Εξειδίκευση τύπου :	Άρθρο σε επιστημονικό περιοδικό
Τίτλος:	Synthesis and evaluation of nitroheterocyclic aromatic adamantane amides with trypanocidal activity. Part II
Δημιουργός/Συγγραφέας:	Foscolos, Angeliki-Sofia Atherton, Richard L Billia, Maria Georgiadis, Markos-Orestis Santarém, Nuno da Silva, Anabela Cordeiro Taylor, Martin C Kelly, John M [EL] Καλογεροπούλου, Θεοδώρα[EN] Calogeropoulou, Theodora Tsotinis, Andrew [EL] Μαυρομούστακος, Θωμάς[EN] Mavromoustakos, Thomas Papanastasiou, Ioannis P
Ημερομηνία:	2025-11-06
Γλώσσα:	Αγγλικά
DOI:	10.1039/d5md00527b
Άλλο:	41355869
Περίληψη:	In this article, we report the design, synthesis, and biological evaluation of a new series of nitroheterocyclic aromatic adamantane amides targeting trypanosomes. These compounds feature diverse substituents on the adamantane scaffold, variations in side chain linker length, and a range of nitroheterocyclic moieties. This work represents a continuation of our previous efforts, with a particular focus on elucidating the structural and functional role of the linker connecting the phenyladamantane core to the nitroheterocyclic ring. The structure-activity relationship data underscore the importance of strategic modifications in enhancing the pharmacological profile of these compounds against trypanosome parasites. Further modifications are recommended to optimize the physicochemical properties of the current derivatives to improve intracellular targeting of trypanosomatids, an important clinical stage in their life cycle.
Τίτλος πηγής δημοσίευσης:	RSC medicinal chemistry
Θεματική Κατηγορία:	[EL] Φαρμακευτική χημεία[EN] Pharmaceutical chemistry [EL] Θεραπευτική. Φαρμακολογία[EN] Therapeutics.Pharmacology [EL] Τοξικολογία[EN] Toxicology. Poisons [EL] Μικροβιολογία[EN] Microbiology [EL] Οργανική χημεία[EN] Organic chemistry
Λέξεις-Κλειδιά:	Trypanocidal activity Adamantane derivatives Nitroheterocyclic compounds Neglected Tropical Diseases (NTDs) Selectivity Index (SI)
Όροι και προϋποθέσεις δικαιωμάτων:	This article is Open Access.
Ηλεκτρονική διεύθυνση στον εκδότη (link):	https://doi.org/10.1039/D5MD00527B
Εμφανίζεται στις συλλογές:	Ινστιτούτο Χημικής Βιολογίας - Επιστημονικό έργο