Azolo[d]pyridazinones in medicinal chemistry

2020 ◽  
Author(s):  
Oya Unsal Tan ◽  
Keriman Ozadali Sari
Keyword(s):  
Medicinal Chemistry ◽  
Biological Activities ◽  
Antimicrobial Activities ◽  
Drug Candidates ◽  
Strategic Design ◽  
Research Fields ◽  
Comprehensive Information ◽  
Privileged Structure ◽  
Molecular Modeling Studies ◽  
Pyridazinone Derivatives

Azolo[ d]pyridazinone is a privileged structure and versatile pharmacophore whose derivatives are associated with diverse biological activities, in particular antidiabetic, antiasthmatic, anticancer, analgesic, anti-inflammatory, antithrombotic, antidepressant and antimicrobial activities. The importance of this scaffold against some targets like PDE, COX and DPP-4 has been reviewed in detail previously. In the present review, we have summarized comprehensive information on azolo[ d]pyridazinone derivatives investigated by many researchers for their diverse pharmacological activities, structure–activity relationship and molecular modeling studies since 2000. The review may lead scientists in the research fields of organic synthesis, medicinal chemistry and pharmacology to the strategic design and development of azolo[ d]pyridazinone-based drug candidates in the future.

scholarly journals Bunium persicum: A Review of Ethnopharmacology, Phytochemistry, and Biological Activities

2020 ◽  
Author(s):  
Zahra Majidi ◽  
Fatemeh Bina ◽  
Niloofar Kahkeshani ◽  
Roja Rahimi
Keyword(s):  
Biological Activities ◽  
Chemical Constituents ◽  
Antimicrobial Activities ◽  
Modern Medicine ◽  
Pharmacological Activities ◽  
Bunium Persicum ◽  
Comprehensive Information ◽  
Wide Range ◽  
Coa Reductase ◽  
Biological And Pharmacological Activities

Bunium persicum (Boiss) B. Fedtsh (Apiaceae, Persian name: Zireh Kermani) has been used to treat various diseases in traditional and folkloric medicine including gastrointestinal, respiratory, nasopharyngeal, cardiac, ocular, neurological, rheumatological and urinary tract diseases. Its essential oil contains different monoterpenes, sesquiterpenes and phenyl propenes. Other chemical constituents identified in B. persicum are phenolic compounds, fatty acids, carboxylic acids, and carbohydrates. Wide range of biological and pharmacological activities including antioxidant, analgesic, anti-inflammatory, acetylcholinesterase inhibitory, anticonvulsant, HMG-CoA reductase inhibitory, anti-pancreatic lipase, anticancer, antidiabetic, antihistamine, antidiarrheal, antispasmodic, antihematoxic, antityrosinase and antimicrobial activities have been reported from this plant in modern medicine. This article summarizes comprehensive information attributing traditional uses, phytochemistry, and pharmacological activities of Zireh Kermani.

An Overview on Glyco-Macrocycles: Potential New Lead and their Future in Medicinal Chemistry

2020 ◽  
Vol 27 (20) ◽  
pp. 3386-3410
Author(s):  
Kartikey Singh ◽  
Rama Pati Tripathi
Keyword(s):  
Biological Activity ◽  
Medicinal Chemistry ◽  
Potential Role ◽  
Biological Activities ◽  
Natural Sources ◽  
Small Segment ◽  
Drug Candidates ◽  
Wide Range ◽  
Vast Range ◽  
Chiral Macrocycles

Macrocycles cover a small segment of molecules with a vast range of biological activity in the chemotherapeutic world. Primarily, the natural sources derived from macrocyclic drug candidates with a wide range of biological activities are known. Further evolutions of the medicinal chemistry towards macrocycle-based chemotherapeutics involve the functionalization of the natural product by hemisynthesis. More recently, macrocycles based on carbohydrates have evolved a considerable interest among the medicinal chemists worldwide. Carbohydrates provide an ideal scaffold to generate chiral macrocycles with well-defined pharmacophores in a decorated fashion to achieve the desired biological activity. We have given an overview on carbohydrate-derived macrocycle involving their synthesis in drug design and discovery and potential role in medicinal chemistry.

The Quinazoline-Chalcone and Quinazolinone-Chalcone Hybrids: A Promising Combination for Biological Activity.

