Recent Advancement of Pyrazole Scaffold Based Neuroprotective Agents: A Review

2021 ◽  
Vol 20 ◽  
Author(s):  
Subham Das ◽  
Saleem Akbar ◽  
Bahar Ahmed ◽  
Rikeshwar Prasad Dewangan ◽  
Mohammad Kashif Iqubal ◽  
...  
Keyword(s):  
Biological Activities ◽  
Neuroprotective Agents ◽  
Wide Range ◽  
Recent Developments ◽  
Ic50 Values ◽  
Structural Activity Relationship ◽  
Pharmaceutical Industries ◽  
Neurological Conditions ◽  
Nitrogen Containing Compounds

: As a source of therapeutic agents, heterocyclic nitrogen-containing compounds and their derivatives are still interesting and essential. Pyrazole, a five-member heteroaromatic ring with two nitrogen atoms, has a major impact on chemical industries as well as pharmaceutical industries. Due to its wide range of biological activities against various diseases, it has been identified as a biologically important heterocyclic scaffold. The treatment of neurological disorders has always been a difficult task. Therefore, identifying therapeutically effective molecules for neurological conditions remains an open challenge in biomedical research and development. For developing novel entities as neuroprotective agents, recently, pyrazole scaffold has attracted medicinal chemists worldwide. The major focus of research in this area is to discover novel molecules as neuroprotective agents with minimal adverse effects and better effectiveness in improving the neurological condition. This review mainly covers recent developments in the neuropharmacological role of pyrazole incorporated compounds, including their structural-activity relationship (SAR), which also further includes IC50 values (in mM as well as in μM), recent patents, and a brief history as neuroprotective agents.

Recent Developments on Synthesis of Indole Derivatives Through Green Approaches and Their Pharmaceutical Applications

2020 ◽  
Vol 24 (22) ◽  
pp. 2665-2693
Author(s):  
Dipayan Mondal ◽  
Pankaj Lal Kalar ◽  
Shivam Kori ◽  
Shovanlal Gayen ◽  
Kalpataru Das
Keyword(s):  
Biological Activities ◽  
Synthetic Methods ◽  
Pharmaceutical Chemistry ◽  
Indole Derivatives ◽  
Biological Studies ◽  
Recent Developments ◽  
Pharmaceutical Industries ◽  
Green Methodology ◽  
Conventional Methods ◽  
High Yields

Indole moiety is often found in different classes of pharmaceutically active molecules having various biological activities including anticancer, anti-viral, anti-psychotic, antihypertensive, anti-migraine, anti-arthritis and analgesic activities. Due to enormous applications of indole derivatives in pharmaceutical chemistry, a number of conventional synthetic methods as well as green methodology have been developed for their synthesis. Green methodology has many advantages including high yields, short reaction time, and inexpensive reagents, highly efficient and environmentally benign over conventional methods. Currently, the researchers in academia as well as in pharmaceutical industries have been developing various methods for the chemical synthesis of indole based compounds via green approaches to overcome the drawbacks of conventional methods. This review reflects the last ten years developments of the various greener methods for the synthesis of indole derivatives by using microwave, ionic liquids, water, ultrasound, nanocatalyst, green catalyst, multicomponent reaction and solvent-free reactions etc. (please see the scheme below). Furthermore, the applications of green chemistry towards developments of indole containing pharmaceuticals and their biological studies have been represented in this review.

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.

Synthesis, Antioxidant and Antiurease Activities of Some New 5,6- dichloro-2-(4-fluorobenzyl)-1H-benzimidazole Derivatives Containing Furan, Oxadiazole, Triazole and Thiadiazole Moieties

2019 ◽  
Vol 16 (8) ◽  
pp. 939-947
Author(s):  
Hakan Bektas ◽  
Canan Albay ◽  
Emre Menteşe ◽  
Bahar Bilgin Sokmen ◽  
Zafer Kurt ◽  
...  
Keyword(s):  
Biological Activities ◽  
Benzimidazole Derivatives ◽  
Wide Range ◽  
Ic50 Values ◽  
Urease Inhibitory

Background:Benzimidazoles and its derivatives have been attracting interest for many years because of their biological activities. Benzimidazoles containing different heterocyclic moieties have wide range of biological activities such as antimicrobial, antioxidant, anticancer, antiviral, etc.Methods:In this study, some benzimidazole derivatives containing furan, oxadiazole, triazole and thiadiazole moieties have been synthesized and then evaluated for their antioxidant and antiurease activities.Results:The results showed that all the tested benzimidazoles indicated remarkable urease inhibitory potentials with IC50 values ranging between 0.303±0.03 to 0.591±0.08 µM.Conclusion:In conclusion, synthesized benzimidazole derivatives showed good antioxidant and antiurease activities. Heterocyclic groups on benzimidazole nucleus enhance the activities.

