scholarly journals Microwave-assisted multicomponent reactions in heterocyclic chemistry and mechanistic aspects

2021 ◽  
Vol 17 ◽  
pp. 819-865
Author(s):  
Shivani Gulati ◽  
Stephy Elza John ◽  
Nagula Shankaraiah
Keyword(s):  
Multicomponent Reactions ◽  
Multiple Point ◽  
Heterocyclic Chemistry ◽  
Biologically Relevant ◽  
Microwave Assisted ◽  
The Past ◽  
High Yields ◽  
Microwave Assistance ◽  
Enhanced Yield ◽  
Shed Light

Microwave-assisted (MWA) multicomponent reactions (MCRs) have successfully emerged as one of the useful tools in the synthesis of biologically relevant heterocycles. These reactions are strategically employed for the generation of a variety of heterocycles along with multiple point diversifications. Over the last few decades classical MCRs such as Ugi, Biginelli, etc. have witnessed enhanced yield and efficiency with microwave assistance. The highlights of MWA-MCRs are high yields, reduced reaction time, selectivity, atom economy and simpler purification techniques, such an approach can accelerate the drug discovery process. The present review focuses on the recent advances in MWA-MCRs and their mechanistic insights over the past decade and shed light on its advantage over the conventional approach.

Synthesis of Drugs and Biorelevant N-heterocycles Employing Recent Advances in C-N Bond Formation

2020 ◽  
Vol 24 (20) ◽  
pp. 2293-2340
Author(s):  
Firdoos Ahmad Sofi ◽  
Prasad V. Bharatam
Keyword(s):  
Kinase Inhibitors ◽  
Bond Formation ◽  
Comprehensive Review ◽  
Biologically Relevant ◽  
Lead Compounds ◽  
Heterocyclic Molecules ◽  
The Past ◽  
Anti Cancer ◽  
Modern Methods ◽  
Bond Formation Reactions

C-N bond formation is a particularly important step in the generation of many biologically relevant heterocyclic molecules. Several methods have been reported for this purpose over the past few decades. Well-known named reactions like Ullmann-Goldberg coupling, Buchwald-Hartwig coupling and Chan-Lam coupling are associated with the C-N bond formation reactions. Several reviews covering this topic have already been published. However, no comprehensive review covering the synthesis of drugs/ lead compounds using the C-N bond formation reactions was reported. In this review, we cover many modern methods of the C-N bond formation reactions, with special emphasis on metal-free and green chemistry methods. We also report specific strategies adopted for the synthesis of drugs, which involve the C-N bond formation reactions. Examples include anti-cancer, antidepressant, anti-inflammatory, anti-atherosclerotic, anti-histaminic, antibiotics, antibacterial, anti-rheumatic, antiepileptic and anti-diabetic agents. Many recently developed lead compounds generated using the C-N bond formation reactions are also covered in this review. Examples include MAP kinase inhibitors, TRKs inhibitors, Polo-like Kinase inhibitors and MPS1 inhibitors.

Reactivity of Barbituric, Thiobarbituric Acids and Their Related Analogues: Synthesis of Substituted and Heterocycles-based Pyrimidines

2020 ◽  
Vol 24 (14) ◽  
pp. 1610-1642 ◽  
Author(s):  
Ahmed El-Mekabaty ◽  
Hassan A. Etman ◽  
Ahmed Mosbah ◽  
Ahmed A. Fadda
Keyword(s):  
Xanthine Oxidase ◽  
Multicomponent Reactions ◽  
Biological Activities ◽  
Present Review ◽  
Urease Inhibitors ◽  
Effective Catalyst ◽  
Inhibitory Activities ◽  
Catalyst Reusability ◽  
High Yields ◽  
Nano Catalysts

Barbituric, thiobarbituric acids and their related analogs are reactive synthons for the synthesis of drugs and biologically, and pharmaceutically active pyrimidines. The present review aimed to summarize the recent advances in the synthesis of different alkylsubstituted, fused cycles, spiro-, and binary heterocycles incorporated pyrimidine skeleton based on barbituric derivatives. In this sequence, the eco-friendly techniques under catalytic conditions were used for the diverse types of multicomponent reactions under different conditions for the synthesis of various types of heterocycles. Nano-catalysts are efficient for the synthesis of these compounds in high yields and effective catalyst reusability. The compounds are potent antibacterial, cytotoxic, xanthine oxidase inhibitory activities, and attend as urease inhibitors. The projected mechanisms for the synthesis of pyranopyrimidines, benzochromenopyrimidines, chromeno-pyranopyrimidines, spiroxyindoles, oxospiro-tricyclic furopyrimidines, pyrimidine-based monoand bicyclic pyridines were discussed. The potent and diverse biological activities for instance, antioxidant, antibacterial, cytotoxic, and xanthine oxidase inhibitory activities, as well as urease inhibitors, are specified.

