Heterocyclic rings have long piqued the interest of medicinal chemists. Quinazolinone is a fused nitrogen‐based heterocyclic moiety. Some of quinazolinone derivatives have emerged as marketed drugs. A tremendous number of pharmacological activities such as anticancer, anticonvulsant, antimalarial, antifungal, antibacterial, antiinflammatory, MMP inhibitors, antidiabetic, antileishmanial, and hypolipidemic properties have been explored. A number of quinazolinone derivatives have already paved way in various stages of clinical trials. An extensive literature on developed synthetic schemes based on green chemistry and biological activities of quinazolinone has been included in this study. The content of patent filed and granted of various quinazolinone‐based compounds are also mentioned.

Histone deacetylases (HDACs) are essential for maintaining homeostasis by catalyzing histone deacetylation. Aberrant expression of HDACs is associated with various human diseases. Although HDAC inhibitors are used as effective chemotherapeutic agents in clinical practice, their applications remain limited due to associated side effects induced by weak isoform selectivity. HDAC1 displays unique structure and cellular localization as well as diverse substrates and exhibits a wider range of biological functions than other isoforms. HDAC1 displays a unique structure primarily found in the nucleus and involved in epigenetic and transcriptional regulation.HDAC1 is ubiquitously expressed and associated with Sin3, NuRD, and CoRest transcription repressive complexes responsible for distinct cellular processes like cell proliferation and survival.HDAC1 inhibitors have been effectively used to treat various cancers such as gastric, breast, colorectal, prostate, colon, lung, ovarian, pancreatic, and inflammation reactions without exerting significant toxic effects. In this review, we summarize four major structural classes of HDAC1 inhibitors (i.e., hydroxamic acid derivatives, benzamides, hydrazides, and thiols) with their structural activity relationship. This review is a comprehensive work on HDAC1 inhibitors to achieve deep insight of knowledge about the structural information of HDAC1 inhibitors. It may provide up-to-date direction for the development of new selective HDAC1 inhibitors as anticancer agents.

The 4‐thiazolidinone moiety is a privileged scaffold showing diversity in biological responses like antiinflammatory, antidiabetic, anticancer, antitubercular, anesthetic, hypnotic, antiviral and many more. As a result of this, researchers have been studying and synthesizing this class of heterocycles through several simple as well as complex pathways as the target scaffold for biological studies. This review recapitulates the recent advances in the chemical and biological activities of 4‐thiazolidinones that have proved to be of immense importance in the discovery and development of several molecules and, thereby, the treatment of many ailments. This study will add to previously published reviews by examining the research on various biological activities of 4‐thiazolidinones, including patents, with a focus on structure–activity relationship (SAR) investigations. Literature and patents emphasizing synthetic schemes and biological activities of 4‐thiazolidinones have covered the data in the last decade. Here, sufficient efforts have been put into place to compile the synthetic strategies, establish SARs and enlist various patents so far for this fantastic molecule. The facile synthetic schemes and a vast range of biological activity profiles possessed by this nucleus may provide researchers with new opportunities toward novel therapeutics.

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Acquired immune deficiency syndrome (AIDS) caused by human immunodeficiency virus continues to scavenge lives of millions around the world. Reverse transcriptase (RT) also known as the RNA-directed DNA polymerase enzyme is responsible for converting RNA into viral DNA through process known as reverse transcription. Investigations on the pathogenic aspects of the RT enzyme, its associated elements such as gag (group-specific antigen gene), pol (polymerase gene), and env (environmental gene) (envelope gene) reveals its contribution towards emergence of resistance to all various anti-HIV drugs. Therefore, research into the control and blockage of the RT pathway has been a prominent focus in the quest for novel targets for HIV treatment. A slew of heterocyclics has been claimed to play a significant part in the fight against doomy HIV, saving the lives of millions of people throughout the world and providing hope for HIV treatment. Due to their improved potency and selectivity, as well as the fact that they have fewer off-target effects against the several targets implicated in RT inhibition, heterocyclics are becoming more and more useful. The RT inhibition pathway, the function of numerous heterocyclic scaffolds, and their ability to inhibit the RT enzyme pathway have all been the main topics of this paper. Recent advances in RT inhibitors in the last eight years (2014-2022) including mechanisms of action, preclinical and clinical investigations, structural activity relationships, and docking studies, to investigate mechanistic studies that would eventually aid in the design and development of powerful RT inhibitors have also discussed.