Chain-breaking/Preventive Antioxidant, Urate-lowering, and Anti-inflammatory Effects of Pure Curcumin

2020 ◽  
Vol 17 (1) ◽  
pp. 66-74
Author(s):  
Seghira Bisset ◽  
Widad Sobhi ◽  
Chawki Bensouici ◽  
Abdelhalim Khenchouche
Keyword(s):  
Uric Acid ◽  
Xanthine Oxidase ◽  
Acid Production ◽  
Biological Activities ◽  
Antioxidant Effect ◽  
Metal Chelating ◽  
Wide Range ◽  
Chain Breaking ◽  
Pharmaceutical Industries ◽  
Anti Inflammatory

Background: Several researches have shown that therapeutic compounds or phytochemicals from natural sources are important in the food as it is valuable in pharmaceutical industries due to their fewer side effects and potent against various diseases. Curcumin, a major polyphenol derived from turmeric spice, which used in many foods, has a wide range of biological activities, with quite a safety. Objective: The goal of this study was to investigate the antioxidant, urate-lowering, and antiinflammatory effects of pure curcumin. Methods: The antioxidant activity was evaluated for chain-breaking antioxidant effect (radicalscavenging and reducing abilities assays) and for preventive antioxidant effect with metal chelating assay, the urate-lowering was assayed on aspectrophotometer by measuring the inhibition of uric acid production by xanthine oxidase (XO) enzyme, and the anti-inflammatory effect was estimated using in vitro albumin denaturation inhibition. Results: Curcumin showed a significant and good chain-breaking antioxidant effect, both in free radical- scavenging assays (Galvinoxyl radical, ABTS, and hydroxyl radical), and in reducing abilities methods (reducing power, Cupric ion reducing antioxidant capacity and O-phenanthroline assays). In preventive antioxidant effect, assessed with the metal chelating assay, curcumin showed significant effect but with high concentration compared with standard. In the xanthine/xanthine oxidase system, curcumin significantly inhibited uric acid production (IC50=0.71 ± 0.06 mg/mL). Regarding antiinflammatory activity, curcumin showed significant inhibition of albumin denaturation with an IC50 value of 1181.69 ± 1.11μg/mL. Conclusion: These results indicated that curcumin showed promising antioxidant, anti-gout and antiinflammatory properties and might be used as potential, natural drugs against oxidative and inflammation- related diseases.

scholarly journals Securitisation gaps: Towards ideational understandings of state weakness

2021 ◽  
pp. 1-20
Author(s):  
Kevork Oskanian
Keyword(s):  
The State ◽  
Collective Knowledge ◽  
State Action ◽  
Role Of The State ◽  
Wide Range ◽  
State And Society ◽  
Interpretive Approach ◽  
Recent Developments ◽  
The Republic

Abstract This article contributes a securitisation-based, interpretive approach to state weakness. The long-dominant positivist approaches to the phenomenon have been extensively criticised for a wide range of deficiencies. Responding to Lemay-Hébert's suggestion of a ‘Durkheimian’, ideational-interpretive approach as a possible alternative, I base my conceptualisation on Migdal's view of state weakness as emerging from a ‘state-in-society's’ contested ‘strategies of survival’. I argue that several recent developments in Securitisation Theory enable it to capture this contested ‘collective knowledge’ on the state: a move away from state-centrism, the development of a contextualised ‘sociological’ version, linkages made between securitisation and legitimacy, and the acknowledgment of ‘securitisations’ as a contested Bourdieusian field. I introduce the concept of ‘securitisation gaps’ – divergences in the security discourses and practices of state and society – as a concept aimed at capturing this contested role of the state, operationalised along two logics (reactive/substitutive) – depending on whether they emerge from securitisations of the state action or inaction – and three intensities (latent, manifest, and violent), depending on the extent to which they involve challenges to state authority. The approach is briefly illustrated through the changing securitisation gaps in the Republic of Lebanon during the 2019–20 ‘October Uprising’.

