Medicinal Chemistry - Project Leader; Technology Innovation & External Platforms presso Alfasigma - parla di #scienze #farmaci #farmaceutico #ricerca #innovazione #sociale
RECENT DEVELOPMENTS TOWARDS THE SYNTHESIS OF TRIAZOLE DERIVATIVES, IN MEDICINAL CHEMISTRY Heterocyclic chemistry is a broad and important field within medicinal chemistry, due to its extensive applications in drug design and discovery. Heterocyclic bioactive molecules, which contain heteroatoms such as nitrogen, oxygen, and sulfur, play a crucial role in biological applications. Among these, azoles, which are five-membered heterocyclic compounds, are key structural components in various biologically active natural products. The core structures of azoles include triazole, oxazole, oxadiazole, tetrazole, pentazole, pyrazole, imidazole, thiadiazole, and thiazole ring systems. These compounds exhibit diverse biological activities, such as antibacterial, anticancer, antiviral, anti-inflammatory, antimalarial, and antituberculosis properties. Azoles possess several key characteristics of highly potent antifungal agents, and this class of compounds has played a crucial role in controlling both invasive and superficial fungal infections. Amongst azoles, triazoles are especially important heterocyclic compounds due to their excellent pharmacological properties and their role as essential components in cells and organisms. The term “triazole” was first introduced by Bladin in the early 1880s. Triazoles are heterocyclic compounds with molecular formula C2H3N3 consisting of a ring with three nitrogen atoms and two carbon atoms. They exist in two isomeric forms, 1,2,3-triazole and 1,2,4-triazole, which can exhibit tautomerism based on the position of the hydrogen atom. Triazoles interact readily with proteins, enzymes, and receptors in organisms, giving them a wide range of biological activities. These include antifungal, anticancer, antiviral, and antibacterial effects. Their derivatives have been extensively utilized in various medicinal scaffolds. For instance, Itraconazole (1992), Fluconazole (1990), and Voriconazole (2002), widely used antifungals. Ribavirin (2003), a broad-spectrum antiviral drug employed in the treatment of hepatitis. Rizatriptan (1998), an antimigraine agent. Letrozole (1997), Anastrozole (2000), Talazoparib (2018), and Vorozole (1984) as anticancer drugs. Rufinamide (2008), approved by the FDA for treating pediatric epilepsy. Tazobactam (1986) is an antibiotic, and Maraviroc (2007) is an anti-HIV drug. Issam Ameziane El Hassani et al., have just published (open access) in Organics 2024, a concise overview of triazole pharmacophore synthesis and serves as a valuable resource for researchers in the field. #Triazole #TriazoleChemistry https://lnkd.in/dzrq5aGA
"Recent Developments Towards the Synthesis of Triazole Derivatives: A Review" From their Abstract Triazoles are a key part of heterocyclic chemistry, acting as essential building blocks in organic synthesis, materials science, and medicinal chemistry. They form a five-membered ring with three nitrogen and two carbon atoms and exist in two isomeric forms: 1,2,3-triazole and 1,2,4-triazole. Triazole compounds are noted for their wide range of biological activities, including antimicrobial, anticancer, and anti-inflammatory properties. This excellent review (open access) provides a comprehensive look at the synthesis of triazole derivatives, covering both traditional methods and modern techniques like microwave and ultrasound-assisted methods. Source: Issam Ameziane El Hassani et al. Recent Developments Towards the Synthesis of Triazole Derivatives: A Review. Organics 2024, 5, 450-471. https://lnkd.in/gj9tNzRY; https://lnkd.in/ggd3W4Tk #heterocyclic #1_2_3_triazole #1_2_4_triazole #microwave #ultrasound #green_chemistry #synthetic_reactions
