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.

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. 

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.

Synthesis and Reactions of Perimidines and Their Fused Systems

2020 ◽  
Vol 24 (15) ◽  
pp. 1669-1716 ◽  
Author(s):  
Thoraya A. Farghaly ◽  
Sami A. Al-Hussain ◽  
Zeinab A. Muhammad ◽  
Magda A. Abdallah ◽  
Magdi E. A. Zaki
Keyword(s):  
Chemical Reactions ◽  
Heterocyclic Compounds ◽  
Antifungal Agents ◽  
Biological Activities ◽  
Lone Pair ◽  
Pharmacological Activities ◽  
Synthetic Analogs ◽  
Interesting Class ◽  
Derivatives Of

Perimidines are peri-naphtho-fused derivatives of pyrimidine. They are of particular interest as they are a rare example of an azine in which the lone pair of electrons of pyrrole-like nitrogen participates in the π-system of the molecule. Perimidine is an interesting class of heterocyclic compounds. Various synthetic analogs of perimidines have been prepared and evaluated for many pharmacological activities in different models with desired findings. They exhibit biological activities as antitumor, antiulcer, antimicrobial, and antifungal agents. This review is an attempt to organize the synthesis and chemical reactions of perimidine analogs reported to date systematically since 1955. It should be noted that this review is the first one that includes the preparation and reactions of the perimidine ring.

Benzimidazole: A Milestone in the Field of Medicinal Chemistry

2020 ◽  
Vol 20 (7) ◽  
pp. 532-565 ◽  
Author(s):  
Mahesh S. Vasava ◽  
Manoj N. Bhoi ◽  
Sanjay K. Rathwa ◽  
Divya J. Jethava ◽  
Prachi T. Acharya ◽  
...  
Keyword(s):  
Medicinal Chemistry ◽  
Benzimidazole Derivatives ◽  
Drug Candidate ◽  
Pharmacological Activities ◽  
Drug Candidates ◽  
The Future ◽  
Anti Inflammatory ◽  
Anti Fungal ◽  
Derivatives Of ◽  
Anti Hiv

In the last 2-3 decades, the broad research in the application of benzimidazole derivatives made it important for mankind. Many scientists have worked on benzimidazole derivatives and they found that this compound has a diverse role in the field of medicinal chemistry. Few benzimidazole derivatives are currently in the market as a drug candidate against various diseases. Moreover, the benzimidazole derivatives exhibit pharmacological activities such as anti-tuberculosis, anti-malarial, antihistamine, antimicrobial, antiviral, antidiabetic, anticancer, anti-fungal, anti-inflammatory, analgesic, anti-HIV, etc. In this review, we have summarized various derivatives of benzimidazole which have been prepared by many researchers to understand the chemistry as well as diverse pharmacological activities. These findings may lead the scientists who are working in the field of medicinal chemistry to the development of benzimidazole based drug candidates in the future.

scholarly journals Triazole analogues as potential pharmacological agents: a brief review

2021 ◽  
Vol 7 (1) ◽  
Author(s):  
Sachin Kumar ◽  
Sukhbir Lal Khokra ◽  
Akash Yadav
Keyword(s):  
Oxygen Atom ◽  
Heterocyclic Compounds ◽  
Triazole Ring ◽  
Literature Survey ◽  
Current Status ◽  
Pharmacological Properties ◽  
Pharmacological Activities ◽  
Pharmacological Agents ◽  
Main Text ◽  
Synthetic Procedure

Abstract Background A large number of studies have recently reported that, because of their significant biological and pharmacological properties, heterocyclic compounds and their derivatives have attracted a strong interest in medicinal chemistry. The triazole nucleus is one of the most important heterocycles which has a feature of natural products as well as medicinal agents. Heterocyclic nitrogen is abundantly present in most medicinal compounds. The derivatization of triazole ring is based on the phenomenon of bio-isosteres in which substituted the oxygen atom of oxadiazole nucleus with nitrogen triazole analogue. Main text This review focuses on recent synthetic procedure of triazole moiety, which comprises of various pharmacological activities such as antimicrobial, anticonvulsant, anti-inflammatory, analgesic, antitubercular, anthelmintic, antioxidant, antimalarial, antiviral, etc.. Conclusion This review highlights the current status of triazole compounds as different multi-target pharmacological activities. From the literature survey, triazole is the most widely used compound in different potential activities.

scholarly journals A molecular modelling approach for identifying antiviral selenium-containing heterocyclic compounds that inhibit the main protease of SARS-CoV-2: an in silico investigation

