scholarly journals NAFTOIMIDAZÓIS E NAFTOXAZÓIS - PROMISSORES COMPONENTES DE SISTEMAS TERANÓSTICOS

Química Nova ◽  
2021 ◽  
Author(s):  
Victória Santos ◽  
Délis Guimarães ◽  
Rodolfo Nishimura ◽  
Larissa Rolim ◽  
Arlan Gonsalves ◽  
...  
Keyword(s):  
Systematic Review ◽  
Optical Properties ◽  
Broad Spectrum ◽  
Therapeutic Agent ◽  
Biological Activities ◽  
Biological Systems ◽  
Fluorescence Emission ◽  
Imaging Agents ◽  
Synthetic Routes ◽  
Aromatic Systems

NAPHTHOIMIDAZOLES AND NAPHTHOXAZOLES - PROMISING COMPONENTS OF THERANOSTIC SYSTEMS. Theranostic can be used to define therapeutic and imaging agents in a system. It is consisting of four components: signal emitter, therapeutic agent, targeting ligand and carrier. Naphthoimidazole and naphthoxazole are extended aromatic systems, and can participate in theranostic systems (TS) acting as a therapeutic agent and/or a signal emitter considering of their broad spectrum of biological activities and their optical properties of fluorescence emission. This systematic review investigated the applicability of the naphthoimidazole and naphthoxazole nuclei as constituents of TS and shows the synthesis methodologies described in the articles selected. Among the scientific articles suitable for the criteria of the systematic review, more than 35% described the evaluation of biological activities, mainly the naphthoimidazole derivatives, and approximately 18% explored the fluorescence emission of naphthoxazole derivatives and their applicability in biological systems. Among the selected articles 53% and 44% show synthetic routes for the preparation of naphthoxazoles and naphthoimidazoles, respectively. It was observed that both nuclei can be synthesized from various reagents, such as naphthoquinones, naphthols, naphthoic acids, aminonaphthoquinones and cyanophthalides. The results of this study suggests that naphthoimidazole and naphthoxazole derivatives are promising for application as components of TS, and there are various synthetic possibilities for obtaining these heterocycles.

Recent Advances in Transition Metal Mediated Synthetic Approaches to Quinoline Derivatives

2020 ◽  
Vol 17 ◽  
Author(s):  
Rukhsana Tabassum ◽  
Muhammad Ashfaq ◽  
Hiroyuki Oku
Keyword(s):  
Transition Metal ◽  
Heterocyclic Compounds ◽  
Therapeutic Agent ◽  
Biological Activities ◽  
Quinoline Derivatives ◽  
Quinoline Ring ◽  
Pharmacological Activities ◽  
Synthetic Routes ◽  
Synthetic Approaches ◽  
Significant Attention

Abstract:: Synthesis of heterocyclic compounds containing quinoline scaffold attracted a significant attention of organic chemists due to their importance as therapeutic agent in pharmaceutical industry. Quinolone molecule exhibit extensive biological activities a few of which are antiviral, anti-inflammatory antibacterial, antifungal, antiproliferative, anthelmintic and anticonvulsant. A variety of synthetic routes has been developed for construction compounds bearing quinoline nucleus due to its broad spectrum of pharmacological activities. This review describes recent development in transition metal mediated synthetic protocols of these important heterocycles by formation of quinoline ring or by substitution of quinoline rings including both modified conventional name reactions and novel routes with highly functionalized quinoline products.

scholarly journals Traditional Uses, Chemical Constituents, and Biological Activities ofBixa orellanaL.: A Review

2014 ◽  
Vol 2014 ◽  
pp. 1-11 ◽  
Author(s):  
Daniela de Araújo Vilar ◽  
Marina Suênia de Araujo Vilar ◽  
Túlio Flávio Accioly de Lima e Moura ◽  
Fernanda Nervo Raffin ◽  
Márcia Rosa de Oliveira ◽  
...  
Keyword(s):  
Systematic Review ◽  
Therapeutic Agent ◽  
Biological Activities ◽  
Chemical Constituents ◽  
Indigenous Communities ◽  
Pharmaceutical Products ◽  
Biological Applications ◽  
Bixa Orellana ◽  
American Continent ◽  
Potential Use

Bixa orellanaL., popularly known as “urucum,” has been used by indigenous communities in Brazil and other tropical countries for several biological applications, which indicates its potential use as an active ingredient in pharmaceutical products. The aim of this work was to report the main evidence found in the literature, concerning the ethnopharmacology, the biological activity, and the phytochemistry studies related toBixa orellanaL. Therefore, this work comprises a systematic review about the use ofBixa orellanain the American continent and analysis of the data collected. This study shows the well-characterized pharmacological actions that may be considered relevant for the future development of an innovative therapeutic agent.

