Recent Synthetic Strategies for Monocyclic Azole Nucleus and Its Role in Drug Discovery and Development

2018 ◽  
Vol 15 (3) ◽  
pp. 321-340 ◽  
Author(s):  
Neha ◽  
Ashish Ranjan Dwivedi ◽  
Rakesh Kumar ◽  
Vinod Kumar
Keyword(s):  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Review Article ◽  
Drug Discovery And Development ◽  
Drug Candidates ◽  
Drug Molecules ◽  
Current Review ◽  
Biological Potential ◽  
Recent Developments ◽  
Potent Drug

Background: In recent years, the development and diversification of heterocyclic compounds has become central to the discovery of bioactive compounds with novel or improved pharmacological properties. In particular, N-containing heterocycles are proved to be promising leads and drug candidates, and received huge attention of the medicinal chemists. Objective: Many drugs especially antibiotics are becoming obsolete due to the development of multidrug resistance. Moreover, toxicity and other side effects of some drugs necessitated the quest for safer and more potent drug candidates. The current review article described biological potential of various monocyclic azoles. Recent developments in the synthesis of azole derivatives have been also reviewed. Conclusion: The presence of N-heterocyclic rings can influence the pharmacokinetics, pharmacodynamics, pKa and bioavailability profile of the drug molecules. Compounds containing monocyclic azole rings showed various biological activities and number of molecules are in clinical practice. A number of important leads and potential drug candidates containing azole nucleus are in advance stages of drug developments. Thus, simple, atom economic and more efficient synthetic strategies are desired for the synthesis of new libraries of the compounds.

scholarly journals Biological Potential and Chemical Properties of Pyridine and Piperidine Fused Pyridazine Compounds: Pyridopyridazine a Versatile Nucleus

2016 ◽  
Vol 1 (1) ◽  
pp. 29 ◽  
Author(s):  
Mohammad Asif
Keyword(s):  
Nitrogen Atom ◽  
Structural Feature ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Chemical Properties ◽  
Pharmacological Properties ◽  
Drug Molecules ◽  
Biological Potential ◽  
Different Types ◽  
And Chemical Properties

Pyridopyridazine compounds are important nitrogen atom containing heterocyclic compounds due to their pharmacological versatility. This heterocycle system characterized a structural feature for different types of bioactive compounds that exhibiting various types of biological activities which make it an attractive scaffold for the design and development of new drug molecules. This article provided information about the pharmacological properties of pyridopyridazines derivatives.

Recent developments of quinoline derivatives and their potential biological activities

2020 ◽  
Vol 17 ◽  
Author(s):  
Mustapha Dib ◽  
Hajiba Ouchetto ◽  
Khadija Ouchetto ◽  
Abderrafia Hafid ◽  
Mostafa Khouili
Keyword(s):  
Drug Discovery ◽  
Organic Synthesis ◽  
Heterocyclic Compounds ◽  
Recent Progress ◽  
Biological Activities ◽  
Quinoline Derivatives ◽  
Quinoline Ring ◽  
Research Groups ◽  
Drug Discovery And Development ◽  
Recent Developments

: Heterocyclic compounds containing the quinoline ring play a significant role in organic synthesis and therapeutic chemistry. Polyfunctionalized quinolines have attracted the attention of many research groups, especially those who work on the drug discovery and development. These derivatives have been widely explored by the research biochemists and are reported to possess wide biological activities. This review focuses on the recent progress in the synthesis of heterocyclic compounds based-quinoline and their potential biological activities.

scholarly journals Recent Advances in the Synthesis of β-Carboline Alkaloids

Molecules ◽  
2021 ◽  
Vol 26 (3) ◽  
pp. 663
Author(s):  
Tímea Szabó ◽  
Balázs Volk ◽  
Mátyás Milen
Keyword(s):  
Natural Products ◽  
Pharmacological Activity ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Antimicrobial Drug ◽  
Drug Candidates ◽  
Recent Developments ◽  
Pharmacological Potential ◽  
Key Steps ◽  
Synthetic Approaches

β-Carboline alkaloids are a remarkable family of natural and synthetic indole-containing heterocyclic compounds and they are widely distributed in nature. Recently, these alkaloids have been in the focus of interest, thanks to their diverse biological activities. Their pharmacological activity makes them desirable as sedative, anxiolytic, hypnotic, anticonvulsant, antitumor, antiviral, antiparasitic or antimicrobial drug candidates. The growing potential inherent in them encourages many researchers to address the challenges of the synthesis of natural products containing complex β-carboline frameworks. In this review, we describe the recent developments in the synthesis of β-carboline alkaloids and closely related derivatives through selected examples from the last 5 years. The focus is on the key steps with improved procedures and synthetic approaches. Furthermore the pharmacological potential of the alkaloids is also highlighted.