2021 ◽  
Author(s):  
Ahmed Rakib ◽  
Zulkar Nain ◽  
Saad Ahmed Sami ◽  
Shafi Mahmud ◽  
Ashiqul Islam ◽  
...  
Keyword(s):  
Immune Responses ◽  
Heterocyclic Compounds ◽  
Case Fatality ◽  
Biologically Active ◽  
Dynamics Simulation ◽  
World Health ◽  
Drug Candidate ◽  
Drug Candidates ◽  
Host Immune Responses ◽  
Main Protease

Abstract Coronavirus disease 2019 (COVID-19), an infectious disease caused by the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), has been declared a global pandemic by the World Health Organization, and the situation worsens daily, associated with acute increases in case fatality rates. The main protease (Mpro) enzyme produced by SARS-CoV-2 was recently demonstrated to be responsible for not only viral reproduction but also impeding host immune responses. The element selenium (Se) plays a vital role in immune functions, both directly and indirectly. Thus, we hypothesised that Se-containing heterocyclic compounds might curb the activity of SARS-CoV-2 Mpro. We performed a molecular docking analysis and found that several of the selected selenocompounds showed potential binding affinities for SARS-CoV-2 Mpro, especially ethaselen (49), which exhibited a docking score of −6.7 kcal/mol compared with the −6.5 kcal/mol score for GC376 (positive control). Drug-likeness calculations suggested that these compounds are biologically active and possess the characteristics of ideal drug candidates. Based on the binding affinity and drug-likeness results, we selected the 16 most effective selenocompounds as potential anti-COVID-19 drug candidates. We also validated the structural integrity and stability of the drug candidate through molecular dynamics simulation. Using further in vitro and in vivo experiments, we believe that the targeted compound identified in this study (ethaselen) could pave the way for the development of prospective drugs to combat SARS-CoV-2 infections and trigger specific host immune responses.

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

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 Anticancer Potential of Betulonic Acid Derivatives

2021 ◽  
Vol 22 (7) ◽  
pp. 3676
Author(s):  
Adelina Lombrea ◽  
Alexandra Denisa Scurtu ◽  
Stefana Avram ◽  
Ioana Zinuca Pavel ◽  
Māris Turks ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Betulonic Acid ◽  
Pharmacological Activities ◽  
Cellular Resistance ◽  
Drug Candidates ◽  
Starting Point ◽  
Derivatives Of ◽  
Biological And Pharmacological Activities

Clinical trials have evidenced that several natural compounds, belonging to the phytochemical classes of alkaloids, terpenes, phenols and flavonoids, are effective for the management of various types of cancer. Latest research has proven that natural products and their semisynthetic variants may serve as a starting point for new drug candidates with a diversity of biological and pharmacological activities, designed to improve bioavailability, overcome cellular resistance, and enhance therapeutic efficacy. This review was designed to bring an update regarding the anticancer potential of betulonic acid and its semisynthetic derivatives. Chemical derivative structures of betulonic acid including amide, thiol, and piperidine groups, exert an amplification of the in vitro anticancer potential of betulonic acid. With the need for more mechanistic and in vivo data, some derivatives of betulonic acids may represent promising anticancer agents.

scholarly journals Review of antibacterial and antifungal activity of 1,2,4-triazole derivatives

2018 ◽  
pp. 63-68
Author(s):  
Т. О. Samura
Keyword(s):  
Antifungal Activity ◽  
Heterocyclic Compounds ◽  
Practical Importance ◽  
Complex Compounds ◽  
Biologically Active ◽  
Alkyl Aryl ◽  
Triazole Derivatives ◽  
Antimicrobial And Antifungal Activity ◽  
Antibacterial And Antifungal ◽  
Derivatives Of

Derivatives of 1,2,4-triazole is a very  perspective class of heterocyclic compounds which have high therapeutic effectiveness. The main direction of research on these derivatives are antifungal, antiviral, antibacterial, soothing, hypnotic, anticonvulsant, anti-inflammatory and other activities. The aim was to analyze literature data and generalize recent advances in the study of antimicrobial and antifungal action of 1,2,4-triazole derivatives which can help to create new biologically active substances of this type of activity. Bibliosemantical method, systems thinking and the results of our own research were used in the work. The results of the literature review of antimicrobial and antifungal activity among new alkyl, aryl and heteryl derivatives of 1,2,4-triazole and among complex compounds, which contain 1,2,4-triazole are as ligands were analyzed and systematized. Some dependence of this type of activity on specialty of chemical structure of heterocyclic system derivatives was specified. Perspective of purposeful synthesis of new derivatives of 1,2,4-triazole and products of their transformation as available object for studying biological activity and expanding knowledge about antimicrobial and antifungal activity of this class of heterocyclic compounds were shown with informational analysis. Topicality and practical importance of finding biologically active compounds and receiving biologically active substance by synthesis of new derivatives of 1,2,4-triazole with high antimicrobial activity in relation to gram-negative and gram-positive bacteria were demonstrated.

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