A Brief Review on the Development of Novel Potentially Active Azetidin-2-ones Against Cancer

2020 ◽  
Vol 24 (5) ◽  
pp. 473-486 ◽  
Author(s):  
Ligia S. da Silveira Pinto ◽  
Thatyana R. Alves Vasconcelos ◽  
Claudia Regina B. Gomes ◽  
Marcus Vinícius N. de Souza
Keyword(s):  
Side Effects ◽  
Anticancer Agents ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Present Review ◽  
Pharmacological Properties ◽  
Important Group ◽  
Wide Range ◽  
Anti Inflammatory

Azetidin-2-ones (β-lactams) and its derivatives are an important group of heterocyclic compounds that exhibit a wide range of pharmacological properties such as antibacterial, anticancer, anti-diabetic, anti-inflammatory and anticonvulsant. Efforts have been made over the years to develop novel congeners with superior biological activities and minimal potential for undesirable side effects. The present review aimed to highlight some recent discoveries (2013-2019) on the development of novel azetidin-2-one-based compounds as potential anticancer agents.

Quinoline: an attractive scaffold in drug design

2021 ◽  
Vol 21 ◽  
Author(s):  
Lucas F. E. Moor ◽  
Thatyana R. A. Vasconcelos ◽  
Raisa da R. Reis ◽  
Ligia S. S. Pinto ◽  
Thamires M. da Costa
Keyword(s):  
Side Effects ◽  
Drug Design ◽  
Heterocyclic Compounds ◽  
Rational Design ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Bioactive Molecules ◽  
Pharmacological Properties ◽  
Important Group ◽  
Wide Range

: Quinoline and its derivatives comprise an important group of heterocyclic compounds that exhibits a wide range of pharmacological properties such as antibacterial, antiviral, anticancer, antiparasitic, anti-Alzheimer and anticholesterol. In fact, the quinoline nucleus is found in the structure of many drugs and in rational design in medicinal chemistry for the discovery of novel bioactive molecules. Persistent efforts have been made over the years to develop novel congeners with superior biological activities and minimal potential for undesirable side effects. This review highlights some discoveries on the development of quinoline-based compounds in recent years (2013-2019) focusing on their biological activities, including anticancer, antitubercular, antimalarial, anti-ZIKV, anti-DENV, anti-Leishmania and anti-Alzheimer’s disease.

Pharmacologically potentials of different substituted coumarin derivatives

2019 ◽  
Author(s):  
Chem Int
Keyword(s):  
Benzene Ring ◽  
Bioactive Compounds ◽  
Biological Activities ◽  
Pharmacological Properties ◽  
Coumarin Derivatives ◽  
Wide Range ◽  
Anti Oxidant ◽  
Anti Inflammatory ◽  
Coumarin Compounds

Coumarin and its derivatives are widely spread in nature. Coumarin goes to agroup as benzopyrones, which consists of a benzene ring connected to a pyronemoiety. Coumarins displayed a broad range of pharmacologically useful profile.Coumarins are considered as a promising group of bioactive compounds thatexhibited a wide range of biological activities like anti-microbial, anti-viral,antiparasitic, anti-helmintic, analgesic, anti-inflammatory, anti-diabetic, anticancer,anti-oxidant, anti-proliferative, anti-convulsant, and antihypertensiveactivities etc. The coumarin compounds have immense interest due to theirdiverse pharmacological properties. In particular, these biological activities makecoumarin compounds more attractive and testing as novel therapeuticcompounds.

scholarly journals A review on Indole and Benzothiazole derivatives its importance

2019 ◽  
Vol 9 (1-s) ◽  
pp. 505-509 ◽  
Author(s):  
Shaheen Sulthana ◽  
P. Pandian
Keyword(s):  
Heterocyclic Compounds ◽  
Structural Modification ◽  
Biological Activities ◽  
New Product ◽  
Review Article ◽  
Literature Survey ◽  
Pharmacological Activities ◽  
Benzothiazole Derivatives ◽  
Wide Range ◽  
Anti Inflammatory