Triazole As Potent Anti-Cancer Agent- A Pharmacophoric Scaffold

2021 ◽  
Vol 17 ◽  
Author(s):  
Nidhi Kala ◽  
Kalpana Praveen Rahate
Keyword(s):  
Characteristic Feature ◽  
Biological Activities ◽  
Heterocyclic Ring ◽  
Ring System ◽  
Review Article ◽  
Current Review ◽  
Anti Cancer ◽  
Good Template ◽  
Cancer Agent

: Triazole is the main five-membered Nitrogen-containing basic heterocyclic ring system reported for their biological activities and compounds with multiple pharmacophores, which fetch together acquaintance of a target with sympathetic types of the molecule that might interact with the target. In addition, healthy, adaptable, and scalable chemistry must be employed to achieve the task. This characteristic feature of triazole would make a good template for a lead cohort library. The current review article focuses on recent advancements in triazole moiety as an anti-cancer agent with their mechanism pathways of synthesized analogues.

scholarly journals Natural Products as Modulators of Sirtuins

Molecules ◽  
2020 ◽  
Vol 25 (14) ◽  
pp. 3287 ◽  
Author(s):  
Berin Karaman Mayack ◽  
Wolfgang Sippl ◽  
Fidele Ntie-Kang
Keyword(s):  
Natural Products ◽  
Drug Discovery ◽  
Histone Deacetylases ◽  
High Throughput Screening ◽  
Chemical Space ◽  
Class Iii ◽  
Drug Candidates ◽  
Starting Point ◽  
Recent Developments ◽  
Potent Drug

Natural products have been used for the treatment of human diseases since ancient history. Over time, due to the lack of precise tools and techniques for the separation, purification, and structural elucidation of active constituents in natural resources there has been a decline in financial support and efforts in characterization of natural products. Advances in the design of chemical compounds and the understanding of their functions is of pharmacological importance for the biomedical field. However, natural products regained attention as sources of novel drug candidates upon recent developments and progress in technology. Natural compounds were shown to bear an inherent ability to bind to biomacromolecules and cover an unparalleled chemical space in comparison to most libraries used for high-throughput screening. Thus, natural products hold a great potential for the drug discovery of new scaffolds for therapeutic targets such as sirtuins. Sirtuins are Class III histone deacetylases that have been linked to many diseases such as Parkinson`s disease, Alzheimer’s disease, type II diabetes, and cancer linked to aging. In this review, we examine the revitalization of interest in natural products for drug discovery and discuss natural product modulators of sirtuins that could serve as a starting point for the development of isoform selective and highly potent drug-like compounds, as well as the potential application of naturally occurring sirtuin inhibitors in human health and those in clinical trials.

scholarly journals Synthesis of Hydroxybenzodiazepines with Potential Antioxidant and Antifungal Action

2021 ◽  
Author(s):  
Elizeu Caiana ◽  
Bruno de Veras ◽  
Antônia de Souza ◽  
Neide Queiroz
Keyword(s):  
Antifungal Activity ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Sporothrix Schenckii ◽  
Aqueous Solubility ◽  
Cell Permeability ◽  
Biological Potential ◽  
In Silico Studies ◽  
Total Antioxidant ◽  
Antifungal Action

Benzodiazepines derivatives are nitrogen heterocyclic compounds that have various industrial, synthetic, and medicinal applications. Therefore, its potential fully justifies every effort towards the improvement of new, selective, and competent production of these heterocyclic compounds. The novelty of this study encompasses the synthesis of new hydroxylated analogs of 1,5-benzodiazepine together with the evaluation of their biological potential as antioxidants and antifungals candidates. Additionally, the reported antifungal activity against fungi of the Sporothrix schenckii complex inaugurates an unprecedented property for this class of compounds. The results of biological activities assays suggest that the novel 2,7-dimethyl-2,4-bis(4-hydroxyphenyl)-2,3-dihydro1H-1,5-benzodiazepine possesses a high antifungal activity against all fungal strains evaluated of the Sporothrix genus and outstanding total antioxidant capacity. Besides, in silico studies have evidenced that the hydroxylated derivatives have the best aqueous solubility and cell permeability profile, which makes them superior in comparison with the commercial antifungal itraconazole, a drug commonly used in the treatment of sporotrichosis.

