A REVIEW ON RECENT ADVANCES IN CHEMISTRY, SYNTHESIS AND BIOLOGICAL APPLICATIONS OF ISATIN DERIVATIVES

2018 ◽  
pp. 16-22
Author(s):  
Shukla PK ◽  
Singh MP ◽  
Patel R
Keyword(s):  
Heterocyclic Compounds ◽  
Biologically Active ◽  
Biological Applications ◽  
Plant Origin ◽  
Recent Past ◽  
Pharmacological Activities ◽  
Naturally Occurring ◽  
Recent Advances ◽  
Biological Aspects ◽  
Isatin Derivatives

Indole and its derivatives have engaged a unique place in the chemistry of nitrogen heterocyclic compounds. The recognition of the plant growthhormone, heteroauxin, the significant amino acids, tryptamine & tryptophan and anti-inflammatory drug, indomethacine are the imperativederivatives of indole which have added stimulus to this review work. Isatin (1H-indole-2,3-dione), an indole derivative of plant origin. Althoughit is a naturally occurring compound, but was synthesized by Erdmann and Laurent in 1840 before it was found in nature. Isatin is a versatileprecursor for many biologically active molecules and its diversified nature makes it a versatile substrate for further modifications. It is concernedin many pharmacological activities like anti-malarial, antiviral, anti-allergic, antimicrobial etc; isatin and its derivatives have been also found todemonstrate promising outcomes against various cancer cell lines. This review provides a brief overview on the recent advances and futureperspectives on chemistry and biological aspects of isatin and its derivatives reported in the recent past.

Recent Advances in Therapeutic Applications of Bisbenzimidazoles

2020 ◽  
Vol 16 (4) ◽  
pp. 454-486 ◽  
Author(s):  
Smita Verma ◽  
Vishnuvardh Ravichandiran ◽  
Nihar Ranjan ◽  
Swaran J.S. Flora
Keyword(s):  
Heterocyclic Compounds ◽  
Wide Spectrum ◽  
Dna Recognition ◽  
Present Review ◽  
Pharmacological Activities ◽  
Structural Motifs ◽  
Therapeutic Applications ◽  
The Past ◽  
Recent Advances

Nitrogen-containing heterocycles are one of the most common structural motifs in approximately 80% of the marketed drugs. Of these, benzimidazoles analogues are known to elicit a wide spectrum of pharmaceutical activities such as anticancer, antibacterial, antiparasitic, antiviral, antifungal as well as chemosensor effect. Based on the benzimidazole core fused heterocyclic compounds, crescent-shaped bisbenzimidazoles were developed which provided an early breakthrough in the sequence-specific DNA recognition. Over the years, a number of functional variations in the bisbenzimidazole core have led to the emergence of their unique properties and established them as versatile ligands against several classes of pathogens. The present review provides an overview of diverse pharmacological activities of the bisbenzimidazole analogues in the past decade with a brief account of its development through the years.

scholarly journals Recent Advances in Chalcones: Synthesis, Transformation and Pharmacological Activities

2019 ◽  
pp. 1-16
Author(s):  
Oluwaseyi Bukky Ovonramwen ◽  
Bodunde Joseph Owolabi ◽  
Amowie Philip Oviawe
Keyword(s):  
Organic Synthesis ◽  
Heterocyclic Compound ◽  
Heterocyclic Compounds ◽  
Condensation Reaction ◽  
Review Article ◽  
Pharmacological Activities ◽  
Usual Approach ◽  
Recent Advances ◽  
Anti Cancer ◽  
Multifunctional Molecules

Chalcones are useful intermediates in the synthesis of heterocyclic compound and the unique reagents in organic synthesis. The usual approach to obtain chalcones is through Claisen-Schmidt condensation. Several novel heterocyclic chalcone analogs have emerged. Chalcones are multifunctional molecules that possess promising pharmacological activities. Chalcones are known for anti-cancer, antioxidant, anti-inflammatory, anti-microbial, anti-tubercular, antileishmanial, antimalarial, anthelmintic, osteogenic activities. This review article focuses on recent applications of Claisen-Schmidt condensation reaction employed in the synthesis of chalcone, its transformation to heterocyclic compounds and pharmacological activities.

scholarly journals Chemistry and Biological Activities of 1,2,4-Triazolethiones—Antiviral and Anti-Infective Drugs

Molecules ◽  
2020 ◽  
Vol 25 (13) ◽  
pp. 3036
Author(s):  
Ashraf A. Aly ◽  
Alaa A. Hassan ◽  
Maysa M. Makhlouf ◽  
Stefan Bräse
Keyword(s):  
Natural Products ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Biologically Active ◽  
Biological Applications ◽  
Active Moiety ◽  
Interesting Class

Mercapto-substituted 1,2,4-triazoles are very interesting compounds as they play an important role in chemopreventive and chemotherapeutic effects on cancer. In recent decades, literature has been enriched with sulfur- and nitrogen-containing heterocycles which are used as a basic nucleus of different heterocyclic compounds with various biological applications in medicine and also occupy a huge part of natural products. Therefore, we shed, herein, more light on the synthesis of this interesting class and its application as a biologically active moiety. They might also be suitable as antiviral and anti-infective drugs.

