Phytochemical investigation of Beilschmiedia alloiophylla has resulted in the isolation of one new alkaloid, 2-hydroxy-9-methoxyaporphine (1), and ten known natural products, laurotetanine (2), liriodenine (3), boldine (4), secoboldine (5), isoboldine (6), asimilobine (7), oreobeiline (8), 6-epioreobeiline (9), β-amyrone (10), and (S)-3-methoxynordomesticine (11). Chemical studies on the bark of B. kunstleri afforded compounds 2 and 4 along with one bisbenzylisoquinoline alkaloid, N-dimethylphyllocryptine (12). Structures of compounds 1-12 were elucidated on the basis of spectroscopic methods. All of these isolates were evaluated for their anti-acetylcholinesterase (AChE), anti-α-glucosidase, anti-leishmanial and anti-fungal activities. Compounds 1-12 exhibited strong to moderate bioactivities in aforementioned bioassays.
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http://dx.doi.org/10.1016/j.fitote.2011.11.009 | DOI Listing |
Sci Rep
January 2025
Department of Medicinal Chemistry, Faculty of Pharmacy, Kerman University of Medical Sciences, Kerman, Iran.
Leishmaniasis is a parasitic disease caused by protozoan organisms belonging to the Leishmania genus, affecting many individuals worldwide, with the burden surpassing one million cases. This disease leads to considerable morbidity and mortality, predominantly within tropical and subtropical regions. The current therapeutic options for leishmaniasis are far from ideal, as they fail to achieve a level of efficacy that can be deemed universally effective.
View Article and Find Full Text PDFMini Rev Med Chem
January 2025
Department of Chemistry, Faculty of Science, Universiti Teknologi Malaysia, Johor Bahru 81310, Johor, Malaysia.
Indole, a ubiquitous structural motif in bioactive compounds, has played a pivotal role in drug discovery. Among indole derivatives, indole-3-carboxaldehyde (I3A) has emerged as a particularly promising scaffold for the development of therapeutic agents. This review delves into the recent advancements in the chemical modification of I3A and its derivatives, highlighting their potential applications in various therapeutic areas.
View Article and Find Full Text PDFPharmaceuticals (Basel)
November 2024
Laboratório de Bioquímica de Tripanosomatídeos, Instituto Oswaldo Cruz, Fundação Oswaldo Cruz, Rio de Janeiro 21040-900, Brazil.
Leishmaniasis, caused by protozoa and transmitted by vectors, presents varied clinical manifestations based on parasite species and host immunity. The lack of effective vaccines or treatments has prompted research into new therapies, including thiourea derivatives, which have demonstrated antiprotozoal activities. We synthesized two series of ,'-disubstituted thiourea derivatives through the reaction of isothiocyanates with amines.
View Article and Find Full Text PDFInt J Parasitol Drugs Drug Resist
December 2024
São Paulo State University (Unesp), School of Pharmaceutical Sciences, Araraquara, São Paulo, Brazil. Electronic address:
Leishmaniasis is a neglected disease that remains with a limited number of drugs available for chemotherapy and has an increased drug resistance that affects treatment outcomes. Metal-based drugs such as cyclopalladated complex [Pd(dmba)(μ-N)] (CP2), a Leishmania topoisomerase IB inhibitor involved in calcium dysregulation and mitochondrial dysfunction of the parasite, had been an alternative to outline the appearance of chemoresistance. To identify new molecular targets and point out possible resistance mechanisms, a CP2-resistant Leishmania amazonensis (LaR) was selected by stepwise exposure to increasing drug pressure until a line capable of growth in 13.
View Article and Find Full Text PDFSci Rep
December 2024
Department of Statistics, College of Natural and Computational Sciences, Gambella University, Gambella, Ethiopia.
Visceral leishmaniasis (VL) is a neglected tropical disease that mostly affects the working-class and impoverished segments of society, having a significant negative effect on the economic development of the affected nation. While anti-leishmanial medications lower mortality among VL patients, patients may still die or require more time to recover (TTR) while receiving treatment. In this regard, there are limited studies in Ethiopia.
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