In recent years heterocyclic compounds analogues and derivatives have attracted wide attention due to their useful biological and pharmacological properties. Indole, Benzothiazole and its analogs are versatile substrates, which can be used for the synthesis of numerous heterocyclic compounds. Indole, Benzothiazole and its derivatives are used in organic synthesis and they are used in evaluating new product that possesses different biological activities. Hence, their extensive structural modification has result in different analogues of Indole and Benzothiazole derivatives depicting wide range of biological and pharmacological activities such as antiviral, anticonvulsant, anti-inflammatory, analgesic, antimicrobial and anticancer. This review article literature survey summarizes the synthesis and pharmacological activities of Indole, Benzothiazole and its derivatives. Keywords: Indole, Benzothiazole, antiviral, anticonvulsant, anti-inflammatory, analgesic, antimicrobial and anticancer

Coumarin: A Promising Scaffold for Design and Development of Bioactive Agents

2020 ◽  
Vol 16 (6) ◽  
pp. 837-852 ◽  
Author(s):  
Hanan M. Alshibl ◽  
Ebtehal S. Al-Abdullah ◽  
Hamad M. Alkahtani
Keyword(s):  
Biological Activities ◽  
Biologically Active ◽  
Present Review ◽  
Coumarin Derivatives ◽  
Design And Development ◽  
Strong Potential ◽  
Starting Point ◽  
Wide Range ◽  
Anti Inflammatory ◽  
Bioactive Agents

Background: As coumarin derivatives are known to prevent and treat various diseases, they have attracted the attention of medicinal chemists. They have strong potential as drugs because their benzopyrone structure can interact noncovalently with numerous enzymes and receptors. Methods: The aim of this review was to summarize the most recently published literature on coumarin derivatives in terms of their antioxidant, antimicrobial, anti-inflammatory, anticancer, and other miscellaneous properties. Results: Coumarin derivatives have a wide range of biological activities. They exhibit antioxidant, antimicrobial, anti-inflammatory, anticancer, anti-coagulant, and anti-Alzheimer effects. Conclusion: The coumarin nucleus is an interesting starting point for the design and development of novel bioactive agents. The present review may help medicinal chemists design biologically active molecules based on the coumarin nucleus.

Trienamines for the Organocatalytic Synthesis of Nitrogen-Containing Heterocycles

2019 ◽  
Vol 23 (10) ◽  
pp. 1078-1089 ◽  
Author(s):  
Jessica R. Gutiérrez Cano ◽  
Julio López ◽  
Miguel A. Vázquez ◽  
David Cruz Cruz ◽  
Clarisa Villegas Gómez
Keyword(s):  
Anticancer Agents ◽  
Heterocyclic Compounds ◽  
Chemical Space ◽  
Biological Activities ◽  
Enantioselective Synthesis ◽  
Present Contribution ◽  
Important Group

Nitrogen-containing heterocycles (NCH), constitute an important group of molecules, which are widely extended in whole chemical space. These compounds are of great interest due to their diverse biological activities. Currently, many compounds derived from NCH are used as powerful drugs for the treatment of diseases ranging from bactericides to anticancer agents. During last decade, the enantioselective synthesis of numerous heterocyclic compounds has been achieved through the use of chiral organocatalysts. The present contribution explores the application of the aminocatalysis towards the synthesis of NCH, particularly through the trienamine catalysis.

scholarly journals 1,2,3-Triazoles: Lead Molecules For Promising Drugs: A Review

2021 ◽  
Vol 33 (12) ◽  
pp. 2896-2918
Author(s):  
Rakesh Singh ◽  
Harpreet Kaur ◽  
Pankaj Gupta
Keyword(s):  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Parent Nucleus ◽  
Biological Properties ◽  
Biologically Active ◽  
Hiv Protease ◽  
Present Review ◽  
Hiv Protease Inhibitors ◽  
Drug Molecules ◽  
Wide Range

