  
Jana Staničová
Keyword(s):  
Photodynamic Therapy ◽  
Biological Activities ◽  
Chemical Properties ◽  
Physical And Chemical Properties ◽  
Anticancer Activities ◽  
Model Compounds ◽  
Antitumor Effects ◽  
Biophysical Characterization ◽  
Physical And Chemical ◽  
And Chemical Properties

Photosensitive compounds found in herbs have been reported in recent years as having a variety of interesting medicinal and biological activities. In this review, we focus on photosensitizers such as hypericin and its model compounds emodin, quinizarin, and danthron, which have antiviral, antifungal, antineoplastic, and antitumor effects. They can be utilized as potential agents in photodynamic therapy, especially in photodynamic therapy (PDT) for cancer. We aimed to give a comprehensive summary of the physical and chemical properties of these interesting molecules, emphasizing their mechanism of action in relation to their different interactions with biomacromolecules, specifically with DNA.

scholarly journals Use of Cerium Nitrate Nanoparticles in Biological Environment Along with the Factors Effecting It: An Empirical Overview

2021 ◽  
Author(s):  
Zarish Fatima ◽  
Sameer Quazi ◽  
Shreelaxmi Gavas ◽  
Tomasz Karpiński
Keyword(s):  
Biological Activities ◽  
Chemical Properties ◽  
Physical And Chemical Properties ◽  
Medical Field ◽  
Physiochemical Properties ◽  
Synthesis Of Nanoparticles ◽  
Biological Environment ◽  
Physical And Chemical ◽  
Nano Ceria ◽  
And Chemical Properties

The advancement in the production and usage of the cerium oxide nanoparticles have diverted the attention of scientists towards their usage in medical field and therapeutic usage. The clinical usage of these Nano ceria is based on their ability to moderate the oxidative stress and this is only because of their ability to change their valent state from +3 to +4 which makes them ideal for scavenging radicals for use in a number of systemic and neurodegenerative disorders. This review aims to synthesize the basic methods used for the synthesis of nanoparticles along with the use of ligand, stabilizing agent and other components. This review also concludes that how various physical and chemical properties of nanoparticles effect the basic biological activities such as antimicrobial activity, cytotoxicity and many others. However, during the standardization, some of the physiochemical properties, methods used for preparation and catalytic abilities must be taken into account.

Recent patents, regulatory issues, and toxicity of nanoparticles in neuronal disorders

2020 ◽  
Vol 21 ◽  
Author(s):  
Abdul Muheem ◽  
Mohammed Asadullah Jahangir ◽  
Chandra Prakash Jaiswal ◽  
Mohammed Jafar ◽  
Mohammad Zaki Ahmad ◽  
...  
Keyword(s):  
Developmental Toxicity ◽  
Chemical Properties ◽  
Primary Concern ◽  
Negative Effects ◽  
Regulatory Issues ◽  
Safety Regulations ◽  
Regulatory Guidelines ◽  
The Central Nervous System ◽  
Physical And Chemical ◽  
Neuronal Disorders

Background:: From last few decades, nanoparticles have witnessed breakthroughs in the treatment of neurological disorders due to their unique physiochemical properties which make them effective drug delivery system. However, there is not much information available on the toxicity of nanoparticles in neuronal disorders. The toxic effect of nanoparticles on brain disorders and their regulatory issues is the primary concern of the healthcare industry. Methods:: A strategical literature search was performed on a various bibliographic database such as Scopus, PubMed, SciFinder, Google Scholar, Medline, Google patent, Derwent Innovation, and Orbit Intelligence for retrieval of peerreviewed articles and patents on regulatory issues and toxicity of nanoparticles in neuronal disorders over the past four decades or so. The relevant hits of articles and patents were analyzed and citation search for the relevant documents was carried out. Results:: The literature documents have been summarized regarding the existing regulatory issues and toxicity of nanoparticles on neuronal disorders with a focus on the detailed mechanism of developmental toxicity of nanoparticles. The focus of this report is to emphasize the negative effects of nanoparticle on neuronal disorders which may partially contribute to management of toxicity of nanoparticles. Conclusion:: Although nanoparticles have unique physical and chemical properties that explain the broad range of application for the central nervous system, they can also manifest neurotoxic effects due to cell necrosis, a generation of free radicals, immune responses and neuroinflammation. Thus, this review highlights on risk assessment, safety regulations and regulatory guidelines of nanoparticles which may reduce adverse reactions in humans and animals.

Current Pharmaceutical Aspects of Synthetic Quinoline Derivatives

2020 ◽  
Vol 20 ◽  
Author(s):  
Rukhsana Tabassum ◽  
Muhammad Ashfaq ◽  
Hiroyuki Oku
Keyword(s):  
Fungal Infections ◽  
Biological Activities ◽  
Chemical Properties ◽  
New Drugs ◽  
Quinoline Derivatives ◽  
Wide Range ◽  
Anti Cancer ◽  
Anti Fungal ◽  
Physical And Chemical ◽  
And Chemical Properties

Abstract:: Quinoline derivatives are considered as broad spectrum pharmacological compounds that exhibit wide range of biological activities. Integration of quinoline moiety can improve its physical and chemical properties and also pharmacological behavior. Due to its wide range of pharmaceutical applications it is very popular compound to design new drugs for treatment of multiple diseases like cancer, dengue fever, malaria, tuberculosis, fungal infections, AIDS, Alzheimer’s disease and diabetes . In this review our major focus is to pay attention on biological activities of quinoline compounds in treatment of these diseases such as, anti-viral, anti-cancer, anti-malarial, anti-bacterial, anti-fungal, anti-tubercular and anti-diabetic.

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