Synthetic Routes for 1,4-disubstituted 1,2,3-triazoles: A Review

2019 ◽  
Vol 23 (8) ◽  
pp. 860-900 ◽  
Author(s):  
Chander P. Kaushik ◽  
Jyoti Sangwan ◽  
Raj Luxmi ◽  
Krishan Kumar ◽  
Ashima Pahwa
Keyword(s):  
Solid Phase ◽  
Click Reaction ◽  
Biological Activities ◽  
Triazole Ring ◽  
Copper Catalysts ◽  
Biologically Active ◽  
Pharmaceutical Chemistry ◽  
Biological Targets ◽  
Synthetic Routes ◽  
High Yields

N-Heterocyclic compounds like 1,2,3-triazoles serve as a key scaffolds among organic compounds having diverse applications in the field of drug discovery, bioconjugation, material science, liquid crystals, pharmaceutical chemistry and solid phase organic synthesis. Various drugs containing 1,2,3-triazole ring which are commonly available in market includes Rufinamide, Cefatrizine, Tazobactam etc., Stability to acidic/basic hydrolysis along with significant dipole moment support triazole moiety for appreciable participation in hydrogen bonding and dipole-dipole interactions with biological targets. Huisgen 1,3-dipolar azide-alkyne cycloaddition culminate into a mixture of 1,4 and 1,5- disubstituted 1,2,3-triazoles. In 2001, Sharpless and Meldal came across with a copper(I) catalyzed regioselective synthesis of 1,4-disubstituted 1,2,3-triazoles by cycloaddition between azides and terminal alkynes. This azide-alkyne cycloaddition has been labelled as a one of the important key click reaction. Click synthesis describes chemical reactions that are simple to perform, gives high selectivity, wide in scope, fast reaction rate and high yields. Click reactions are not single specific reaction, but serve as a pathway for construction of simple to complex molecules from a variety of starting materials. In the last few decades, 1,2,3-triazoles attracted attention of researchers all over the world because of their broad spectrum of biological activities. Keeping in view the biological importance of 1,2,3-triazole, in this review we focus on the various synthetic routes for the syntheisis of 1,4-disubstituted 1,2,3-triazoles. This review involves various synthetic protocols which involves copper and non-copper catalysts, different solvents as well as substrates. It will boost synthetic chemists to explore new pathway for the development of newer biologically active 1,2,3-triazoles.

Potentials of Diphenyl Ether Scaffold as a Therapeutic Agent: A Review

2019 ◽  
Vol 19 (17) ◽  
pp. 1392-1406
Author(s):  
Suvarna G. Kini ◽  
Ekta Rathi ◽  
Avinash Kumar ◽  
Varadaraj Bhat
Keyword(s):  
Therapeutic Agent ◽  
Diphenyl Ether ◽  
Biological Properties ◽  
Industrial Applications ◽  
Synthetic Route ◽  
Structure Activity ◽  
Diphenyl Ethers ◽  
Antiviral Activities ◽  
Synthetic Routes ◽  
The 19Th Century

Diphenyl ethers (DPE) and its analogs have exhibited excellent potential for therapeutic and industrial applications. Since the 19th century, intensive research is perpetuating on the synthetic routes and biological properties of DPEs. Few well-known DPEs are Nimesulide, Fenclofenac, Triclosan, Sorafenib, MK-4965, and MK-1439 which have shown the potential of this moiety as a lead scaffold for different pharmacological properties. In this review, we recapitulate the diverse synthetic route of DPE moiety inclusive of merits and demerits over the classical synthetic route and how this moiety sparked an interest in researchers to discern the SAR (Structure Activity Relationship) for the development of diversified biological properties of DPEs such as antimicrobial, antifungal, antiinflammatory & antiviral activities.

