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.
Development in the medicinal chemistry of quinazolinone. SAR have been described. In vitro and in vivo biological activities
Tuberculosis (TB) is an airborne infection caused by the bacteria Mycobacterium Tuberculosis (MTB). It mainly affects the lungs and causes severe coughing, fever, and chest pains. With the rising ...prevalence of drug-resistant and inactive Tuberculosis (TB), there is an essential need to discover more effective molecules capable of combating this heinous illness. Pyrazinamide is a first-line tuberculosis therapy that shortens prophylactic duration from twelve to six months. The majority of presently used tuberculosis medications were found by a mix of serendipity and innovative chemical alterations of an existing lead drug. Given that the majority of these discoveries occurred years ago, there is a definite need to use fresh methodologies and technology for discovery to meet the grave danger posed by tuberculosis and the rise of treatment resistance strains. Although current research has provided significant insight into TB transmission, diagnosis, and treatment in the last four years, much more progress is needed to successfully reduce tuberculosis prevalence and eventually eradicate it. The disease continues to be a public health concern, second only to HIV/AIDS in high fatality rates. This review focuses on current efforts to translate the anti-tubercular activity of all known pyrazinamide analogues and proposes a novel approach for developing new anti-tubercular drugs based on the fusion of pyrazinamide with various heterocyclic rings that shorten treatment for drug-sensitive and multidrug-resistant tuberculosis.
•Design strategy and rational approach has been incorporated.•Basic synthetic strategy of Purine is discussed.•Various structural activity and purine exploitation at 2, 6, 7 and 9 position.•Numerous ...pathways and cancer-causing targets inhibitors possessing purine derivatives are discussed.•Detailed structural activity relationships of the compounds are discussed.
Impacting the lives of millions throughout the globe, cancer is the world's leading cause of death. In cancer treatment and prognosis, a number of anticancer medicines have been known to perform crucial roles. Nonetheless, despite advancements, developed drugs have fallen short of the mark, and cancer research is now at a crossroads, requiring a new paradigm in designing innovative anticancer agents with multitargeted effects that not only increase drug efficacy but also eliminate associated drug side-effects. Purine is a fused imidazole and pyrimidine ring found in human biomolecules such as ATP, GTP, NADH, alkaloids, and other coenzymes. Purine moiety heterocycles can be rewarded with significant anticancer activity, and tampered with in a range of places whereby several purine derivatives have previously received approval to treat cancer. These biomolecules have the potential to interact with numerous signalling pathways. Considering this characteristic of the purine moiety, its synthetic derivatives and research are of keen interest in the creation of inductive approach medications. This article discusses the potential of the purine moiety based on various targets of cancer as a novel anticancer treatment synthesized between 2017-2022 in response to the challenge of drug resistance in cancer therapy. The data assembled are based on purine SARs, Ki, IC50 values, in silico computational investigations along with their reported X-ray co-crystal structures of cancer targeting proteins. We are certain that the current review study will assist future medicinal researchers in their investigation of rational approaches for the development and design of selective and specific cancer targets with their medications in a range of clinical contexts.
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Multidrug-resistant tuberculosis continues to pose a health security risk and remains a public health emergency. Antimicrobial resistance result from treatment regimens that are both ...insufficient and incomplete leading to the emergence of multidrug-resistant tuberculosis, extensively drug-resistant tuberculosis and totally drug-resistant tuberculosis. The impact of tuberculosis on the people suffering from HIV (Human immunodeficiency virus infection) have resulted in the increased research efforts in designing and discovery of novel antitubercular drugs that may result in decreasing treatment duration, minimising the need for multiple drug intake, minimising cytotoxicity and enhancing the mechanism of action of drug. While many drugs are available to treat tuberculosis, a precise and timely cure is still absent. Consequently, further investigation is needed to identify more recent molecular equivalents that have the potential to swiftly remove this disease. Isoniazid (INH), a treatment for tuberculosis (TB), targets the enzyme InhA (mycobacterium enoyl acyl carrier protein reductase), the Mycobacterium tuberculosis enoyl-acyl carrier protein (ACP) reductase, most common INH resistance is circumvented by InhA inhibitors that do not require KatG (catalase-peroxidase) activation, as a result, researchers are trying to work in the area of development of InhA inhibitors which could help in eradicating the era of tuberculosis from the world.
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.
Various biological activities of 4‐thiazolidinone moeities.
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 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 developing new selective HDAC1 inhibitors as anticancer agents.
Cancer growth, annexation, and metastatic spread are all aided by the formation of new blood vessels (angiogenesis). The commencement of the VEGF pathway leads to signal transduction that enhances ...endothelial cell survival, relocation, and divergence from pre‐existing vasculature. The ability of solid malignancies to bloom and spread depends critically on their ability to establish their independent blood circulation (tumor angiogenesis). VEGFR is a major receptor tyrosine kinase that regulates angiogenesis, cell growth, and metastasis, diminishing apoptosis, cytoskeletal function, and other biological processes VEGFR has proven to be a remarkable focus for a variety of anticancer medicines in clinical studies. This Review explores the development of anti‐VEGF‐based antiangiogenic therapies having different scaffolds. This review had focused on SAR and docking studies of previously reported molecules.
Abstract Butadienyl ketene is a useful intermediate because of its role as a 2p-component in cycloaddition reactions with a variety of substrates such as simple or conjugated imines and dienes. This ...review article summarizes recent reports on the generation of butadienyl ketene in situ and their cycloaddition reactions to afford heterocyclic systems. The chemistry of butadienyl ketene is explored with a focus on its 2+2 and 4+2 cycloaddition reactions with a variety of imines and azadiene derivatives such as 1,3-diazabuta-1,3-dienes, for the synthesis of four- and six-membered heterocycles, respectively.
Abstract
A highly eco-friendly greener approach based on the mechanochemical method using mortar and pestle is explored for the preparation of a variety of functionalized 4-thiazolidinones. The ...developed methodology does not require the use of harmful or expensive reagents and organic solvents and requires very less reaction time with easy isolation. The explored greener approach for the synthesis of 4-thiazolidinones is an important in terms of their usefulness for their valuable pharmacological properties.
