Recent Development in Substituted Benzothiazole as an Anticonvulsant Agent

2020 ◽  
Vol 21 ◽  
Author(s):  
Amol Kale ◽  
Rajendra Kakde ◽  
Smita Pawar ◽  
Rutuja Thombare
Keyword(s):  
Antiepileptic Drugs ◽  
Heterocyclic Compounds ◽  
Neuronal Excitability ◽  
Scientific Literature ◽  
Biological Activities ◽  
Ring System ◽  
Gingival Hyperplasia ◽  
Anticonvulsant Agent ◽  
Large Panel ◽  
Heterocyclic Structure

: Heterocyclic compounds and its derivatives gained more attention due to their valuable biological and pharmacological properties. Benzothiazole is a heterocyclic structure containing bicyclic ring system with large panel of applications. The benzothiazole is present in many new products undergoing research with the hope that it possesses various biological activities. Epilepsy is a diverse group of diseases marked by neuronal excitability and hypersynchronous neuronal activity of motor, sensory or autonomic events with or without loss of consciousness.. Presently many antiepileptic drugs like Lamotrigine, stiripentol tiagabine, pregabalin, felbamate and topiramate are available and effective toward only 60-80% of patients along with undesirable side effects, such as hepatotoxicity, gastrointestinal disturbance, drowsiness, gingival hyperplasia, and hirsutism. Thus many attempts are still going on to develop antiepileptic drugs with safer profile. This review is mainly focus on compilation of reported scientific literature data in the recent one-decade on anticonvulsant activity of benzothiazole compounds.

scholarly journals Syntheses, Evaluation and Characterization of Some 1, 3, 4-Oxadiazoles as Antimicrobial Agents

2009 ◽  
Vol 6 (4) ◽  
pp. 1133-1138 ◽  
Author(s):  
Niti Bhardwaj ◽  
S. K. Saraf ◽  
Pankaj Sharma ◽  
Pradeep Kumar
Keyword(s):  
Heterocyclic Compounds ◽  
Antimicrobial Agents ◽  
Biological Activities ◽  
Condensation Reaction ◽  
Reaction Scheme ◽  
Ring System ◽  
Indole Ring ◽  
Different Strains ◽  
Derivatives Of

1,3,4-Oxadiazoles show various biological activities and have been synthesized from different compounds. 1,3,4-oxadiazole is popularly known for its antimicrobial, anti-inflammatory, pesticidal and antihypertensive activitiesetc. It is well known that the synthesis of heterocyclic compounds tend to contain multi-structure in a molecule. The ring formation involves the condensation reaction. The challenge is to develop the ring system by incorporating the indole nucleus into it through the proposed reaction scheme. There are two free positions for the substitution in the oxadiazole ring system. In this study, it was planned to incorporate the oxadiazole ring system into indole ring. Synthesis of derivatives of 1,3,4-oxadiazoles from different benzaldehydes Characterization of the synthesized compounds along with their antimicrobial activity on different strains.

scholarly journals Biological Aspects of Emerging Benzothiazoles: A Short Review

2013 ◽  
Vol 2013 ◽  
pp. 1-12 ◽  
Author(s):  
Ruhi Ali ◽  
Nadeem Siddiqui
Keyword(s):  
Heterocyclic Compounds ◽  
Scientific Literature ◽  
Biological Activities ◽  
Research Work ◽  
Short Review ◽  
Biological Properties ◽  
Therapeutic Agents ◽  
Benzothiazole Derivatives ◽  
Wide Range ◽  
Biological Aspects

In recent years heterocyclic compounds analogues and derivatives have attracted wide attention due to their useful biological and pharmacological properties. Benzothiazole is among the usually occurring heterocyclic nuclei in many marine as well as natural plant products. Benzothiazole is a privileged bicyclic ring system with multiple applications. It is known to exhibit a wide range of biological properties including anticancer, antimicrobial, and antidiabetic, anticonvulsant, anti-inflammatory, antiviral, antitubercular activities. A large number of therapeutic agents are synthesized with the help of benzothiazole nucleus. During recent years there have been some interesting developments in the biological activities of benzothiazole derivatives. These compounds have special significance in the field of medicinal chemistry due to their remarkable pharmacological potentialities. This review is mainly an attempt to present the research work reported in the recent scientific literature on different biological activities of benzothiazole compounds.

scholarly journals Recent Developments and Biological Activities of 5-Oxo-Imidazolones Derivatives: A Review

2021 ◽  
pp. 287-305
Author(s):  
N. Yellasubbaiah ◽  
V. Velmurugan ◽  
B. Nagasudha
Keyword(s):  
Drug Discovery ◽  
Biological Property ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Ring System ◽  
Present Review ◽  
Modern Drug ◽  
Recent Developments ◽  
Biological Potency

Heterocyclic compounds are essential primary units for both the synthetic and natural starting points. 5-oxo-imidazolone is a 5-member ring system that contains 3 carbons and 2 nitrogens that are arranged at 3 and 1 positions, and ─C═O at the 5th position of the ring. 5-oxo-imidazolone is known as a privileged molecule because of its all biological potency. This biological property increased the attention of many investigators to analyze this ring system and expose several activities. The present review aims to outline the various activities reported on the synthesis and the biological potencies of 5-oxo-imidazolone derivatives. 5-oxo-imidazolone is an important pharmacophore in modern drug discovery.

