scholarly journals Study on the regioselectivity of the N-ethylation reaction of N-benzyl-4-oxo-1,4-dihydroquinoline-3-carboxamide

2019 ◽  
Vol 15 ◽  
pp. 388-400
Author(s):  
Pedro N Batalha ◽  
Luana da S M Forezi ◽  
Maria Clara R Freitas ◽  
Nathalia M de C Tolentino ◽  
Ednilsom Orestes ◽  
...  
Keyword(s):  
Medicinal Chemistry ◽  
Biological Activities ◽  
Organic Substances ◽  
Reaction Paths ◽  
Acid Base ◽  
Pharmacological Activities ◽  
Dft Methods

4-Oxoquinolines are a class of organic substances of great importance in medicinal chemistry, due to their biological and synthetic versatility. N-1-Alkylated-4-oxoquinoline derivatives have been associated with different pharmacological activities such as antibacterial and antiviral. The presence of a carboxamide unit connected to carbon C-3 of the 4-oxoquinoline core has been associated with various biological activities. Experimentally, the N-ethylation reaction of N-benzyl-4-oxo-1,4-dihydroquinoline-3-carboxamide occurs at the nitrogen of the oxoquinoline group, in a regiosselective way. In this work, we employed DFT methods to investigate the regiosselective ethylation reaction of N-benzyl-4-oxo-1,4-dihydroquinoline-3-carboxamide, evaluating its acid/base behavior and possible reaction paths.

scholarly journals Synthesis and Biological Activities of Some Pyrimidine Derivatives: A Review

2020 ◽  
Vol 36 (6) ◽  
pp. 1001-1015
Author(s):  
Nadia Ali Ahmed Elkanzi
Keyword(s):  
Nitrogen Atom ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Heterocyclic Ring ◽  
Ring System ◽  
Pyrimidine Derivatives ◽  
Pharmacological Activities ◽  
Cardiovascular Agents ◽  
Anti Hiv ◽  
Biological And Pharmacological Activities

Nitrogen containing synthetically and biologically important heterocyclic ring system namely pyrimidine possess both biological and pharmacological activities, and defend as aromatic six heterocyclic with 1and 3 nitrogen atom in ring. Preparation of pyrimidine via different methods offer its importance in fields of medicinal chemistry and Chemistry. Pyrimidines and their derivatives act as anti-inflammatory, anti-malaria, anti-tumor, cardiovascular agents, anti-neoplastic, anti-tubercular, anti- HIV, diuretic ,anti-viral, anti-microbial, ,analgesic .This review give light up on biological and pharmacological activities of pyrimidine nucleus.

Green Chemistry Synthesis Methods of Oxazine and Thiazine Derivatives as Promising Scaffolds in Medicinal Chemistry: A Mini-Review

2020 ◽  
Vol 17 ◽  
Author(s):  
Mohammad Asif ◽  
Mohammad Imran
Keyword(s):  
Green Chemistry ◽  
Green Synthesis ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Synthetic Methods ◽  
Bioactive Molecules ◽  
Synthesis Methods ◽  
Design And Development ◽  
Pharmacological Activities ◽  
Oxazine Derivatives

: Green synthesis of oxazine and thiazine derivatives have concerned a great impact of concern of medicinal researchers and provided a lead molecule for the design and development of various potential bioactive molecules. This review associated additional green synthetic information and it would extend a great deal of help to researchers in synthesizing the most productive, economical, and clinically important thiazine and oxazine derivatives which will be expected to show potent pharmacological activities. This has led to the discovery of various compounds that have diverse types of interesting biological activities. Propose of this article is to study the various synthetic methods of oxazine and thiazine derivatives by green chemistry methods and their biological activities. We expect that this article will be interesting for researchers concerned with oxazine and thiazine compounds.

scholarly journals Importance of Fluorine in Benzazole Compounds

Molecules ◽  
2020 ◽  
Vol 25 (20) ◽  
pp. 4677
Author(s):  
Thuraya Al-Harthy ◽  
Wajdi Zoghaib ◽  
Raid Abdel-Jalil
Keyword(s):  
Small Molecules ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Short Review ◽  
Significant Enhancement ◽  
Pharmacological Activities ◽  
The Past ◽  
To Receive

Fluorine-containing heterocycles continue to receive considerable attention due to their unique properties. In medicinal chemistry, the incorporation of fluorine in small molecules imparts a significant enhancement their biological activities compared to non-fluorinated molecules. In this short review, we will highlight the importance of incorporating fluorine as a basic appendage in benzothiazole and benzimidazole skeletons. The chemistry and pharmacological activities of heterocycles containing fluorine during the past years are compiled and discussed.

