Current Updates on Oxazolidinone and Its Significance

Oxazolidinone is a five-member heterocyclic ring exhibiting potential medicinal properties with preferential antibacterial activity. Scientists reported various synthetic procedures for this heterocyclic structure. Current review articles tried to cover each and every potential aspect of oxazolidinone like synthetic routes, pharmacological mechanism of action, medicinal properties, and current research activities.

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Review: Studies on the Synthesis of Quinolone Derivatives with Their Antibacterial Activity (Part 1)

Current Organic Chemistry ◽

10.2174/1385272824999200427082108 ◽

2020 ◽

Vol 24 (8) ◽

pp. 817-854

Author(s):

Anil Kumar ◽

Nishtha Saxena ◽

Arti Mehrotra ◽

Nivedita Srivastava

Keyword(s):

Antibacterial Activity ◽

Antibacterial Properties ◽

Structure Activity Relationship ◽

New Drugs ◽

Activity Relationship ◽

Structure Activity ◽

Medicinal Properties ◽

Synthetic Routes ◽

Quinolone Derivatives

Quinolone derivatives have attracted considerable attention due to their medicinal properties. This review covers many synthetic routes of quinolones preparation with their antibacterial properties. Detailed study with structure-activity relationship among quinolone derivatives will be helpful in designing new drugs in this field.

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Diversified Synthetic Pathway of 1, 4-Dihydropyridines: A Class of Pharmacologically Important Molecules

Mini-Reviews in Medicinal Chemistry ◽

10.2174/1389557520666200807130215 ◽

2020 ◽

Vol 20 ◽

Author(s):

Shubham Khot ◽

Pratibha B. Auti ◽

Samrat A. Khedkar

Keyword(s):

Pharmacological Action ◽

Heterocyclic Ring ◽

Channel Blockers ◽

Transmembrane Conductance Regulator ◽

Transmembrane Conductance ◽

Current Review ◽

Regulator Protein ◽

Cystic Fibrosis Transmembrane ◽

Hiv 1 ◽

Dihydropyridine Derivatives

: The current review discusses the different synthetic pathways for one of the most important and interesting heterocyclic ring systems 1,4-dihydropyridine. This cyclic system depicts diverse pharmacological action at several receptors, channels, and enzymes. Dihydropyridine moiety plays an important role in several calcium-channel blockers. Moreover, it has been exploited for the treatment of a variety of cardiovascular diseases due to its potential antihypertensive, anti-angina, vasodilator, and cardiac depressant activities. Furthermore, it also shows antibacterial, anticancer, antileishmanial, anticoagulant, anticonvulsant, anti-tubercular, antioxidant, antiulcer, and neuroprotective properties. Several reports have demonstrated dihydropyridine derivatives as a potentiator of cystic fibrosis transmembrane conductance regulator protein, potent antimalarial agent and HIV-1 protease inhibitor. Herein, we have briefly reviewed different novel chemistry and synthesis of 1,4-dihydropyridine.

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Proteomic response of Escherichia coli to a membrane lytic and iron chelating truncated Amaranthus tricolor defensin

BMC Microbiology ◽

10.1186/s12866-021-02176-4 ◽

2021 ◽

Vol 21 (1) ◽

Author(s):

Tessa B. Moyer ◽

Ashleigh L. Purvis ◽

Andrew J. Wommack ◽

Leslie M. Hicks

Keyword(s):

Escherichia Coli ◽

Antibacterial Activity ◽

Antimicrobial Peptides ◽

Mechanism Of Action ◽

Gram Negative Bacteria ◽

Amaranthus Tricolor ◽

Core Motif ◽

Gram Negative ◽

E Coli ◽

Membrane Lysis

Abstract Background Plant defensins are a broadly distributed family of antimicrobial peptides which have been primarily studied for agriculturally relevant antifungal activity. Recent studies have probed defensins against Gram-negative bacteria revealing evidence for multiple mechanisms of action including membrane lysis and ribosomal inhibition. Herein, a truncated synthetic analog containing the γ-core motif of Amaranthus tricolor DEF2 (Atr-DEF2) reveals Gram-negative antibacterial activity and its mechanism of action is probed via proteomics, outer membrane permeability studies, and iron reduction/chelation assays. Results Atr-DEF2(G39-C54) demonstrated activity against two Gram-negative human bacterial pathogens, Escherichia coli and Klebsiella pneumoniae. Quantitative proteomics revealed changes in the E. coli proteome in response to treatment of sub-lethal concentrations of the truncated defensin, including bacterial outer membrane (OM) and iron acquisition/processing related proteins. Modification of OM charge is a common response of Gram-negative bacteria to membrane lytic antimicrobial peptides (AMPs) to reduce electrostatic interactions, and this mechanism of action was confirmed for Atr-DEF2(G39-C54) via an N-phenylnaphthalen-1-amine uptake assay. Additionally, in vitro assays confirmed the capacity of Atr-DEF2(G39-C54) to reduce Fe3+ and chelate Fe2+ at cell culture relevant concentrations, thus limiting the availability of essential enzymatic cofactors. Conclusions This study highlights the utility of plant defensin γ-core motif synthetic analogs for characterization of novel defensin activity. Proteomic changes in E. coli after treatment with Atr-DEF2(G39-C54) supported the hypothesis that membrane lysis is an important component of γ-core motif mediated antibacterial activity but also emphasized that other properties, such as metal sequestration, may contribute to a multifaceted mechanism of action.