Review: Phytochemicals of the Seriphidium, Economically and Pharmaceutically Important Genus of Asteraceae Family

2020 ◽  
Vol 17 (2) ◽  
pp. 158-168
Author(s):  
Nusrat Shafiq ◽  
Sahrish Shafiq ◽  
Naila Rafiq ◽  
Shagufta Parveen ◽  
Irum Javed ◽  
...  
Keyword(s):  
Secondary Metabolites ◽  
Biological Activities ◽  
Chemical Constituents ◽  
Local Communities ◽  
Review Article ◽  
Pyridine Derivatives ◽  
Biological Potential ◽  
Medicinal Properties ◽  
Phenolic Derivatives ◽  
Asteraceae Family

Seriphidium plants were reported to be utilized by local communities to cure their ailments in the form of paste, tincture, tea, nutraceuticals due to their medicinal properties. Most of the species are used as food, forage and ornamentals, etc. Due to the significant properties of the Seriphidium plants, the present article was designed to compile the data of major aspects and chemical constituents of genus Seriphidium responsible for their significant uses. This review article comprehensively covers the biological potential of different plants with their secondary metabolites and describes an overview of the biological activities of the different species belonging to genus Seriphidium. The main secondary metabolites isolated from different species of the genus Seriphidium are triterpenoid, sesquiterpenes, flavonoids, coumarins, chromones, anthraquinones, polyphenols and their glycosides, phenolic derivatives, balchanins, costunolides, Vulgarin, pyridine derivatives, ceramides, biphenyls, isoflavones. All these compounds are used in the drug industry.

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

scholarly journals A CONCISE OVERVIEW ON HETEROCYCLIC COMPOUNDS EXHIBITING PESTICIDAL ACTIVITIES

2021 ◽  
Vol 9 (08) ◽  
pp. 989-1004
Author(s):  
Shailendra Yadav ◽  
◽  
Sushma Singh ◽  
Chitrasen Gupta ◽  
◽  
...  
Keyword(s):  
Organic Compounds ◽  
Heterocyclic Compounds ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Review Article ◽  
Diverse Group ◽  
Concise Overview ◽  
Physiological Properties ◽  
Pharmaceutical Industries

Heterocyclic compounds are numerous and diverse group of organic compounds. Heterocycles are abundantly found in nature and express various physiological properties. Heterocycles are intricately linked to all aspects of life. There are many heterocyclic compounds currently known, and the number is constantly rising owing to extensive synthetic development and their applications. Heterocyclic compounds are used significantly in a number of areas, including biochemistry and medicinal chemistry, and some others. They are predominantly synthesized in agrochemical and pharmaceutical industries due to their potential biological activities. This review article focuses on recently synthesized heterocyclic compounds and their different pesticidal activities such as antifungal, antibacterial, antiviral, nematocidal, insecticidal, acaricidal, and herbicidal.

Anti-neuropathic and anticonvulsant activities of various substituted triazoles analogues

2019 ◽  
Author(s):  
Chem Int
Keyword(s):  
Heterocyclic Compounds ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Review Article ◽  
Biological Profile ◽  
Triazole Derivatives ◽  
Anti Inflammatory ◽  
New Compounds ◽  
Anticonvulsant Activities

Various heterocyclic compounds along their derivatives were evaluated for their biological activities as antiviral, antitumor, anticonvulsant, antibacterial, antifungal, antituberculosis, analgesic, anti-inflammatory, antidiabetic, antihistamine and other biological activities. The triazole moiety seems to be very small, but in the biological profile has attracted the attention of many researchers to explore this skeleton to its multiple potential against several activities. The triazole derivatives possess a great importance in medicinal chemistry and can be used for the synthesis of numerous heterocyclic compounds with different biological activities. This review article covers the information of triazoles derivatives having different psychopharmacological actions. Thus triazole acts as a promising medicinal agent for the scientists working over this field. This review can be helpful to develop various more new compounds possessing triazoles moiety that could be better in terms of efficacy and lesser toxicity.

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