1,4-Diazepines: A Review on Synthesis, Reactions and Biological Significance

2019 ◽  
Vol 16 (5) ◽  
pp. 709-729 ◽  
Author(s):  
Muhammad A. Rashid ◽  
Aisha Ashraf ◽  
Sahibzada S. Rehman ◽  
Shaukat A. Shahid ◽  
Adeel Mahmood ◽  
...  
Keyword(s):  
Biological Activities ◽  
Biological Significance ◽  
Biological Evaluation ◽  
Wide Range ◽  
Pharmaceutical Industries ◽  
Biological Aspects ◽  
Synthetic Routes ◽  
Biological Attributes ◽  
Synthesis Reactions ◽  
Potential Use

Background:1,4-Diazepines are two nitrogen containing seven membered heterocyclic compounds and associated with a wide range of biological activities. Due to its medicinal importance, scientists are actively involved in the synthesis, reactions and biological evaluation of 1,4-diazepines since number of decades.Objective:The primary purpose of this review is to discuss the synthetic schemes and reactivity of 1,4- diazepines. This article also describes biological aspects of 1,4-diazepine derivatives, that can be usefully exploited for the pharmaceutical sector.Conclusion:This review summarizes the abundant literature on synthetic routes, chemical reactions and biological attributes of 1,4-diazepine derivatives. We concluded that 1,4-diazepines have significant importance due to their biological activities like antipsychotic, anxiolytic, anthelmintic, anticonvulsant, antibacterial, antifungal and anticancer. 1,4-diazepine derivatives with significant biological activities could be explored for potential use in the pharmaceutical industries.

scholarly journals Oral Antibiotic for Empirical Management of Acute Dentoalveolar Infections—A Systematic Review

Antibiotics ◽  
2021 ◽  
Vol 10 (3) ◽  
pp. 240
Author(s):  
Leanne Teoh ◽  
Monique C Cheung ◽  
Stuart Dashper ◽  
Rodney James ◽  
Michael J McCullough
Keyword(s):  
Systematic Review ◽  
Clinical Outcomes ◽  
Broad Spectrum ◽  
Dental Treatment ◽  
Clinical Success ◽  
Empirical Therapy ◽  
Oral Antibiotic ◽  
Dose Frequency ◽  
Odontogenic Infections ◽  
Broad Spectrum Antibiotics

Concerns regarding increasing antibiotic resistance raise the question of the most appropriate oral antibiotic for empirical therapy in dentistry. The aim of this systematic review was to investigate the antibiotic choices and regimens used to manage acute dentoalveolar infections and their clinical outcomes. A systematic review was undertaken across three databases. Two authors independently screened and quality-assessed the included studies and extracted the antibiotic regimens used and the clinical outcomes. Searches identified 2994 studies, and after screening and quality assessment, 8 studies were included. In addition to incision and drainage, the antibiotics used to manage dentoalveolar infections included amoxicillin, amoxicillin/clavulanic acid, cefalexin, clindamycin, erythromycin, metronidazole, moxifloxacin, ornidazole and phenoxymethylpenicillin. Regimens varied in dose, frequency and duration. The vast majority of regimens showed clinical success. One study showed that patients who did not receive any antibiotics had the same clinical outcomes as patients who received broad-spectrum antibiotics. The ideal choice, regimen and spectrum of empirical oral antibiotics as adjunctive management of acute dentoalveolar infections are unclear. Given that all regimens showed clinical success, broad-spectrum antibiotics as first-line empirical therapy are unnecessary. Narrow-spectrum agents appear to be as effective in an otherwise healthy individual. This review highlights the effectiveness of dental treatment to address the source of infection as being the primary factor in the successful management of dentoalveolar abscesses. Furthermore, the role of antibiotics is questioned in primary space odontogenic infections, if drainage can be established.

scholarly journals Fludarabine Inhibits Infection of Zika Virus, SFTS Phlebovirus, and Enterovirus A71

Viruses ◽  
2021 ◽  
Vol 13 (5) ◽  
pp. 774
Author(s):  
Chengfeng Gao ◽  
Chunxia Wen ◽  
Zhifeng Li ◽  
Shuhan Lin ◽  
Shu Gao ◽  
...  
Keyword(s):  
Broad Spectrum ◽  
Zika Virus ◽  
Therapeutic Agent ◽  
Viral Infections ◽  
Rna Virus ◽  
Emerging Viruses ◽  
Enterovirus A71 ◽  
Ic50 Values ◽  
High Doses ◽  
Severe Fever