Anodyne activities of New Tetrazole derivatives from Triazine

2020 ◽  
Vol 11 (3) ◽  
pp. 3377-3383
Author(s):  
Arulmozhi R ◽  
Abirami N ◽  
Helen P Kavitha ◽  
Arulmurugan S ◽  
Vinoth Kumar J
Keyword(s):  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Pharmaceutical Chemistry ◽  
Tail Flick ◽  
Structural Fragment ◽  
Hot Plate ◽  
Standard Drug ◽  
New Class ◽  
Novel Drugs ◽  
Tetrazole Derivatives

The creation of novel drugs containing a tetrazole ring as a structural fragment has contributed considerably to the outstanding achievements of the pharmaceutical chemistry in the last decade. Tetrazoles are the heterocyclic compounds having diverse biological activities such as analgesic, antiinflammation, antimicrobial, anticancer, antidiabetic, etc., and an impending source in biosciences. In this paper, the authors describe the synthesis of novel tetrazoles from N, N-( 6-Phenyl-1,3,5-triazine-2,4-diyl) dibenzamide (PTDDB) and 2-phenyl-4, 6-di(2H-tetrazole-2-yl)-1,3,5-triazine(5a-i) were prepared per the proposed scheme. A new class of tetrazole heterocycles were synthesised and characterised. I n vivo analysis was carried out on the analgesic property of synthesised tetrazole derivatives (5a, 5b, 5c). Characterisation studies such as IR, 1H NMR, 13C NMR, Mass and elemental analysis were performed for the synthesised tetrazole derivatives. Some of the tetrazole derivatives 5a, 5b, and 5c were tested for anodyne activity using morphine as the standard drug. The data reveals that all the three compounds 5a, 5b and 5c taken for the study show analgesic activity by hot plate method and tail flick methods. Among tested compounds, compound 5c is found to have potent analgesic (anodyne) activity. The results of the study indicate that the sample taken for the study show fairly good business using morphine as the standard drug.

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.

Heterocycle Compounds with Antimicrobial Activity

2020 ◽  
Vol 26 (8) ◽  
pp. 867-904 ◽  
Author(s):  
Maria Fesatidou ◽  
Anthi Petrou ◽  
Geronikaki Athina
Keyword(s):  
Heterocyclic Compounds ◽  
Bacterial Infections ◽  
Scientific Community ◽  
Antimicrobial Agents ◽  
Fungal Infections ◽  
Biological Activities ◽  
Literature Survey ◽  
New Findings ◽  
Wide Range ◽  
Number Of Microorganisms

Background: Bacterial infections are a growing problem worldwide causing morbidity and mortality mainly in developing countries. Moreover, the increased number of microorganisms, developing multiple resistances to known drugs, due to abuse of antibiotics, is another serious problem. This problem becomes more serious for immunocompromised patients and those who are often disposed to opportunistic fungal infections. Objective: The objective of this manuscript is to give an overview of new findings in the field of antimicrobial agents among five-membered heterocyclic compounds. These heterocyclic compounds especially five-membered attracted the interest of the scientific community not only for their occurrence in nature but also due to their wide range of biological activities. Method: To reach our goal, a literature survey that covers the last decade was performed. Results: As a result, recent data on the biological activity of thiazole, thiazolidinone, benzothiazole and thiadiazole derivatives are mentioned. Conclusion: It should be mentioned that despite the progress in the development of new antimicrobial agents, there is still room for new findings. Thus, research still continues.

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.

Single Heterocyclic Compounds as Monoamine Oxidase Inhibitors: From Past to Present

2020 ◽  
Vol 20 (10) ◽  
pp. 908-920 ◽  
Author(s):  
Su-Min Wu ◽  
Xiao-Yang Qiu ◽  
Shu-Juan Liu ◽  
Juan Sun
Keyword(s):  
Monoamine Oxidase ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
The Past ◽  
Structure Activity ◽  
Receptor Interactions ◽  
Heterocyclic Derivatives ◽  
Inhibitory Activities ◽  
Leading Compounds ◽  
Heterocyclic Moiety

Inhibitors of monoamine oxidase (MAO) have shown therapeutic values in a variety of neurodegenerative diseases such as depression, Parkinson’s disease and Alzheimer’s disease. Heterocyclic compounds exhibit a broad spectrum of biological activities and vital leading compounds for the development of chemical drugs. Herein, we focus on the synthesis and screening of novel single heterocyclic derivatives with MAO inhibitory activities during the past decade. This review covers recent pharmacological advancements of single heterocyclic moiety along with structure- activity relationship to provide better correlation among different structures and their receptor interactions.

Resolving the Mystery of Ring Opening in the Synthesis of Benzo[d][1, 3]oxazin-4-one and Quinazolin-4(3H)-one

2019 ◽  
Vol 16 (11) ◽  
pp. 898-905
Author(s):  
Harun Patel ◽  
Rahul Pawara ◽  
Sanjay Surana
Keyword(s):  
Characteristic Feature ◽  
Ring Opening ◽  
Biological Activities ◽  
Heterocyclic Ring ◽  
Ring System ◽  
Time Saving ◽  
Fusion Strategy ◽  
Good Template ◽  
Lead Generation

Quinazoline is the six-membered heterocyclic ring system reported for its versatile biological activities. This characteristic feature of quinazoline makes it a good template for a lead generation library. Ring opening is one of the major concerns in the synthesis of quinazolin-4(3H)-one that results in diamide formation. Here, alternative fusion strategy is reported, which is a time-saving and costeffective method to overcome the ring opening problem associated with the synthesis of benzo[ d][1,3]oxazin-4-one and quinazolin-4(3H)-one.

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