Recent advances of thiazole hybrids in biological applications

2019 ◽  
Vol 11 (15) ◽  
pp. 1979-1998 ◽  
Author(s):  
Mehmet Gümüş ◽  
Mehmet Yakan ◽  
İrfan Koca
Keyword(s):  
Biological Activity ◽  
Heterocyclic Compounds ◽  
Chemical Reactivity ◽  
Biological Properties ◽  
The Other ◽  
Hybrid Structures ◽  
Thiazole Ring ◽  
Biological Applications ◽  
Recent Advances ◽  
Recent Developments

Thiazoles have attracted much synthetic interest due to their wide variety of biological properties and are important members of heterocyclic compounds. In recent years, studies on the synthesis of thiazole compounds have been increasing because of the properties of this core. In particular, the hybrid structures in which the thiazole ring and the other nuclei are linked have gained popularity. Hybrid structures are formed by the combination of different groups of chemical reactivity and biological activity characteristics. In this review, we highlight recent developments related to hybrid structures containing a thiazole core, recently developed as anticancer, antibacterial, anti-inflammatory, analgesic, anti-tubercular, antialzheimer and antidiabetic compounds.

Dual Acting Isatin-heterocyclic Hybrids: Recent Highlights as Promising Pharmacological Agents

2018 ◽  
Vol 16 (2) ◽  
pp. 220-236 ◽  
Author(s):  
Srinubabu Maddela ◽  
Githa Elizabeth Mathew ◽  
Della Grace Thomas Parambi ◽  
Fakhria Aljoufi ◽  
Bijo Mathew
Keyword(s):  
Single Molecule ◽  
Heterocyclic Compounds ◽  
Structural Modification ◽  
Drug Efficacy ◽  
Biologically Active ◽  
Synergistic Activity ◽  
Pharmacological Activities ◽  
Pharmacological Agents ◽  
Drug Candidates ◽  
Derivatives Of

Background: For the development of suitable lead molecules to different diseases is a highly challenging task for medicinal chemists. Nowadays, hybrid pharmacophore concept has developed as a useful structural modification tool in the drug design of new drug candidates for different diseases. Hybrid pharmacophore approach consists of combination of two or more pharmacophoric moieties from different biologically active compounds with complementary functions or different mechanisms of action into a single molecule. This often results in synergistic activity or enhanced drug efficacy. Objective: To develop the suitable leads for different diseases there will be a lot of scope to study the substitution of heterocyclic moieties on the different positions of isatin ring. The broad and potent activities of the isatin and their derivatives have been established them as pharmacologically significant scaffolds. In this review, an attempt has been made with specifically emphasizing the hybridization of Isatin with different derivatives of heterocyclic compounds on the different positions of the isatin ring (aryl ring, isatin nitrogen and C2/C3 carbonyl moieties). Conclusion: This review highlighted the recent advances of dual acting isatin-heterocyclic hybrids presenting various pharmacological activities viz., anticancer, antitubercular, anti-inflammatory and antimicrobial.

Recent Advances in the Transition Metal Catalyzed Addition of Carboxylic Acids to Alkynes

2021 ◽  
Vol 25 ◽  
Author(s):  
Victorio Cadierno
Keyword(s):  
Natural Products ◽  
Transition Metal ◽  
Carboxylic Acids ◽  
Heterocyclic Compounds ◽  
Biologically Active ◽  
Recent Advances ◽  
Enol Esters ◽  
Cascade Processes ◽  
Transition Metal Catalyzed ◽  
Metal Catalyzed

: Recent advances in the metal-catalyzed hydrofunctionalization of alkynes with carboxylic acids are comprehensively reviewed. Both inter- and intramolecular processes, leading respectively to enol esters and lactones, are discussed, as well as the involvement of these transformations in the synthesis of natural products and biologically active molecules, and the assembly of elaborated heterocyclic compounds though cascade processes. Literature published since 2011 is covered.

scholarly journals 2-Acetylbenzimidazole: a Valuable Synthon for the Synthesis of Biologically Active Molecules

2020 ◽  
Vol 11 (4) ◽  
pp. 11562-11591
Keyword(s):  
Heterocyclic Compounds ◽  
Heterocyclic System ◽  
Biological Activities ◽  
Biologically Active ◽  
Online Search ◽  
Convenient Synthesis ◽  
Anti Cancer ◽  
Pharmacological Interest ◽  
Main Motive ◽  
Biological Aspects