Role of Enzymes From Microbes in the Treatment of Recalcitrant From Industries

2018 ◽  
pp. 395-420
Author(s):  
Veena Gayathri Krishnaswamy
Keyword(s):  
Fresh Water ◽  
Azo Dyes ◽  
Azo Dye ◽  
Dye Degradation ◽  
Anthropogenic Activities ◽  
Bacterial Degradation ◽  
Wide Range ◽  
Pharmaceutical Industries ◽  
Degradation Of Azo Dye

The limited availability of fresh water is a global crisis. The growing consumption of fresh water due to anthropogenic activities has taken its toll on available water resources. Unfortunately, water bodies are still used as sinks for waste water from domestic and industrial sources. Azo dyes account for the majority of all dye stuffs, produced because they are extensively used in the textile, paper, food, leather, cosmetics, and pharmaceutical industries. Bacterial degradation of azo dyes under certain environmental conditions has gained momentum as a method of treatment, as these are inexpensive, eco-friendly, and can be applied to wide range of such complex dyes. The enzymatic approach has attracted much interest with regard to degradation of azo dyes from wastewater. The oxido-reductive enzymes are responsible for generating highly reactive free radicals that undergo complex series of spontaneous cleavage reactions, due to the susceptibility of enzymes to inactivation in the presence of the other chemicals. The oxidoreductive enzymes, such as lignin peroxidase, laccases, tyrosinase, azoreductase, riboflavin reductive, polyphenol oxidase, and aminopyrine n-demethylase, have been mainly utilized in the bacterial degradation of azo dye. Along with the reductive enzymes, some investigators have demonstrated the involvement in some other enzymes, such as Lignin peroxides and other enzymes. This chapter reviews the importance of enzymes in dye degradation.

scholarly journals The State of Matter in Simulations of Core-Collapse supernovae—Reflections and Recent Developments

2017 ◽  
Vol 34 ◽  
Author(s):  
Tobias Fischer ◽  
Niels-Uwe Bastian ◽  
David Blaschke ◽  
Mateusz Cierniak ◽  
Matthias Hempel ◽  
...  
Keyword(s):  
Equation Of State ◽  
Degrees Of Freedom ◽  
The State ◽  
Core Collapse ◽  
Heavy Nuclei ◽  
Isospin Asymmetry ◽  
Wide Range ◽  
Recent Developments ◽  
State Of Matter

AbstractIn this review article, we discuss selected developments regarding the role of the equation of state in simulations of core-collapse supernovae. There are no first-principle calculations of the state of matter under supernova conditions since a wide range of conditions is covered, in terms of density, temperature, and isospin asymmetry. Instead, model equation of state are commonly employed in supernova studies. These can be divided into regimes with intrinsically different degrees of freedom: heavy nuclei at low temperatures, inhomogeneous nuclear matter where light and heavy nuclei coexist together with unbound nucleons, and the transition to homogeneous matter at high densities and temperatures. In this article, we discuss each of these phases with particular view on their role in supernova simulations.

scholarly journals The Pathological Mechanisms of Estrogen-Induced Cholestasis: Current Perspectives

2021 ◽  
Vol 12 ◽  
Author(s):  
Yue Zu ◽  
Jinyu Yang ◽  
Chengliang Zhang ◽  
Dong Liu
Keyword(s):  
Intrahepatic Cholestasis ◽  
Fetal Death ◽  
Inflammatory Responses ◽  
Biological Activities ◽  
Hormone Replacement ◽  
Intrauterine Fetal Death ◽  
Wide Range ◽  
Cell Membrane Fluidity ◽  
Meconium Stained Amniotic Fluid