Microwave Assisted Organic Synthesis: Cross Coupling and Multicomponent Reactions

2013 ◽  
Vol 17 (5) ◽  
pp. 474-490 ◽  
Author(s):  
Amit Kumar Gupta ◽  
Neetu Singh ◽  
Krishna Nand Singh
Keyword(s):  
Organic Synthesis ◽  
Multicomponent Reactions ◽  
Cross Coupling ◽  
Microwave Assisted

Reputation and Gossip in Game Theory

2019 ◽  
pp. 213-229
Author(s):  
Charles Roddie
Keyword(s):  
Game Theory ◽  
Strategic Behavior ◽  
Third Party ◽  
The Past ◽  
Past Behavior ◽  
Future Behavior ◽  
The Game Theory ◽  
Shed Light

When interacting with others, it is often important for you to know what they have done in similar situations in the past: to know their reputation. One reason is that their past behavior may be a guide to their future behavior. A second reason is that their past behavior may have qualified them for reward and cooperation, or for punishment and revenge. The fact that you respond positively or negatively to the reputation of others then generates incentives for them to maintain good reputations. This article surveys the game theory literature which analyses the mechanisms and incentives involved in reputation. It also discusses how experiments have shed light on strategic behavior involved in maintaining reputations, and the adequacy of unreliable and third party information (gossip) for maintaining incentives for cooperation.

scholarly journals Evolution of Cancer Vaccines—Challenges, Achievements and Future Directions

Vaccines ◽  
2021 ◽  
Vol 9 (5) ◽  
pp. 535
Author(s):  
Ban Qi Tay ◽  
Quentin Wright ◽  
Rahul Ladwa ◽  
Christopher Perry ◽  
Graham Leggatt ◽  
...  
Keyword(s):  
Cancer Vaccines ◽  
New Drugs ◽  
Delivery Methods ◽  
Future Directions ◽  
The Past ◽  
New Directions ◽  
Tumour Antigens ◽  
Target Characteristics ◽  
Toxic Responses ◽  
Shed Light

The development of cancer vaccines has been intensively pursued over the past 50 years with modest success. However, recent advancements in the fields of genetics, molecular biology, biochemistry, and immunology have renewed interest in these immunotherapies and allowed the development of promising cancer vaccine candidates. Numerous clinical trials testing the response evoked by tumour antigens, differing in origin and nature, have shed light on the desirable target characteristics capable of inducing strong tumour-specific non-toxic responses with increased potential to bring clinical benefit to patients. Novel delivery methods, ranging from a patient’s autologous dendritic cells to liposome nanoparticles, have exponentially increased the abundance and exposure of the antigenic payloads. Furthermore, growing knowledge of the mechanisms by which tumours evade the immune response has led to new approaches to reverse these roadblocks and to re-invigorate previously suppressed anti-tumour surveillance. The use of new drugs in combination with antigen-based therapies is highly targeted and may represent the future of cancer vaccines. In this review, we address the main antigens and delivery methods used to develop cancer vaccines, their clinical outcomes, and the new directions that the vaccine immunotherapy field is taking.

scholarly journals Imidazole: Having Versatile Biological Activities

2013 ◽  
Vol 2013 ◽  
pp. 1-12 ◽  
Author(s):  
Amita Verma ◽  
Sunil Joshi ◽  
Deepika Singh
Keyword(s):  
Natural Products ◽  
Nucleic Acid ◽  
Biological Activities ◽  
Imidazole Ring ◽  
Heterocyclic Ring ◽  
Heterocyclic Chemistry ◽  
The Past ◽  
Poorly Soluble ◽  
Anti Hiv ◽  
Imidazole Compounds

Imidazoles have occupied a unique position in heterocyclic chemistry, and its derivatives have attracted considerable interests in recent years for their versatile properties in chemistry and pharmacology. Imidazole is nitrogen-containing heterocyclic ring which possesses biological and pharmaceutical importance. Thus, imidazole compounds have been an interesting source for researchers for more than a century. The imidazole ring is a constituent of several important natural products, including purine, histamine, histidine, and nucleic acid. Being a polar and ionisable aromatic compound, it improves pharmacokinetic characteristics of lead molecules and thus is used as a remedy to optimize solubility and bioavailability parameters of proposed poorly soluble lead molecules. There are several methods used for the synthesis of imidazole-containing compounds, and also their various structure reactions offer enormous scope in the field of medicinal chemistry. The imidazole derivatives possess extensive spectrum of biological activities such as antibacterial, anticancer, antitubercular, antifungal, analgesic, and anti-HIV activities. This paper aims to review the biological activities of imidazole during the past years.

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