2020 ◽  
Vol 20 ◽  
Author(s):  
Eduardo Bustos Mass ◽  
Gilmar Vieira Duarte ◽  
Dennis Russowsky
Keyword(s):  
Biological Activity ◽  
Drug Discovery ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Pharmaceutical Research ◽  
Antimicrobial Activities ◽  
Molecular Hybridization ◽  
Hybrid Compounds ◽  
Synthetic Methodologies ◽  
Number Of Publications

: Quinazoline and/or chalcones derivatives are important targets in several areas of chemical sciences, mainly, in the medicinal chemistry and pharmaceutical research. The purpose of this review is to systematize the information available in the literature, including patents, regarding the benefits exerted by the combination of these two pharmacophores into single molecules. These hybrid compounds can exhibit different biological activities, causing a synergistic or a new effect, compared to the individuals. The variability of biological activities includes anticancer, anti-Alzheimer, antiviral and antimicrobial activities, among others. Additionally, synthetic methodologies to prepare the different molecular architectures were discussed based on their similarities. The increasing number of publications indicates the importance of molecular hybridization on the field of drug discovery.

scholarly journals DESIGN, SYNTHESIS AND ANTIMICROBIAL STUDIES OF 5-BENZYLIDENE SUBSTITUTED RHODANINE CONTAINING HETEROCYCLES

2021 ◽  
pp. 28-34
Author(s):  
CICI MATHEW ◽  
BINDU SARASWATI ◽  
NAND LAL ◽  
JOYAMMA VARKEY
Keyword(s):  
Antibacterial Activity ◽  
Antifungal Activity ◽  
Candida Tropicalis ◽  
Candida Glabrata ◽  
Antimicrobial Agents ◽  
Biological Activities ◽  
Antimicrobial Activities ◽  
Design Synthesis ◽  
Drug Candidates ◽  
Antimicrobial Studies

Objective: The principal objective of the study was to synthesize and evaluate the biological activities of a novel class of 5-benzylidene substituted rhodanine derivatives as antimicrobial agents. Methods: All the synthesized compounds (D1-D10) were screened for their antimicrobial activities using microdilution methods as per the reported procedure. All compounds were evaluated as potential antimicrobial agents against gram-positive bacteria: Bacillus cereus, Staphylococcus aureus, gram negative bacteria: Escherichia coli Pseudomonas aeruginosa and Klebsiella pneumoniae Fungal cultures used in the study were Aspergillus niger, Candida albicans, Candida parapsilosis, Candida tropicalis and Candida glabrata. Results: Compound D6 showed good antifungal activity in the MIC range 16μg/ml against Candida tropicalis and Compound D10 showed good antifungal activity in the MIC range 16μg/ml against Candida glabrata. Compounds D2 and D5 showed good antibacterial activity at 32μg/ml. all the other compounds showed moderate antibacterial activity. Conclusion: Based on the above results, it can be concluded that the compounds may lead to the development of more potent antimicrobial drug candidates in the near future.

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.

Click Reactions in Chemistry of Triterpenes - Advances Towards Development of Potential Therapeutics

2018 ◽  
Vol 25 (5) ◽  
pp. 636-658 ◽  
Author(s):  
Jan Pokorny ◽  
Lucie Borkova ◽  
Milan Urban
Keyword(s):  
Biological Activities ◽  
Synthetic Approach ◽  
Clinical Use ◽  
New Approach ◽  
Click Reactions ◽  
Drug Candidates ◽  
The Past ◽  
Low Toxicity ◽  
New Compounds ◽  
Potential Therapeutics

Triterpenoids are natural compounds with a large variety of biological activities such as anticancer, antiviral, antibacterial, antifungal, antiparazitic, antiinflammatory and others. Despite their low toxicity and simple availability from the natural resources, their clinical use is still severely limited by their higher IC50 and worse pharmacological properties than in the currently used therapeutics. This fact encouraged a number of researchers to develop new terpenic derivatives more suitable for the potential clinical use. This review summarizes a new approach to improve both, the activity and ADME-Tox properties by connecting active terpenes to another modifying molecules using click reactions. Within the past few years, this synthetic approach was well explored yielding a lot of great improvements of the parent compounds along with some less successful attempts. A large quantity of the new compounds presented here are superior in both activity and ADME-Tox properties to their parents. This review should serve the researchers who need to promote their hit triterpenic structures towards their clinical use and it is intended as a guide for the chemical synthesis of better drug candidates.

Potential Triazole-based Molecules for the Treatment of Neglected Diseases

2019 ◽  
Vol 26 (23) ◽  
pp. 4403-4434 ◽  
Author(s):  
Susimaire Pedersoli Mantoani ◽  
Peterson de Andrade ◽  
Talita Perez Cantuaria Chierrito ◽  
Andreza Silva Figueredo ◽  
Ivone Carvalho
Keyword(s):  
Effective Treatment ◽  
Chagas Disease ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Neglected Diseases ◽  
Triazole Derivatives ◽  
Wide Range ◽  
The World ◽  
Great Relevance ◽  
The Moment

Neglected Diseases (NDs) affect million of people, especially the poorest population around the world. Several efforts to an effective treatment have proved insufficient at the moment. In this context, triazole derivatives have shown great relevance in medicinal chemistry due to a wide range of biological activities. This review aims to describe some of the most relevant and recent research focused on 1,2,3- and 1,2,4-triazolebased molecules targeting four expressive NDs: Chagas disease, Malaria, Tuberculosis and Leishmaniasis.

