Synthesis and Anticancer Perspective of Pyridopyrimidine Scaffold - An Overview

The core pyridopyrimidines are gaining interest in organic and heterocyclic chemistry in recent days, as this scaffold acts as a building block because of its wide range of biological and pharmacological applications like anticancer, antimicrobial, fungicidal, antiviral, CNS, antibacterial, and anti-inflammatory properties. This review mainly emphasizes the evolution in anticancer properties of pyridopyrimidines since 2008 especially the method of synthesis and anticancer activity of synthesized compounds with reporting of active anticancer scaffolds. Important starting materials which are widely used for the synthesis are 2-thioxopyrimidine, ethyl 2-cyanoacetate, 2-amino-3-cyano-4-trifluoromethyl-6-phenyl-pyridine, 2-amino-4,6-disubstituted nicotinonitrile, 2-chloro-3-pyridine carboxylic acid, in which 2-thioxopyrimidine is found to be mostly employed in the synthesis. Pyridopyrimidines which are synthesized from different starting materials, in which the more active compounds are reported here which may help in further discovery/ development of novel molecules.

Quinazoline and its diverse array of therapeutic application:A review

Heterocyclic chemistry being an important branch of chemistry includes many ring structures with heteroatoms such as nitrogen, oxygen, and sulfur. Quinazoline is an important nitrogen containing benzofused heterocycle and has several therapeutic actions such as antimalarial, antimicrobial, anticancer, and anticonvulsant. Quinazoline was first isolated from alkaloid vasicine. Vasicine, deoxyvasicine, tryptanthrin, and rutecarpine are some of the potent naturally occurring quinazolines. Substitutions on different positions of quinazoline ring lead to different activities. Detailed survey of activities of quinazoline such as anticancer, anticonvulsant, antifungal, antibacterial, and antidiabetic according to structure–activity relationship and marketed preparations containing quinazoline as an active moiety is described in this review.

An Important Potential Anti-Epileptic/Anticonvulsant Active Group: A Review of 1,2,4-Triazole Groups and Their Action

Epilepsy is one of the most common encountered neurological disorders. Many individuals continue to have seizures despite medical and surgical treatments, suggesting new antiepileptic/anticonvulsant drugs are required. Triazole compounds are widely used in pharmaceuticals and have gained significant importance in medicinal chemistry. This article is an attempt to systematically review the research of triazole derivatives in the design and development of anticonvulsant agents during the past two decades through extensive literature research. The results show that triazole occupy a distinct niche in heterocyclic chemistry and represent a key motif in medicinal chemistry because of their capability to exhibit an array of properties and bioactivities, Therefore, 1,2,4-triazole seems to be an important pharmacophore, especially in the field of antiepileptic, which is of great explored potentiality and utilized value. Through in-depth research on this type of structure, it is believed that more 1,2,4-triazole compounds will be developed as anti-epileptic drugs for clinical use.

A Meticulous Review on Coumarin Derivatives as a Marvel Medication for Thousands of Ailments

Coumarin derivatives have progressively enticed medicinal chemists because of their potential role in preventing and treating ailments. They epitomize a key motif nucleus in heterocyclic chemistry and a privileged structure in medicinal chemistry because of its extensive-range pharmacological activity. Regardless of the advancement in medicine over the past century, cancer is still remain the prominent source of death in the world and it makes indispensible needs to synthesize the compounds with coumarin as the core nucleus. Synthesis of various coumarin derivatives and evaluation of their pharmacological effects can perceive a solution to certain enigmatic demands in health sector. This review article is fixated on different synthetic routes of coumarin nucleus containing compounds. The review article also highlights different biological activities such as anticancer, antibacterial, anti- inflammatory, antihyperlipidemic and enzyme inhibition activities.

