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- Volume 21, Issue 1, 2024
Letters in Drug Design & Discovery - Volume 21, Issue 1, 2024
Volume 21, Issue 1, 2024
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HDAC Inhibitors against SARS-CoV-2
Authors: Negar Omidkhah, Farzin Hadizadeh and Razieh GhodsiFollowing the coronavirus outbreak, global efforts to find a vaccine and drug affecting Covid- 19 have been widespread. Reusing some of the available drugs has had relatively satisfactory results. One of the classes of drugs studied against SARS-CoV-2 is the HDAC inhibitors collected in this review. Among the most important points of this study can be mentioned: (a) SARS-COV-2 infection can influence the ACE/ACE2-ATR1-C Read More
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A Review on Synthesis and Biological Potential of Dihydropyridines
Authors: Shilpi Pathak, Supriya Jain and Abhishek PratapDihydropyridine is an outstanding heterocyclic compound with a wide range of pharmacological potential, including antimicrobial, antioxidant, antitubercular, antiarrhythmic, insecticidal, antihypertensive, vasodilator, anti-inflammatory, antibacterial, antidiabetic and superlative moiety in drug discovery. It is also a versatile pharmacophore, a privileged scaffold, and a distinguished heterocyclic compound. Excellent outcom Read More
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Nature-derived Alkaloids as a Promising Bioactive Compound in Drug Discovery to Meet Global Leishmania Needs
Authors: Fatemeh Sharifi, Neda Mohamadi, Ardavan Abiri, Iraj Sharifi, Majid F. Harandi and Fariba SharififarBackground: Natural products have been important resources for potential drug development. Among the many classes of natural products, alkaloids have the most therapeutic applications. Treatment of leishmaniasis by chemical drugs remains a challenge because of toxic side effects, limited efficacy, and drug resistance. This review focuses to embrace all researches on leishmanicidal alkaloids over a specific range of t Read More
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An Insight into the Role of Biodegradable Controlled-release Polymers and Nanoformulations for Enhanced Brain Drug Delivery
More LessNeurological or brain disorders are increasingly recognized as major causes of death and disability worldwide, eventually leading to the burden of non-communicable and communicable diseases in the world. Biodegradable functions of polymers provide promising solutions to meet the therapeutic needs of neurological disorders owing to advantages such as the usage of biodegradable polymers in drug delivery approac Read More
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Synthetic and Pharmacological Expedition of Pyrazolo[1,5-a]pyridine: A Comprehensive Review
Authors: Neetu Agrawal, Dimple Bansal and Vertika GautamFused nitrogen-containing heterocyclic compounds have been identified to display a prominent role in medicinal chemistry, biochemistry, and other streams of science. Countless derivatives of pyrazolo[ 1,5-a] pyridine have been investigated by researchers for their distinct pharmacological characterization. In this article, we have revealed and arranged the various routes of synthesis and therapeutic activities such as dopam Read More
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Network Pharmacology-Based Prediction of Active Ingredients and Mechanisms of Zanthoxyli Bungeanum Against Lung Carcinoma
Authors: Qian Yang, Xiao-peng Shi, Shanbo Ma, Yuhan Chen, Jin Wang, Long Li and Shan MiaoBackground: Zanthoxyli Bungeanum (ZB) has been reported to have an effect on lung carcinoma (LC). However, the defined pharmacological mechanism of ZB on LC has not been expounded completely because of the complicated ingredients.Objective: The aim of this work was to explore the active ingredients and mechanisms of ZB against LC by network pharmacology.Methods: In this study, systemic network pharmacolo Read More
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N-function Heterocycles as Promising Anticancer Agents: A Case Study with a Decision Model in a Fuzzy Environment
Authors: Merve Bulut, Salih Ökten, Evrencan Özcan and Tamer ErenObjective: This study aimed to evaluate the data according to five accepted criteria for the effects of twenty promising anticancer agents on five different cancer types and determine the most effective compounds for further in vitro and in vivo studies with a multi-criteria decision-making method (MCDM), which rationalizes decision making in a fuzzy environment to avoid the high cost and time requirements of further prec Read More
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QSAR of SARS-CoV-2 Main Protease Inhibitors Utilizing Theoretical Molecular Descriptors
Authors: Sisir Nandi, Mohit Kumar and Anil K. SaxenaBackground: COVID-19 is caused by a novel strain of severe acute respiratory syndrome coronaviruses (SARS-CoV-2). It has claimed casualties around the world since the end of 2019 due to its high virulence and quick multiplicity in the human body. Hence, there has been a requirement to develop effective remedial measures to mitigate the mortality. Scientists have been able to develop corona vaccines to provide immunit Read More
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An Ultrasound-assisted Three Component Protocol for the Regio and Stereo-selective Synthesis of Some Novel Dispiroheterocycles and Their Biological Evaluation as Anti-inflammatory, Anti-obesity Agents
Authors: Sanjeev Kumar, Bhavna Saroha, Ekta Lathwal, Gourav Kumar, Suresh Kumar, Ramesh Kumar, Priyanka Arya and Neera RaghavBackground: The increasing utilization of spiro compounds in drug discovery, led us to design and synthesize regioselectively some novel dispiroheterocycles, by a standard 1,3-dipolar cycloaddition reaction between 6-hydroxyaurone and in situ generated azomethine ylides, using ultra-sonication as green energy source. These results are first of its kind in the literature reported so far for the similar conditions. After Read More