A large number of heterocyclic compounds with five membered rings as the parent nucleus such as tetrazoles, imidazoles, triazoles, oxadiazoles, thiadiazoles, thiazoles, etc. have been studied extensively owing to their fascinating biological properties like anticancer, antifungal, antimicrobial, antitumor, anticonvulsant, antiviral, etc. 1,2,3-Triazoles are important class of five-membered biologically active heterocyclic compounds as they exhibit wide range of pharmacological activities. Triazoles are of two types viz. 1,2,3-triazole and 1,2,4-triazole. These compounds have drawn great attention from chemists and biologists since their discovery. In recent years, triazoles has emerged as an interesting field in drug design for many researchers due to their enormous pharmacological scope. The present review aims to sum up the medicinal significance of 1,2,3-triazoles as one of the most significant structures for the development of drug molecules like anticancer, antibacterial, HIV protease inhibitors, antifungal, anti-inflammatory (COX-1/COX-2 inhibitors), antiprotozoal, anticonvulsant, antioxidant and others, which are under clinical trials. Various benzyl and benzyl-halide functionalized 1,2,3-triazole derivatives like rufinamide, mubritinib (TAK-165) and suvorexant showing excellent biological activities have been used as medicine. In present review, more stress has been laid on the major developments in the therapeutic aspects of triazole pharmacophore for the last two decades.

Sulfonamides and Sulphonyl Ester of Quinolines as Non-Acidic, Non- Steroidal, Anti-inflammatory Agents

2020 ◽  
Vol 17 ◽  
Author(s):  
Bilquees Bano ◽  
Kanwal ◽  
Khalid Mohammed Khan ◽  
Almas Jabeen ◽  
Aisha Faheem ◽  
...  
Keyword(s):  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Inhibitory Effect ◽  
Inflammatory Activity ◽  
Spectroscopic Techniques ◽  
Wide Range ◽  
Anti Inflammatory ◽  
Hydroxy Quinoline ◽  
Synthetic Derivatives ◽  
Derivatives Of

Background:: Quinolines are important class of heterocyclic compounds possessing wide range of biological activities. Previously, we had identified Schiff bases of quinoline as potential anti-inflammatory agents, thus the current work is the continuation of our previous study. Objective:: In the current study 3-, 5-, and 8-sulfonamide and 8-sulfonate derivatives of quinoline (1-50) were synthesized and their antiinflammatory potential was evaluated. These synthetic analogs were evaluated for their anti-inflammatory activity via ROS (Reactive oxygen species) inhibitory effect produced from phagocytes from human whole blood. Methods:: The sulfonamide and sulfonate derivatives of quinoline were synthesized via treating 5-, 3-, 8-amino, and 8-hydroxy quinoline with different substituted sulfonyl chlorides in pyridine. The synthetic molecules were characterized using various spectroscopic techniques and screened for their anti-inflammatory potential. Results and Discussion:: Among the synthetic derivatives 1-50, six compounds showed good to moderate anti-inflammatory activity. Compounds 47 (IC50 = 2.9 ± 0.5 μg/mL), 36 (IC50 = 3.2 ± 0.2 μg/mL), and 24 (IC50 = 6.7 ± 0.3 μg/mL) exhibited enhanced activity as compared to the standard ibuprofen (IC50 = 11.2 ± 1.9 μg/mL). Compounds 20 (IC50 = 25.5 ± 0.7 μg/mL), 50 (IC50 = 42.9 ± 5.6 μg/mL), and 8 (IC50 = 53.9 ± 3.1 μg/mL) were moderately active, however, rest of the compounds were found to be inactive. Conclusion:: The sulfonamide and sulfonate derivatives of quinoline were found to have promising anti-inflammatory activity. Further studies on the modification of these molecules may leads to the discovery of new and potential anti-inflammatory agents.