Heterocyclic Chemistry Applied to the Design of N-Acyl Homoserine Lactone Analogues as Bacterial Quorum Sensing Signals Mimics

N-acyl homoserine lactones (AHLs) are small signaling molecules used by many Gram-negative bacteria for coordinating their behavior as a function of their population density. This process, based on the biosynthesis and the sensing of such molecular signals, and referred to as Quorum Sensing (QS), regulates various gene expressions, including growth, virulence, biofilms formation, and toxin production. Considering the role of QS in bacterial pathogenicity, its modulation appears as a possible complementary approach in antibacterial strategies. Analogues and mimics of AHLs are therefore biologically relevant targets, including several families in which heterocyclic chemistry provides a strategic contribution in the molecular design and the synthetic approach. AHLs consist of three main sections, the homoserine lactone ring, the central amide group, and the side chain, which can vary in length and level of oxygenation. The purpose of this review is to summarize the contribution of heterocyclic chemistry in the design of AHLs analogues, insisting on the way heterocyclic building blocks can serve as replacements of the lactone moiety, as a bioisostere for the amide group, or as an additional pattern appended to the side chain. A few non-AHL-related heterocyclic compounds with AHL-like QS activity are also mentioned.

[3 + n] Cycloaddition Reactions: A Milestone Approach for Elaborating Pyridazine of Potential Interest in Medicinal Chemistry and Optoelectronics

During the last few decades, pyridazine derivatives have emerged as privileged structures in heterocyclic chemistry, both because of their excellent chemistry and because of their potential applications in medicinal chemistry and optoelectronics. This review is focused on the recent advances in [3 + n] cycloaddition reactions in the pyridazine series as well as their medicinal chemistry and optoelectronic applications over the last ten years. The stereochemistry and regiochemistry of the cycloaddition reactions are discussed. Applications in optoelectronics (in particular, as fluorescent materials and sensors) and medicinal chemistry (in particular, antimicrobials and anticancer) are also reviewed.

Practical and Regioselective Synthesis of C4-Alkylated Pyridines

The direct position-selective C–4 alkylation of pyridines has been a longstanding challenge in heterocyclic chemistry, particularly from pyridine itself. Historically this has been addressed using pre-functionalized materials to avoid overalkylation and mixtures of regioisomers. This study reports the invention of a simple maleate-derived blocking group for pyridines that enables exquisite control for Minisci-type decarboxylative alkylation at C–4 that allows for inexpensive access to these valuable building blocks. The method is employed on a variety of different pyridines and carboxylic acid alkyl donors, is operationally simple, scalable, and is applied to access known structures in a rapid and inexpensive fashion. Finally, this work points to an interesting strategic departure for the use of Minisci chemistry at the earliest possible stage (native pyridine) rather than current dogma that almost exclusively employs Minisci as a late-stage functionalization technique.

Practical and Regioselective Synthesis of C4-Alkylated Pyridines

The direct position-selective C–4 alkylation of pyridines has been a longstanding challenge in heterocyclic chemistry, particularly from pyridine itself. Historically this has been addressed using pre-functionalized materials to avoid overalkylation and mixtures of regioisomers. This study reports the invention of a simple maleate-derived blocking group for pyridines that enables exquisite control for Minisci-type decarboxylative alkylation at C–4 that allows for inexpensive access to these valuable building blocks. The method is employed on a variety of different pyridines and carboxylic acid alkyl donors, is operationally simple, scalable, and is applied to access known structures in a rapid and inexpensive fashion. Finally, this work points to an interesting strategic departure for the use of Minisci chemistry at the earliest possible stage (native pyridine) rather than current dogma that almost exclusively employs Minisci as a late-stage functionalization technique.

Practical and Regioselective Synthesis of C4-Alkylated Pyridines

The direct position-selective C–4 alkylation of pyridines has been a longstanding challenge in heterocyclic chemistry, particularly from pyridine itself. Historically this has been addressed using pre-functionalized materials to avoid overalkylation and mixtures of regioisomers. This study reports the invention of a simple maleate-derived blocking group for pyridines that enables exquisite control for Minisci-type decarboxylative alkylation at C–4 that allows for inexpensive access to these valuable building blocks. The method is employed on a variety of different pyridines and carboxylic acid alkyl donors, is operationally simple, scalable, and is applied to access known structures in a rapid and inexpensive fashion. Finally, this work points to an interesting strategic departure for the use of Minisci chemistry at the earliest possible stage (native pyridine) rather than current dogma that almost exclusively employs Minisci as a late-stage functionalization technique.

Microwave-assisted multicomponent reactions in heterocyclic chemistry and mechanistic aspects

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.