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The Anticancer Potentials of Substituted Indeno[1,2-b]quinoline Amines against HT29 and SW620: Experimental and In silico Approach
Authors: Salih Ökten, Ali Aydın, Sultan Erkan and Ahmet TutarBackground: This study aimed the determination of the antiproliferative and cytotoxic activities of recently prepared indeno [1,2-b]quinoline amines against colon carcinoma, HT29 and SW620 cell lines by using cell proliferation and cytotoxicity assays.Methods: In vitro inhibition of cell proliferation of indenoquinoline derivatives was determined with an MTT cell proliferation assay. On the other hand, their cell cytotoxicities and apopt Read More
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Neuroprotective Cognitive Effects of Nose-to-brain Delivered Linagliptin Loaded Polymeric Nanosuspension in Animal Model
Authors: Deepika Joshi, Bhavna Kumar, Manmohan Singhal, Samir Bhargava and Kaul AnkurObjective: Insulin resistance is a common link between diabetes mellitus (DM) and dementia. The current work emphasizes the effect of linagliptin on dementia with its neuroprotective effects, which occur directly at the neuronal level, as GLP-1 receptors are exclusively expressed in neurons.Methods: The objective of the study was to formulate linagliptin-loaded polymeric nanosuspension (LS) by nanoprecipitation me Read More
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Buddleoside Inhibits Progression of Liver Cancer by Regulating NFΚB Signaling Pathway
Authors: Li Zhang, Lizhi Sun, Shuchun Gao, Weihua Yang, Yuanmei Zhuang and Mingjie XuBackground: Liver cancer is a severe incurable disease and causes several thousands of deaths each year. Flavonoids are a class of bioactive compounds possessing anti-cancer activity.Objective: The objective of this study is to investigate the role of Buddleoside, one type of flavonoids, in carcinogenesis of liver cancer.Methods: Cell proliferation was detected by CCK-8 method, while cell invasion was by transwell assay, cell Read More
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Analysis of Ultrasound Supported Antimicrobial and Antibiofilm Activities of Disinfection By-product Bromochloroacetonitrile
By Sevda E.R.Introduction: Some microorganism threaten human health by forming biofilm in water systems. Because microorganism in the biofilm structure are more resistant to antimicrobials.Methods: Water systems are disinfected with physical methods, such as ultrasonication techniques and chemical disinfectants. Bromochloroacetonitrile is produced as a by-product from algae and fulvic acid sources during water chlorination. This stu Read More
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Neuroprotective Potential of Polydatin in Combating Parkinson's Disease through the Inhibition of Monoamine Oxidase-B and Catechol-o-Methyl Transferase
Authors: Banashree C. Phukan, Rubina Roy, Shuvasish Choudhury, Pallab Bhattacharya and Anupom BorahAims: This study aims to deduce the plausible contribution of polydatin in dopamine replenishment and dopaminergic neuroprotection to unveil its potential as a drug candidate for Parkinson's disease (PD).Background: Available therapies for the management of dopaminergic degradation in PD provide only symptomatic relief and are associated with various adverse effects. Levodopa (L-DOPA) is an age-old therapy in the treatm Read More
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Formulation and Characterization Studies of Paclitaxel Incorporated Kollidon® SR and Chitosan Nanoparticles: An In vitro Evaluation for Potential Use for Colorectal Cancer Treatment
Authors: Özge A. Koca, Gülay Büyükköroğlu and Ebru BaşaranBackground: Chemotherapy is regarded as first-line therapy in various cancer types besides surgical procedures. However, lack of cell selectivity and poor drug targeting to the cancer zone of the active agents results in accumulation in normal tissues with considerably high severe side effects. Therefore, novel drug delivery systems are required to enhance cancer treatment.Objective: In this study, Paclitaxel (PTX) incorporated Read More
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Volumes & issues
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Volume 21 (2024)
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Volume 20 (2023)
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Volume 19 (2022)
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Volume 18 (2021)
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Volume 17 (2020)
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Volume 16 (2019)
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Volume 15 (2018)
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Volume 14 (2017)
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Volume 13 (2016)
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Volume 12 (2015)
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Volume 11 (2014)
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Volume 10 (2013)
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Volume 9 (2012)
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Volume 8 (2011)
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Volume 7 (2010)
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Volume 6 (2009)
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Volume 5 (2008)
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Volume 4 (2007)
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Volume 3 (2006)
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Volume 2 (2005)
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Volume 1 (2004)
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