scholarly journals An Overview on Synthetic 2-Aminothiazole-Based Compounds Associated with Four Biological Activities

Molecules ◽  
2021 ◽  
Vol 26 (5) ◽  
pp. 1449
Author(s):  
Mohamed Farouk Elsadek ◽  
Badreldin Mohamed Ahmed ◽  
Mohamed Fawzi Farahat
Keyword(s):  
Drug Development ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Present Review ◽  
The Novel ◽  
Structural Variations ◽  
Inflammatory Agent ◽  
Wide Scale ◽  
Anti Inflammatory

Amongst sulfur- and nitrogen-containing heterocyclic compounds, the 2-aminothiazole scaffold is one of the characteristic structures in drug development as this essential revelation has several biological activities abiding it to act as an anticancer, antioxidant, antimicrobial and anti-inflammatory agent, among other things. Additionally, various 2-aminothiazole-based derivatives as medical drugs have been broadly used to remedy different kinds of diseases with high therapeutic influence, which has led to their wide innovations. Owing to their wide scale of biological activities, their structural variations have produced attention amongst medicinal chemists. The present review highlights the recently synthesized 2-aminothiazole-containing compounds in the last thirteen years (2008–2020). The originality of this proposal is based on the synthetic strategies developed to access the novel 2-aminothiazole derivatives (N-substituted, 3-substituted, 4-substituted, multi-substituted, aryl/alkyl substituents or acyl/other substituents). The literature reports many synthetic pathways of these 2-aminothiazoles associated with four different biological activities (anticancer, antioxidant, antimicrobial and anti-inflammatory activities). It is wished that this review will be accommodating for new views in the expedition for rationalistic designs of 2-aminothiazole-based medical synthetic pathways.

Diverse chemical and biological potentials of various pyridazine and pyridazinone derivatives

2019 ◽  
Author(s):  
Chem Int
Keyword(s):  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Biological Properties ◽  
Industrial Chemical ◽  
Anti Inflammatory ◽  
Pyridazinone Derivatives

A series of heterocyclic compounds incorporating pyridazine moiety were for diverse biological activities. Pyridazines and pyridazinones derivatives showed wide spectrum of biological activities such as vasodialator, cardiotonic, anticonvulsant, antihypertensive, antimicrobial, anti-inflammatory, analgesic, anti-feedant, herbicidal, and various other biological, agrochemical and industrial chemical activities. The results illustrated that the synthesized pyridazine/pyridazine compounds have diverse and significant biological activities. Mechanistic insights into the biological properties of pyridazinone derivatives and various synthetic techniques used for their synthesis are also described.

Biologically Active 2,5-Disubstituted-1,3,4-Oxadiazoles

2009 ◽  
Vol 2 (1) ◽  
pp. 390-406
Author(s):  
Harish Rajak ◽  
Murli Dhar Kharya ◽  
Pradeep Mishra
Keyword(s):  
Heterocyclic Compounds ◽  
Medical Literature ◽  
Biological Activities ◽  
Biologically Active ◽  
Pharmacological Properties ◽  
Clinical Use ◽  
Synthetic Drugs ◽  
Physiologic Activity ◽  
Pharmacologically Active

There are vast numbers of pharmacologically active heterocyclic compounds in regular clinical use. The presence of heterocyclic structures in diverse types of compounds is strongly indicative of the profound effects such structure exerts on physiologic activity, and recognition of this is abundantly reflected in efforts to find useful synthetic drugs. The 1,3,4-oxadiazole nucleus has emerged as one of the potential pharmacophore responsible for diverse pharmacological properties. Medical Literature is flooded with reports of a variety of biological activities of 2,5-Disubstituted-1,3,4-oxadiazoles. The present work is an attempt to summarize and enlist the various reports published on biologically active 2,5-disubstituted-1,3,4-oxadiazoles.

Sign in / Sign up

Export Citation Format

Share Document