The Importance of Rhodanine Scaffold in Medicinal Chemistry: A Comprehensive Overview

2020 ◽  
Vol 21 ◽  
Author(s):  
Arif Mermer
Keyword(s):  
Type Ii Diabetes ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Type Ii Diabetes Mellitus ◽  
Mechanisms Of Action ◽  
Type Ii ◽  
Pharmacological Activities ◽  
Comprehensive Overview ◽  
Structure Activity ◽  
Privileged Scaffold

: After the clinical use of epalrestat that contains a rhodanine ring, in type II diabetes mellitus and diabetic complications, rhodanin-based compounds have become an important class of heterocyclic in the field of medicinal chemistry. Various modifications to the rhodanine ring have led to a broad spectrum of biological activity of these compounds. Synthesis of rhodanine derivatives, depended on advenced throughput scanning hits, frequently causes to potent and selective modulators of targeted enzymes or receptors, which apply their pharmacological activities through different mechanisms of action. Rhodanine-based compounds will likely stay a privileged scaffold in drug discovery because of different probability of chemical modifications of the rhodanine ring. We have therefore reviewed their biological activities and structure activity relationship.

Structural Activity Relationship and Importance of Benzothiazole Derivatives in Medicinal Chemistry: A Comprehensive Review

2020 ◽  
Vol 17 (3) ◽  
pp. 323-350
Author(s):  
Mahesh Bhat ◽  
Shiddappa Lagamappa Belagali
Keyword(s):  
Medicinal Chemistry ◽  
Biological Activities ◽  
Bioactive Molecules ◽  
Thiazole Ring ◽  
Structural Variations ◽  
Pharmacological Activities ◽  
Benzothiazole Derivatives ◽  
Methods Of Synthesis ◽  
Structural Activity Relationship ◽  
Interesting Compound

:Benzothiazole (1, 3-benzothiazole) is one of the heterocyclic compounds, which is a weak base having varied biological activities. The unique methine center present in the thiazole ring makes benzothiazole as the most important heterocyclic compound. It is a common and integral structure of many natural and synthetic bioactive molecules. Benzothiazole derivatives show a variety of activities, with less toxic effects and their derivatives showed enhanced activities, which has proven Benzothiazole scaffold as one of the important moieties in medicinal chemistry. Benzothiazole ring containing compounds possess various pharmacological activities such as anti-viral, anti-microbial, antiallergic, anti-diabetic, anti-tumor, anti-inflammatory, anthelmitic and anti-cancer, which makes benzothiazole a rapidly developing and interesting compound in the medicinal chemistry. This review briefly explains the importance, common methods of synthesis of the benzothiazole scaffold and also explains the popular benzothiazole molecules which have applications in various fields of chemistry. A review has been carried out based on various pharmacological activities containing benzothiazole moieties and rationalize the activities based on the structural variations. Literature on benzothiazole derivatives reveals that substitution on the C-2 carbon atom and C-6 are the reasons for a variety of biological activities.

scholarly journals A Review on Five Membered Nitrogen Containing Heterocyclic Compounds with Various Biological Activities

2021 ◽  
Vol 69 (1) ◽  
Author(s):  
incy Joseph ◽  
Meenu C Sanu ◽  
Divya Chacko
Keyword(s):  
Heterocyclic Compounds ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Pharmacological Activities

Heterocyclic compounds are a highly valuable and unique class of compounds. Different heterocyclic analogues have been evaluated for their diverse biological activities. Five membered heterocyclic compounds possess various pharmacological activities. Among them Nitrogen containing five membered heterocyclic compounds have crucial place in medicinal chemistry. This paper aims to review on the pharmacological activities of five membered nitrogen containing heterocyclic compounds.

scholarly journals A Review on Six Membered Nitrogen Containing Heterocyclic Compounds with Various Biological Activities

2021 ◽  
Vol 69 (2) ◽  
Author(s):  
Meenu C Sanu ◽  
Jincy Joseph ◽  
Divya Chacko
Keyword(s):  
Heterocyclic Compounds ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Therapeutic Agents ◽  
Pharmacological Activities ◽  
Valuable Source ◽  
Physiological Properties ◽  
Novel Therapeutic

The heterocycles are currently considered as promising compounds for the development of novel therapeutic agents. The analogs of nitrogen-based heterocycles occupy an exclusive position as a valuable source of therapeutic agents in medicinal chemistry. More than 75% of drugs approved by the FDA and currently available in the market are nitrogen-containing heterocyclic moieties. In the forthcoming decade, a much greater share of new nitrogen-based pharmaceuticals is anticipated. Many new nitrogen-based heterocycles have been designed. The number of novel N-heterocyclic moieties with significant physiological properties and promising applications in medicinal chemistry is ever-growing. This paper aims to review on the pharmacological activities of six membered nitrogen contains heterocyclic compounds.