Benzimidazole is an important moiety from a medicinal chemistry perspective due to its various biological activities such as antimicrobial, anti-cancer, anti-diabetic, anti-Alzheimers, and anti-inflammatory, etc. 2-acetylbenzimidazole is exploited to obtain various heterocyclic compounds of pharmacological interest. This review's main motive is to present the literature on 2-acetylbenzimidazole chemistry and provide valuable and up-to-date information for its applications. The present review is carried out by compiling literature from 1964 to 2020 concerning the synthesis and biological aspects of various heterocyclic compounds derived from 2-acetylbenzimidazole. Literature was collected from various online search engines viz. Google Scholar, PubMed, Science Direct, Core, and Semantic scholar. 2-acetylbenzimidazole has been successfully employed as a synthon to obtain heterocyclic system viz. oxirane, pyrazoline, thiazole, pyrazole, isoxazoline, isoxazole, pyridine, pyrimidine, thiazine, diazepine, and other miscellaneous rings. 2-acetylbenzimidazole has shown promise for the convenient synthesis of various heterocyclic compounds. The reactions can be carried out on various reactive sites of 2-acetylbenzimidazole, which are the carbonyl group and the amino group. This review will help to explore various heterocyclic compounds and particularly in the synthesis of biologically useful compounds.

A Review an Isatin, Isatin Derivatives and their Pharmacological Activity

2021 ◽  
pp. 59-62
Author(s):  
S. Janet Beula ◽  
T. Rama Mohan Reddy ◽  
R. Suthakaran ◽  
Suneetha K.
Keyword(s):  
Pharmacological Activity ◽  
Heterocyclic Compounds ◽  
Indole Derivative ◽  
Pharmacological Action ◽  
Pharmacological Properties ◽  
Important Class ◽  
Pharmacological Activities ◽  
Pharmacological Screening ◽  
Medicinal Drugs ◽  
Isatin Derivatives

Isatin or 1H-indole-2, 3-dione is an indole derivative. Isatin is an important class of heterocyclic compounds. Recently, heterocyclic compounds analogues and their derivatives have attracted strong interest in medicinal chemistry due to their biological and pharmacological properties. The structure have offered a high value of diversity that is proven useful for the development of new medicinal drugs and improved potency,less toxicity and good pharmacological activity. Isatin has a wide varity of pharmacological activities such as an antimicrobial, anticancer, antiviral, anticonvulsant, anti-inflammatory and analgesic etc. The aim of this review is to provide the recent efforts of scinentists in pharmacological screening of isatin, importants and synthesis of isatin derivatives,pharmacological action of isatin and their biological activity.

A Mini-Review on Pharmacological Importance of Benzothiazole Scaffold

2020 ◽  
Vol 17 ◽  
Author(s):  
Mohammad Asif ◽  
Mohd. Imran
Keyword(s):  
Heterocyclic Compounds ◽  
Biologically Active ◽  
Pharmacological Properties ◽  
Pharmacological Activities ◽  
Structural Alterations ◽  
Benzothiazole Derivatives ◽  
Drug Molecules ◽  
Anti Inflammatory ◽  
Almost All

: Heterocyclic compounds are important because they have almost all types of pharmacological properties. Due to these properties of heterocyclic compounds, they attracted the researchers for the development of more effective newer drug molecules. In this review, we are focused on benzothiazole and its derivatives, which are used for the synthesis of various biologically active molecules. Benzothiazole derivatives have been possessed the various type of pharmacological activities like antimicrobial, anti-inflammatory, analgesic, anticonvulsant, antiviral, anthelmintic, antioxidant, anticancer, and other anticipated activities. Hence, structural alterations have resulted in different benzothiazole derivatives that illustrated a wide variety of pharmacological activities.

scholarly journals Synthesis and Evaluation of Important Biologically Active Heterocyclic Compounds: Schiff Bases, Oxadiazole and Pyrazolyl Derivatives

2013 ◽  
Vol 9 (2) ◽  
pp. 1892-1899
Author(s):  
Mona A. Hosny ◽  
Wafaa A. Mokbe ◽  
Emtithal A. El-Sawi
Keyword(s):  
Breast Cancer ◽  
Heterocyclic Compounds ◽  
Biologically Active ◽  
High Antimicrobial Activity ◽  
Pharmacological Activities ◽  
Ic50 Value ◽  
New Compounds ◽  
Value Of It ◽  
Derivatives Of ◽  
Acid Compound

In this work, we prepared an excellent yield of (2-oxo-2H-pyrano[3,2-h] quinolin-4-yl) acetic acid; compound (1) and from the reaction of it with hydrazine hydrate (100%) we obtain 2-(2-oxo-2H-pyrano [3,2-h] quinolin-4-yl) aceto hydrazide (2) which is the starting material for the synthesis of several series of new compounds: such as schiff’s bases (3a-e) and compound (4) in good yields, hydrazide derivatives like compound (5), derivatives of mercapto oxadiazole as compound (6) and derivatives of pyrazolyl as compound (7). All these compounds were found to possess high antimicrobial activity against G+ and G- bacteria and against antifungal as described in scheme (1). Anticancer activity was screened only for compound (1). The IC50 value of it against breast cancer was found = 6.83 µM comparable with that of the drug of doxorubicin which has IC50 = 5.6. As a result these newly compounds from (1) to (7) are considerable as potent compounds for various pharmacological activities. 

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