Viral infections are one of the leading causes in human mortality and disease. Broad-spectrum antiviral drugs are a powerful weapon against new and re-emerging viruses. However, viral resistance to existing broad-spectrum antivirals remains a challenge, which demands development of new broad-spectrum therapeutics. In this report, we showed that fludarabine, a fluorinated purine analogue, effectively inhibited infection of RNA viruses, including Zika virus, Severe fever with thrombocytopenia syndrome virus, and Enterovirus A71, with all IC50 values below 1 μM in Vero, BHK21, U251 MG, and HMC3 cells. We observed that fludarabine has shown cytotoxicity to these cells only at high doses indicating it could be safe for future clinical use if approved. In conclusion, this study suggests that fludarabine could be developed as a potential broad-spectrum anti-RNA virus therapeutic agent.

scholarly journals Non-Nucleoside Agonists of the Adenosine Receptors: An Overview

2019 ◽  
Vol 12 (4) ◽  
pp. 150 ◽  
Author(s):  
Dal Ben ◽  
Lambertucci ◽  
Buccioni ◽  
Martí Navia ◽  
Marucci ◽  
...  
Keyword(s):  
Adenosine Receptors ◽  
Biological Activities ◽  
Great Majority ◽  
Synthetic Route ◽  
Wide Range ◽  
Pharmacological Interest ◽  
Molecular Modeling Studies ◽  
Synthetic Routes ◽  
Alternative Set ◽  
Structural Classes

Potent and selective adenosine receptor (AR) agonists are of pharmacological interest for the treatment of a wide range of diseases and conditions. Among these derivatives, nucleoside-based agonists represent the great majority of molecules developed and reported to date. However, the limited availability of compounds selective for a specific AR subtype (i.e., A2BAR) and a generally long and complex synthetic route for largely substituted nucleosides are the main drawbacks of this category of molecules. Non-nucleoside agonists represent an alternative set of compounds able to stimulate the AR function and based on simplified structures. This review provides an updated overview on the structural classes of non-nucleoside AR agonists and their biological activities, with emphasis on the main derivatives reported in the literature. A focus is also given to the synthetic routes employed to develop these derivatives and on molecular modeling studies simulating their interaction with ARs.

scholarly journals Traditional, phytochemical, and biological aspects of Rosa alba L.: a systematic review

2020 ◽  
Vol 6 (1) ◽  
Author(s):  
Anju Verma ◽  
Rajni Srivastava ◽  
Pankaj Kumar Sonar ◽  
Ramprakash Yadav
Keyword(s):  
Systematic Review ◽  
Biological Activities ◽  
Chemical Constituents ◽  
Research Work ◽  
Biological Properties ◽  
Medicinal And Aromatic Plants ◽  
Research Papers ◽  
Northwest Africa ◽  
The Family ◽  
White Rose

Abstract Background Rosa alba L. belongs to the family Rosaceae. This species is widely cultivated in Europe, Asia, North America, and Northwest Africa due to its fragrance, ornamental, and medicinal values. It is commonly known as white oil-bearing rose, white rose, white rose of York, backyard rose, and sufaid gulab. Main text Rosa alba L. has many biological properties like antioxidant, antimicrobial, antifungal, antifertility, teratogenic, memory enhancing, cytotoxic, and genotoxic activities. The essential oil of Rosa alba L. possesses good antimicrobial activity and consists of many chemical constituents like- citronellol, geraniol, nerol, linalool, citral, carvacrol, eugenol, etc. Conclusion This article briefly reviews the cultivation, traditional uses, phytochemistry, and biological activities of Rosa alba L. Many research papers have been published on the proposed plant and still, there is a very vast scope of research on it. Therefore, this review will be very fruitful for those scientists who are doing or plan to do research work on this plant. All the scientific findings written in this review are explored from Google web, Google Scholar, PubMed, ScienceDirect, Medicinal and Aromatic Plants Abstracts (MAPA), and SciFinder. To date, it is the first systematic review article of such kind, on this plant.

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