Publications

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5 Publications visible to you, out of a total of 5
Synthesis and Evaluation of Nitroheterocyclic Aromatic Adamantanohydrazones with Trypanocidal Activity. Part III

Abstract

Not specified

Authors: Angeliki-Sofia Foscolos, Konstantina Stavropoulou, Nuno Santarém, Anabela Cordeiro da Silva, Martin C. Taylor, Theodora Calogeropoulou, Andrew Tsotinis, Ioannis P. Papanastasiou, John M. Kelly, Susan Wyllie

Date Published: 17th Jun 2026

Publication Type: Journal Article

Synthesis and evaluation of nitroheterocyclic aromatic adamantane amides with trypanocidal activity. Part II

Abstract

New nitroheterocyclic adamantane amides display promising trypanocidal activity. The spacer length between the adamantylphenyl backbone and the nitroheterocyclic ring plays a crucial role in potency.

Authors: Angeliki-Sofia Foscolos, Richard L. Atherton, Maria Billia, Markos-Orestis Georgiadis, Nuno Santarém, Anabela Cordeiro da Silva, Martin C. Taylor, John M. Kelly, Theodora Calogeropoulou, Andrew Tsotinis, Thomas Mavromoustakos, Ioannis P. Papanastasiou

Date Published: 2026

Publication Type: Journal Article

AgamOBP1‐Directed Discovery of Repellents to Control the Spread of Mosquito‐Borne Diseases

Abstract (Expand)

Toward the discovery of novel efficient repellents, protein‐directed dynamic combinatorial chemistry (pdDCC) coupled to saturation‐transfer difference (STD) NMR spectroscopy was initially employed to … identify modulators of the malaria vector Anopheles gambiae Odorant Binding Protein 1 (AgamOBP1). A library of potential binders of AgamOBP1 (secondary amines) generated from two amines and seven aldehydes was designed aiming to enable interactions with critical amino acids at the DEET‐site and to bridge the DEET‐ and Icaridin sIC‐binding pockets, both implicated in repellents recognition. Solubility issues hindered the clear identification of binders among the DCL members, except for one sublibrary, leading us to shift our strategy towards the synthesis of the designed amines, followed by direct evaluation of their binding to AgamOBP1 using 1 H STD NMR spectroscopy. The identified binders were further validated in vitro by fluorescence competition assays, and the most potent compounds which also possessed suitable vapor pressure were evaluated as repellents in arm‐in‐cage behavioral assays against Aedes albopictus . Amines 2A , 3A , 4A , and 6A showed significant repellent activity. The most potent was compound 4A (4‐methyl‐ N ‐(pyridin‐4‐ylmethyl)aniline) which acted as a a DEET‐like repellent at 0.4 μL cm − 2 dose. Thus, our strategy showcased a promising scaffold for further optimization toward efficient mosquito repellents.

Authors: Evanthia Chazapi, Eftichia Kritsi, Constantinos Potamitis, Panagiota G. V. Liggri, Katerina E. Tsitsanou, Christina E. Drakou, Antonios Michaelakis, Dimitrios P. Papachristos, Spyros E. Zographos, Maria Zervou, Theodora Calogeropoulou

Date Published: 21st Sep 2025

Publication Type: Journal Article

Design, synthesis and biological evaluation of antiparasitic dinitroaniline-ether phospholipid hybrids

Abstract (Expand)

A series of nine novel ether phospholipid-dinitroaniline hybrids were synthesized in an effort to deliver more potent antiparasitic agents with improved safety profile compared to miltefosine. The … compounds were evaluated for their in vitro antiparasitic activity against L. infantum, L.donovani, L. amazonensis, L. major and L. tropica promastigotes, L. infantum and L. donovani intracellular amastigotes, Trypanosoma brucei brucei and against different developmental stages of Trypanosoma cruzi. The nature of the oligomethylene spacer between the dinitroaniline moiety and the phosphate group, the length of the side chain substituent on the dinitroaniline and the choline or homocholine head group were found to affect both the activity and toxicity of the hybrids. The early ADMET profile of the derivatives did not reveal major liabilities. Hybrid 3, bearing an 11-carbon oligomethylene spacer, a butyl side chain and a choline head group, was the most potent analogue of the series. It exhibited a broad spectrum antiparasitic profile against the promastigotes of New and Old World Leishmania spp., against intracellular amastigotes of two L. infantum strains and L. donovani, against T. brucei and against T. cruzi Y strain epimastigotes, intracellular amastigotes and trypomastigotes. The early toxicity studies revealed that hybrid 3 showed a safe toxicological profile while its cytotoxicity concentration (CC50) against THP-1 macrophages being >100 μM. Computational analysis of binding sites and docking indicated that the interaction of hybrid 3 with trypanosomatid α-tubulin may contribute to its mechanism of action. Furthermore, compound 3 was found to interfere with the cell cycle in T. cruzi epimastigotes, while ultrastructural studies using SEM and TEM in T. cruzi showed that compound 3 affects cellular processes that result in changes in the Golgi complex, the mitochondria and the parasite’s plasma membrane. The snapshot pharmacokinetic studies showed low levels of 3 after 24 h following oral administration of 100 mg/Kg, while, its homocholine congener compound 9 presented a better pharmacokinetic profile.

Authors: Marina Roussaki, George E. Magoulas, Theano Fotopoulou, Nuno Santarem, Emile Barrias, Ina Pöhner, Sara Luelmo, Pantelis Afroudakis, Kalliopi Georgikopoulou, Paloma Tejera Nevado, Julia Eick, Eugenia Bifeld, María J. Corral, María Dolores Jiménez-Antón, Bernhard Ellinger, Maria Kuzikov, Irini Fragiadaki, Effie Scoulica, Sheraz Gul, Joachim Clos, Kyriakos C. Prousis, Juan J. Torrado, José María Alunda, Rebecca C. Wade, Wanderley de Souza, Anabela Cordeiro da Silva, Theodora Calogeropoulou

Date Published: 1st Sep 2023

Publication Type: Journal Article

Current Treatments to Control African Trypanosomiasis and One Health Perspective

Abstract (Expand)

Human African Trypanosomiasis (HAT, sleeping sickness) and Animal African Trypanosomiasis (AAT) are neglected tropical diseases generally caused by the same etiological agent, Trypanosoma brucei. Despite … important advances in the reduction or disappearance of HAT cases, AAT represents a risky reservoir of the infections. There is a strong need to control AAT, as is claimed by the European Commission in a recent document on the reservation of antimicrobials for human use. Control of AAT is considered part of the One Health approach established by the FAO program against African Trypanosomiasis. Under the umbrella of the One Health concepts, in this work, by analyzing the pharmacological properties of the therapeutic options against Trypanosoma brucei spp., we underline the need for clearer and more defined guidelines in the employment of drugs designed for HAT and AAT. Essential requirements are addressed to meet the challenge of drug use and drug resistance development. This approach shall avoid inter-species cross-resistance phenomena and retain drugs therapeutic activity.

Authors: Alberto Venturelli, Lorenzo Tagliazucchi, Clara Lima, Federica Venuti, Giulia Malpezzi, George E. Magoulas, Nuno Santarem, Theodora Calogeropoulou, Anabela Cordeiro-da-Silva, Maria Paola Costi

Date Published: 27th Jun 2022

Publication Type: Journal Article

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