Estrogens are steroid hormones with a wide range of biological activities. The excess of estrogens can lead to decreased bile flow, toxic bile acid (BA) accumulation, subsequently causing intrahepatic cholestasis. Estrogen-induced cholestasis (EIC) may have increased incidence during pregnancy, and within women taking oral contraception and postmenopausal hormone replacement therapy, and result in liver injury, preterm birth, meconium-stained amniotic fluid, and intrauterine fetal death in pregnant women. The main pathogenic mechanisms of EIC may include deregulation of BA synthetic or metabolic enzymes, and BA transporters. In addition, impaired cell membrane fluidity, inflammatory responses and change of hepatocyte tight junctions are also involved in the pathogenesis of EIC. In this article, we review the role of estrogens in intrahepatic cholestasis, and outlined the mechanisms of EIC, providing a greater understanding of this disease.

scholarly journals Synthesis of Novel 2-(Pyridin-2-yl) Pyrimidine Derivatives and Study of Their Anti-Fibrosis Activity

Molecules ◽  
2020 ◽  
Vol 25 (22) ◽  
pp. 5226
Author(s):  
Yi-Fei Gu ◽  
Yue Zhang ◽  
Feng-li Yue ◽  
Shao-tong Li ◽  
Zhuo-qi Zhang ◽  
...  
Keyword(s):  
Biological Activities ◽  
Collagen Type I ◽  
Type I ◽  
The Novel ◽  
Pyrimidine Derivatives ◽  
Wide Range ◽  
Ic50 Values ◽  
Privileged Structures ◽  
Pyrimidine Moiety

A pyrimidine moiety exhibiting a wide range of pharmacological activities has been employed in the design of privileged structures in medicinal chemistry. To prepare libraries of novel heterocyclic compounds with potential biological activities, a series of novel 2-(pyridin-2-yl) pyrimidine derivatives were designed, synthesized and their biological activities were evaluated against immortalized rat hepatic stellate cells (HSC-T6). Fourteen compounds were found to present better anti-fibrotic activities than Pirfenidone and Bipy55′DC. Among them, compounds ethyl 6-(5-(p-tolylcarbamoyl)pyrimidin-2-yl)nicotinate (12m) and ethyl 6-(5-((3,4-difluorophenyl)carbamoyl)pyrimidin-2-yl)nicotinate (12q) show the best activities with IC50 values of 45.69 μM and 45.81 μM, respectively. Furthermore, the study of anti-fibrosis activity was evaluated by Picro-Sirius red staining, hydroxyproline assay and ELISA detection of Collagen type I alpha 1 (COL1A1) protein expression. Our study showed that compounds 12m and 12q effectively inhibited the expression of collagen, and the content of hydroxyproline in cell culture medium in vitro, indicating that compounds 12m and 12q might be developed the novel anti-fibrotic drugs.

Anti-angiogenesis Potential of Phytochemicals for the Therapeutic Management of Tumors

2020 ◽  
Vol 26 (2) ◽  
pp. 265-278 ◽  
Author(s):  
Samman Munir ◽  
Asad A. Shah ◽  
Muhammad Shahid ◽  
Muhammad S. Ahmed ◽  
Aqsa Shahid ◽  
...  
Keyword(s):  
Cellular Proliferation ◽  
Angiogenesis Inhibitors ◽  
Metastatic Potential ◽  
Biologically Active ◽  
Angiogenic Potential ◽  
Recent Developments ◽  
Pharmaceutical Industries ◽  
Pathological Stages

The role of angiogeneses during the growth and progression of tumors is well documented. Likewise, a balance is generally maintained between the cellular proliferation and the apoptosis, therefore, the tumors can persist for years in a dormant phase. During the past few years, many hypotheses have been proposed relating to the importance of tumor angiogenesis for the development and spread of tumors and preventive or therapeutic capacity of angiogenesis inhibitors as a potential target for controlling the growth of cancerous tissue. The antiangiogenic based therapeutic approaches are considered as the most promising method for the control of tumors, as this therapeutic approach is less likely to attain the drug resistance. Further, the tumor vasculature is an important prognostic marker that can independently predict the pathological stages as well as the metastatic potential of tumors. Various biologically active phytochemicals have been extracted from the dietary sources and the plants that have engaged the scientist and pharmaceutical industries around the globe. The antioxidant, antiinflammatory, anti-proliferative and anti-angiogenic potential of these bioactive phytochemicals is evident from the in vitro studies using cell lines and investigations involving the animal models..The present review is focused on the promising role of anti-angiogenesis-based therapies for the management of tumors and the recent developments relating to the interplay of phytochemicals and angiogenesis for the suppression of tumor cells.

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