ABSTRACT
Heterocyclic hybrid frameworks represent a burgeoning domain within the realms of drug discovery and medicinal chemistry, attracting considerable attention in recent years. Thiazole pharmacophore fragments, inherent in natural products such as peptide alkaloids, metabolites, and cyclopeptides, have demonstrated a broad spectrum of pharmacological potentials. Given their profound biological significance, a plethora of thiazole-based hybrids have been synthesized through the conjugation of thiazole moieties with bioactive pyrazole and pyrazoline fragments. This review systematically presents a compendium of robust methodologies for the synthesis of thiazole-linked hybrids, employing the (3 + 2) heterocyclization reaction, specifically the Hantzsch-thiazole synthesis, utilizing phenacyl bromide as the substrate. The strategic approach of molecular hybridization has markedly enhanced drug efficacy, mitigated resistance to multiple drugs, and minimized toxicity concerns. The resultant thiazole-linked hybrids exhibit a myriad of medicinal properties viz. anticancer, antibacterial, anticonvulsant, antifungal, antiviral, and antioxidant activities. This compilation of methodologies and insights serves as a valuable resource for medicinal chemists and researchers engaged in the design of novel thiazole-linked hybrids endowed with therapeutic attribute.
ABSTRACT
Alzheimer's disease (AD) is a formidable neurodegenerative disorder characterized by cognitive decline, memory impairment and inability to perform everyday tasks. In the pursuit of innovative diagnostic and therapeutic strategies, the synthesis and application of radiolabelled compounds have garnered significant attention. This review delves into the synthesis and biological significance of radiolabelled 1,3-diaryl-2-propen-1-ones, commonly known as chalcones, as Aß imaging probes for AD. These versatile chalcone derivatives have demonstrated noteworthy potential as radiotracers for visualizing Aß imaging probes, which are hallmark pathologies of AD. This review encompasses an exploration of chalcone synthesis via diverse methodologies and their biological implications, both as standalone entities and as precursors for intricate natural products. In addition, the pivotal role of advanced imaging techniques, such as single-photon emission computed tomography (SPECT) and positron emission tomography (PET), using various radioisotopes is highlighted. The use of radiopharmaceutical agents, including [18F]FDG, [18F]FMAPO, [11C]6-Me-BTA-1, [124/125I]IBETA, and [64Cu]YW-7 as potent tools for early diagnosis and therapeutic advancement is explored. This review underscores the critical nexus between radiolabelled chalcones and their pivotal role in advancing diagnostic and therapeutic paradigms in AD research. Furthermore, this study encapsulated the role of radiolabelled chalcone emphasizing their prospective implications for drug development and therapeutic interventions. A focal point of paramount significance is the elucidation of Aß imaging probes and its important role in the combat against AD, with a particular emphasis on their role in facilitating early diagnosis and fostering advancements in therapeutic strategies.
ABSTRACT
The aim of this review is to encapsulate the synthetic protocols and medicinal aspects of a wide range of heterocyclic compounds using the Vilsmeier-Haack (V. H.) reagent. These derivatives act as excellent precursors having different aryl ring functionalities and could be used for the synthesis of a variety of heterocyclic scaffolds. The V. H. reagent, a versatile reagent in organic chemistry, is used to formylate various heterocyclic compounds of medicinal interest. Due to the different chemical interactions, efficacy, and potency of V. H. reagents, plenty of heterocyclic compounds can be synthesized which serve as a constituent in various novel medications and acts as a bridge between biology and chemistry. These carboxylate moieties can effectively cooperate as precursors for several multi-component reactions (MCR) including Strecker synthesis, Bucherer-Berg reaction and post-MCR cyclization, modified variants with various pharmaceutical applications such as anti-tumor, anti-convulsant, anti-chitosomal and so on.
