Future prospects in the treatment of parasitic diseases: 2-amino-1, 3, 4-thiadiazoles in leishmaniasis

G Serban - Molecules, 2019 - mdpi.com
Neglected tropical diseases affect the lives of a billion people worldwide. Among them, the
parasitic infections caused by protozoan parasites of the Trypanosomatidae family have a …

Synthesis of oxadiazole-thiadiazole fluorochromane hybrids and their antioxidant activity

M Rupapara, M Chauhan, CB Sangani, M Afzal… - Journal of Fluorine …, 2023 - Elsevier
In this study, we set out to create some new oxadiazole-thiadiazole fluorochromane hybrid
compounds 7a–7j and test them for their antioxidant properties. β-blockers drug-based 6 …

Further insight into the dual COX-2 and 15-LOX anti-inflammatory activity of 1, 3, 4-thiadiazole-thiazolidinone hybrids: The contribution of the substituents at 5th …

YM Omar, SG Abdel-Moty, HHM Abdu-Allah - Bioorganic Chemistry, 2020 - Elsevier
Herin we report the design, synthesis, full characterization and biological investigation of
new 15-LOX/COX dual inhibitors based on 1, 3-thiazolidin-4-one (15-lipoxygenase …

High-Throughput Phenotypic Screening and Machine Learning Methods Enabled the Selection of Broad-Spectrum Low-Toxicity Antitrypanosomatidic Agents

P Linciano, A Quotadamo, R Luciani… - Journal of Medicinal …, 2023 - ACS Publications
Broad-spectrum anti-infective chemotherapy agents with activity against Trypanosomes,
Leishmania, and Mycobacterium tuberculosis species were identified from a high …

Design, synthesis and antitrypanosomal activity of heteroaryl-based 1, 2, 4-triazole and 1, 3, 4-oxadiazole derivatives

MS Shaykoon, AA Marzouk, OM Soltan, AS Wanas… - Bioorganic …, 2020 - Elsevier
Abstract Two series of novel 1, 2, 4-triazol-3-yl-thioacetamide 3a-b and 4a-b and 5-pyrazin-2-
yl-3H-[1, 3, 4] oxadiazole-2-thiones 9a-h were designed and synthesized. The compounds …

Anti-trypanosomatid structure-based drug design–lessons learned from targeting the folate pathway

J Panecka-Hofman, I Poehner… - Expert Opinion on Drug …, 2022 - Taylor & Francis
Introduction Trypanosomatidic parasitic infections in humans and animals caused by
Trypanosoma brucei, Trypanosoma cruzi, and Leishmania species pose a significant health …

Aryl thiosemicarbazones for the treatment of trypanosomatidic infections

P Linciano, CB Moraes, LM Alcantara… - European Journal of …, 2018 - Elsevier
Basing on a library of thiadiazole derivatives showing anti-trypanosomatidic activity, we
have considered the thiadiazoles opened forms and reaction intermediates …

Enhancement of benzothiazoles as pteridine reductase-1 inhibitors for the treatment of trypanosomatidic infections

P Linciano, C Pozzi, LD Iacono, F di Pisa… - Journal of Medicinal …, 2019 - ACS Publications
2-Amino-benzo [d] thiazole was identified as a new scaffold for the development of improved
pteridine reductase-1 (PTR1) inhibitors and anti-trypanosomatidic agents. Molecular …

Microwave-assisted organic acid–base-co-catalyzed tandem Meinwald rearrangement and annulation of styrylepoxides

Y Shi, S Li, Y Lu, Z Zhao, P Li, J Xu - Chemical Communications, 2020 - pubs.rsc.org
A novel organic acid–base-co-catalyzed conversion of styrylepoxides into [1, 1′-biaryl]-3-
carbaldehydes was realized under microwave irradiation. Styrylepoxides first underwent an …

Multitarget, selective compound design yields potent inhibitors of a kinetoplastid pteridine reductase 1

I Pohner, A Quotadamo… - Journal of Medicinal …, 2022 - ACS Publications
The optimization of compounds with multiple targets is a difficult multidimensional problem
in the drug discovery cycle. Here, we present a systematic, multidisciplinary approach to the …