Synthesis and Biological Activity of Quaternary Quinolinium Salts: A Review

2020 ◽  
Vol 23 (21) ◽  
pp. 2271-2294 ◽  
Author(s):  
Divya Utreja ◽  
Shivali Sharma ◽  
Akhil Goyal ◽  
Komalpreet Kaur ◽  
Sonia Kaushal
Keyword(s):  
Tyrosine Kinases ◽  
Biological Activities ◽  
Polymeric Materials ◽  
Tubulin Polymerization ◽  
Quinoline Derivatives ◽  
Heterocyclic Chemistry ◽  
Biological Profile ◽  
Drug Candidates ◽  
Anti Hiv ◽  
Quinolinium Salts

Heterocyclic chemistry is the only branch of chemistry that has applications in varied areas such as dyes, photosensitizers, coordination compounds, polymeric materials, biological, and many other fields. Quinoline and its derivatives have always engrossed both synthetic chemists and biologists because of their diverse chemical and pharmacological properties as these ring systems can be easily found in various natural products, especially in alkaloids. Among alkaloids, quinoline derivatives i.e. quinolinium salts have attracted much attention nowadays owing to their diverse biological profile such as antimicrobial, antitumor, antifungal, hypotensive, anti-HIV, analgesics and anti-inflammatory, etc. Quinoline and its analogs have recently been examined for their modes of function in the inhibition of tyrosine kinases, proteasome, tubulin polymerization, topoisomerase, and DNA repair. These observations have been guiding scientists for the expansion of new quinoline derivatives with improved and varied biological activities. Quinolinium salts have immense possibilities and scope to investigate these compounds as potential drug candidates. Therefore, we shall present a concise compilation of this work to aid in present knowledge and to help researchers explore an interesting quinoline class having medicinal potential.

Synthesis and Biological Activity of Hydrazones and Derivatives: A Review

2020 ◽  
Vol 20 (5) ◽  
pp. 342-368 ◽  
Author(s):  
Juliana de Oliveira Carneiro Brum ◽  
Tanos Celmar Costa França ◽  
Steven R. LaPlante ◽  
José Daniel Figueroa Villar
Keyword(s):  
Biological Activity ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
New Drugs ◽  
New Drug ◽  
Cancer Inflammation

Hydrazones and their derivatives are very important compounds in medicinal chemistry due to their reported biological activity for the treatment of several diseases, like Alzheimer’s, cancer, inflammation, and leishmaniasis. However, most of the investigations on hydrazones available in literature today are directed to the synthesis of these molecules with little discussion available on their biological activities. With the purpose of bringing lights into this issue, we performed a revision of the literature and wrote this review based on some of the most current research reports of hydrazones and derivatives, making it clear that the synthesis of these molecules can lead to new drug prototypes. Our goal is to encourage more studies focused on the synthesis and evaluation of new hydrazones, as a contribution to the development of potential new drugs for the treatment of various diseases.

Antimicrobial Potential of Benzimidazole Derived Molecules

2019 ◽  
Vol 19 (8) ◽  
pp. 624-646 ◽  
Author(s):  
Yogita Bansal ◽  
Manjinder Kaur ◽  
Gulshan Bansal
Keyword(s):  
Biological Activities ◽  
Benzimidazole Derivative ◽  
Structural Similarity ◽  
Living System ◽  
Axial Ligand ◽  
Benzimidazole Derivatives ◽  
Research Groups ◽  
Structural Resemblance ◽  
Privileged Structure ◽  
Anti Hiv

Structural resemblance of benzimidazole nucleus with purine nucleus in nucleotides makes benzimidazole derivatives attractive ligands to interact with biopolymers of a living system. The most prominent benzimidazole compound in nature is N-ribosyldimethylbenzimidazole, which serves as an axial ligand for cobalt in vitamin B12. This structural similarity prompted medicinal chemists across the globe to synthesize a variety of benzimidazole derivatives and to screen those for various biological activities, such as anticancer, hormone antagonist, antiviral, anti-HIV, anthelmintic, antiprotozoal, antimicrobial, antihypertensive, anti-inflammatory, analgesic, anxiolytic, antiallergic, coagulant, anticoagulant, antioxidant and antidiabetic activities. Hence, benzimidazole nucleus is considered as a privileged structure in drug discovery, and it is exploited by many research groups to develop numerous compounds that are purported to be antimicrobial. Despite a large volume of research in this area, no novel benzimidazole derived compound has emerged as clinically effective antimicrobial drug. In the present review, we have compiled various reports on benzimidazole derived antimicrobials, classified as monosubstituted, disubstituted, trisubstituted and tetrasubstituted benzimidazoles, bisbenzimidazoles, fused-benzimidazoles, and benzimidazole derivative-metal complexes. The purpose is to collate these research reports, and to generate a generalised outlay of benzimidazole derived molecules that can assist the medicinal chemists in selecting appropriate combination of substituents around the nucleus for designing potent antimicrobials.

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