New derivatives of 4-N-benzylamino-4-hetarylbut-1-ene containing a pyridyl nucleus were synthesized from benzylamines and pyridine aldehydes. N-oxide derivatives were obtained from these homoallylamines. Study of the antiparasitic properties of obtained pyridine derivatives as well as of four related benzazepines previously described, was carried out using cytotoxicity assays against Trichomonas vaginalis and epimastigote form of Trypanosoma cruzi protozoa. Compounds showing activity against epimastigote T. cruzi were tested against the amastigote form; unspecific cytotoxicity against macrophages was also studied.
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http://dx.doi.org/10.1002/ardp.200400909 | DOI Listing |
Int J Nanomedicine
December 2024
Department of Zoology, College of Science, King Saud University, Riyadh, 11451, Kingdom of Saudi Arabia.
Introduction: Malaria caused by spp. is the most hazardous disease in the world. It is regarded as a life-threatening hematological disorder caused by parasites transferred to humans by the bite of Anopheles mosquitoes.
View Article and Find Full Text PDFBiomed Pharmacother
December 2024
Structural Biology Laboratory, Oswaldo Cruz Institution, Fiocruz, Rio de Janeiro, Brazil; Programa de Pós-graduação em Biologia Celular e Molecular, Oswaldo Cruz Institution, Fiocruz, Rio de Janeiro, Brazil. Electronic address:
Trichomoniasis, a globally prevalent sexually transmitted infection caused by Trichomonas vaginalis, affects approximately 278 million people each year. It presents a challenge due to resistance to the current treatment, Metronidazole (MTZ), which is also associated with side effects. Cannabis sativa, with more than 100 phytocannabinoids and numerous studies for therapeutic applications, including parasitic infections, has undergone a significant shift in acceptance worldwide, highlighted by legalizations and substantial revenue projections.
View Article and Find Full Text PDFChem Biodivers
December 2024
Universidad Nacional de Colombia, Antioquia, carrera 65 59a-110, 3840, Medellín, COLOMBIA.
Coumarin-chalcone hybrids are promising compounds that could be used as lead structures in the fight against parasitic diseases. In this work, sixteen hybrids of coumarin-chalcone (3-cinnamoyl-2H-chromen-2-ones) were synthesized, and their in vitro biological activity was evaluated against intracellular amastigotes of Leishmania braziliensis and Trypanosoma cruzi; as well as their cytotoxicity in the U-937 cell line. Compounds (E)-3-(3-(3-ethoxy-4-hydroxyphenyl)acryloyl)-7-methoxy-2H-chromen-2-one (H25) and (E)-7-(diethylamino)-3-(4-(methoxyphenyl)acryloyl)-2H-chromen-2-one (H12) showed the highest antileishmanial activity with EC50 values of 18.
View Article and Find Full Text PDFBMC Complement Med Ther
December 2024
Center of Natural Product Medicine Research and Development, Institute of Tropical Disease, Universitas Airlangga, Surabaya, Indonesia.
Background: Neglected tropical diseases (NTDs) afflict nearly 2 billion people worldwide and are caused by various pathogens, such as bacteria, protozoa, and trypanosoma, prevalent in tropical and subtropical regions. Among the 17 NTDs recognized by the World Health Organization (WHO), protozoal infections caused by Plasmodium, Entamoeba, Leishmania, and Trypanosoma are particularly prominent and pose significant public health. Indonesia, endowed with a rich biodiversity owing to its tropical climate, harbors numerous plant species with potent biological activities that hold promise for therapeutic interventions.
View Article and Find Full Text PDFMolecules
December 2024
Medicinal Chemistry Laboratory, Department of Biosciences, Jamia Millia Islamia, New Delhi 110025, India.
In response to the escalating crisis of antimicrobial resistance (AMR), there is an urgent need to research and develop novel antibiotics. This study presents the synthesis and assessment of innovative 4-aminoquinoline-benzohydrazide-based molecular hybrids bearing aryl aldehydes () and substituted isatin warheads (), characterized using multispectroscopic techniques with high purity confirmed by HRMS. The compounds were evaluated against a panel of clinically relevant antibacterial strains including the Gram-positive , , and and a Gram-negative bacterial strain.
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