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Organotellurium compounds: an overview of synthetic methodologies

Reviews in Inorganic Chemistry ◽

10.1515/revic-2020-0006 ◽

2020 ◽

Vol 0 (0) ◽

Author(s):

Muhammad Irfan ◽

Rabia Rehman ◽

Mohd. R. Razali ◽

Muhammad Adnan Iqbal ◽

◽

...

Keyword(s):

Material Science ◽

Electrophilic Substitution ◽

Comprehensive Understanding ◽

Substitution Reactions ◽

Current Review ◽

Synthetic Routes ◽

Electrophilic Substitution Reactions ◽

Synthetic Methodologies ◽

Organotellurium Compounds

AbstractIn wake of emerging applications of organotellurium compounds in biological and material science avenues, the current review describes their key synthetic methodologies while focusing the synthesis of organotellurium compounds through five ligand-to-metal linkages including carbon; carbon-oxygen; carbon-nitrogen; carbon-metal; carbon-sulfur to tellurium. In all of these linkages whether tellurium links with ligands through a complicated or simple pathways, it is often governed through electrophilic substitution reactions. The present study encompasses these major synthetic routes so as to acquire comprehensive understanding of synthetic organotellurium compounds.

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Approaches towards the synthesis of 5-aminopyrazoles

Beilstein Journal of Organic Chemistry ◽

10.3762/bjoc.7.25 ◽

2011 ◽

Vol 7 ◽

pp. 179-197 ◽

Cited By ~ 59

Author(s):

Ranjana Aggarwal ◽

Vinod Kumar ◽

Rajiv Kumar ◽

Shiv P Singh

Keyword(s):

Biological Properties ◽

Synthetic Methods ◽

Medicinal Properties ◽

Synthetic Routes

The biological and medicinal properties of 5-aminopyrazoles have prompted enormous research aimed at developing synthetic routes to these heterocyles. This review focuses on the biological properties associated with this system. Various synthetic methods developed up to 2010 for these compounds are described, particularly those that involve the reactions of β-ketonitriles, malononitrile, alkylidenemalononitriles and their derivatives with hydrazines, as well as some novel miscellaneous methods.

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UJI AKTIVITAS ANTIBAKTERI FORMULASI GEL UNTUK SARIAWAN DARI EKSTRAK DAUN SAGA ( Abrus precatorius Linn. ) TERHADAP BAKTERI Staphylococcus aureus

Jurnal Ilmiah Manuntung ◽

10.51352/jim.v2i2.72 ◽

2017 ◽

Vol 2 (2) ◽

pp. 239

Author(s):

Ratih Dyah Pertiwi ◽

Joni Kristanto ◽

Graha Ayu Praptiwi

Keyword(s):

Staphylococcus Aureus ◽

Antibacterial Activity ◽

Chemical Constituents ◽

Optimal Concentration ◽

Diffusion Method ◽

Abrus Precatorius ◽

Agar Diffusion ◽

Medicinal Properties ◽

Agar Diffusion Method ◽

Gel Preparation

One of plants used by Indonesian people as a traditional medicine is saga plant (Abrus precatorius L.). This plant has medicinal properties as medication for thrush, cough and laryngitis. Chemical constituents contained in sage leaves which work as antibacterial are flavonoid and saponin. This study aims to determine the optimal concentration of saga leaves extract which can be formulated in a gel dosage form with qualified physical evaluation and has antibacterial activity against Staphylococcus aureus. Saga leaves extract is prepared by maceration method using ethanol 70% as solvent, and then the extract obtained is preliminarily tested to see its antibacterial activity against Staphylococcus aureus with agar diffusion method. Gel formulation for thrush is made with dispersion method in three formulas with variants of active substance concentration that is FI (1%), FII (3%) and FIII (5%). Gel preparation antibacterial activity test is conducted with agar diffusion method as a plate cylinder. Based on this research, it was found that the extract of saga leaves which is positively made is efficacious as antibacterial and can be formulated into a gel preparation for thrush with optimal concentration in F III (5%), this is indicated by widest diameter of the inhibition area against Staphylococus aureus bacteria

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Triazole As Potent Anti-Cancer Agent- A Pharmacophoric Scaffold

Current Cancer Therapy Reviews ◽

10.2174/1573394717666211006102147 ◽

2021 ◽

Vol 17 ◽

Author(s):

Nidhi Kala ◽

Kalpana Praveen Rahate

Keyword(s):

Characteristic Feature ◽

Biological Activities ◽

Heterocyclic Ring ◽

Ring System ◽

Review Article ◽

Current Review ◽

Anti Cancer ◽

Good Template ◽

Cancer Agent

: Triazole is the main five-membered Nitrogen-containing basic heterocyclic ring system reported for their biological activities and compounds with multiple pharmacophores, which fetch together acquaintance of a target with sympathetic types of the molecule that might interact with the target. In addition, healthy, adaptable, and scalable chemistry must be employed to achieve the task. This characteristic feature of triazole would make a good template for a lead cohort library. The current review article focuses on recent advancements in triazole moiety as an anti-cancer agent with their mechanism pathways of synthesized analogues.

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