Potential Triazole-based Molecules for the Treatment of Neglected Diseases

2019 ◽  
Vol 26 (23) ◽  
pp. 4403-4434 ◽  
Author(s):  
Susimaire Pedersoli Mantoani ◽  
Peterson de Andrade ◽  
Talita Perez Cantuaria Chierrito ◽  
Andreza Silva Figueredo ◽  
Ivone Carvalho
Keyword(s):  
Effective Treatment ◽  
Chagas Disease ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Neglected Diseases ◽  
Triazole Derivatives ◽  
Wide Range ◽  
The World ◽  
Great Relevance ◽  
The Moment

Neglected Diseases (NDs) affect million of people, especially the poorest population around the world. Several efforts to an effective treatment have proved insufficient at the moment. In this context, triazole derivatives have shown great relevance in medicinal chemistry due to a wide range of biological activities. This review aims to describe some of the most relevant and recent research focused on 1,2,3- and 1,2,4-triazolebased molecules targeting four expressive NDs: Chagas disease, Malaria, Tuberculosis and Leishmaniasis.

A Comprehensive Review on the Therapeutic Versatility of Imidazo [2,1-b]thiazoles

2020 ◽  
Vol 27 (40) ◽  
pp. 6864-6887 ◽  
Author(s):  
Mohd Adil Shareef ◽  
Irfan Khan ◽  
Bathini Nagendra Babu ◽  
Ahmed Kamal
Keyword(s):  
Literature Review ◽  
Medicinal Chemistry ◽  
Therapeutic Agents ◽  
Present Review ◽  
Thiazole Derivatives ◽  
Pharmacological Activities ◽  
Comprehensive Review ◽  
Derivatives Of

Background:: Imidazo[2,1-b]thiazole, a well-known fused five-membered hetrocycle is one of the most promising and versatile moieties in the area of medicinal chemistry. Derivatives of imidazo[2,1-b]thiazole have been investigated for the development of new derivatives that exhibit diverse pharmacological activities. This fused heterocycle is also a part of a number of therapeutic agents. Objective:: To review the extensive pharmacological activities of imidazo[2,1-b]thiazole derivatives and the new molecules developed between 2000-2018 and their usefulness. Method:: Thorough literature review of all relevant papers and patents was conducted. Conclusion:: The present review, covering a number of aspects, is expected to provide useful insights in the design of imidazo[2,1-b]thiazole-based compounds and would inspire the medicinal chemists for a comprehensive and target-oriented information to achieve a major breakthrough in the development of clinically viable candidates.

Tetrazoloquinolines: Synthesis, Reactions, and Applications

2020 ◽  
Vol 24 (4) ◽  
pp. 439-464 ◽  
Author(s):  
Rizk E. Khidre ◽  
Tahah A. Ameen ◽  
Mounir A. I. Salem
Keyword(s):  
Carboxylic Acid ◽  
Chemical Reactions ◽  
Sodium Azide ◽  
Biological Activities ◽  
Quinoline Derivatives ◽  
Pharmacological Activities ◽  
Synthesis Reactions ◽  
Intramolecular Cyclocondensation

This review summarizes the synthesis, reactions, and biological activities of tetrazolo[1,5-a]quinoline derivatives. These derivatives were synthesized by several methods such as i) from the reaction of 2-chloroquinoline with sodium azide ii) from diazotization 2-hydrazinylquinoline derivatives, and iii) from intramolecular cyclocondensation of 2-azidoarylidenes. Also, the chemical reactions and pharmacological activities of some tetrazoloquinolines such as tetrazolo[1,5-a]quinoline-4-carbaldehyde, 5-chlorotetrazolo[ 1,5-a]quinoline, 4-(chloromethyl)tetrazolo[1,5-a]quinoline, tetrazolo[1,5- a]quinoline-4-carboxylic acid, and 5-azidotetrazolo[1,5-a]quinoline were discussed.

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