Neglected parasitic diseases are a group of infections currently considered as a worldwide concern. This fact can be attributed to the migration of these diseases to developed and developing countries, associated with therapeutic insufficiency resulted from the low investment in the research and development of new drugs. In order to overcome this situation, bioprospecting supports medicinal chemistry in the identification of new scaffolds with therapeutically appropriate physicochemical and pharmacokinetic properties. Among them, we highlight the nitrogenous heterocyclic compounds, as they are secondary metabolites of many natural products with potential biological activity. The objective of this work was to review studies within a 10-year timeframe (2009- 2019), focusing on the pharmacological application of nitrogen bioprospectives (pyrrole, pyridine, indole, quinoline, acridine, and their respective derivatives) against neglected parasitic infections (malaria, leishmania, trypanosomiases, and schistosomiasis), and their application as a template for semi-synthesis or total synthesis of potential antiparasitic agents. In our studies, it was observed that among the selected articles, there was a higher focus on the attempt to identify and obtain novel antimalarial compounds, in a way that an extensive amount of studies involving all heterocyclic nitrogen nuclei were found. On the other hand, the parasites with the lowest number of publications up until the present date have been trypanosomiasis, especially those caused by Trypanosoma cruzi, and schistosomiasis, where some heterocyclics have not even been cited in recent years. Thus, we conclude that despite the great biodiversity on the planet, little attention has been given to certain neglected tropical diseases, especially those that reach countries with a high poverty rate.
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http://dx.doi.org/10.2174/1381612826666200701160904 | DOI Listing |
ChemistryOpen
December 2024
MTA TTK Lendület Artificial Transporter Research Group, Institute of Materials and Environmental Chemistry, HUN-REN Research Center for Natural Sciences, H-1117, Budapest, Magyar tudósok krt. 2, Hungary.
Novel tetrahydroisoquinoline and piperidine derivatives were selectively synthesized from substituted indenes or cyclopentenes. The process starts with an oxidative cleavage of the ring olefin bond, which gives reactive diformyl intermediates. By a ring-closing step using chiral (R) or (S) α-methylbenzylamine under a reductive amination protocol facilitated ring formation with ring expansion of the corresponding nitrogen-containing heterocycles.
View Article and Find Full Text PDFJ Agric Food Chem
December 2024
State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guizhou University, Huaxi District, Guiyang 550025, China.
Thiazole and isothiazole are types of five-membered heterocycles that contain both sulfur and nitrogen atoms. They have gained attention in the field of green pesticide research due to their low toxicity, strong biological activity, and ability to undergo diverse structural modifications. By incorporating thiazole and isothiazole groups into various compounds, researchers have been able to create a wide range of pesticides with broad-spectrum effectiveness.
View Article and Find Full Text PDFMol Divers
December 2024
State Key Laboratory of Green Pesticides, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for R&D of Fine Chemicals of Guizhou University, Guiyang, 550025, China.
Pyridazine and pyridazinone belong to the same group of six-membered heterocyclic compounds, and both structurally feature two adjacent nitrogen atoms. Pyridazine and pyridazinone derivatives are frequently used as core structures in the development of new green agrochemicals due to their high activity and environmental friendliness, attracting significant attention from researchers in recent years. Over the past 20 years, significant developments have occurred in the field of pyridazine and pyridazinone derivatives, which exhibit insecticidal, fungicidal, herbicidal, antiviral, and plant growth regulating activities.
View Article and Find Full Text PDFJ Biomol Struct Dyn
December 2024
Laboratory of Drug Design and Discovery, Department of Pharmaceutical Technology, Jadavpur University, Kolkata, India.
Selective inhibition of histone deacetylase 8 (HDAC8) has emerged as a promising approach for treating various diseases, including cancer. However, finding key structural features for HDAC8 inhibition and developing effective and selective HDAC8 inhibitors (HDAC8s) pose significant challenges. In the past few years, the development of various scaffolds for inhibiting HDAC8 has significantly risen and the quest continues.
View Article and Find Full Text PDFActa Crystallogr E Crystallogr Commun
October 2024
Department of Chemistry, KU Leuven, Biomolecular Architecture, Celestijnenlaan 200F, Leuven (Heverlee), B-3001, Belgium.
Two new zinc(II) complexes, tri-ethyl-ammonium di-chlorido-[2-(4-nitro-phen-yl)-4-phenyl-quinolin-8-olato]zinc(II), (CHN){Zn(CHNO)Cl] (), and bis-(tri-ethyl-ammonium) {2,2'-[1,4-phenyl-enebis(nitrilo-methyl-idyne)]diphenolato}bis-[di-chlorido-zinc(II)], (CHN)[Zn(CHNO)Cl] (), were synthesized and their structures were determined using ESI-MS spectrometry, H NMR spectroscopy, and single-crystal X-ray diffraction. The results showed that the ligands 2-(4-nitro-phen-yl)-4-phenyl-quinolin-8-ol () and ,'-bis-(2-hy-droxy-benzyl-idene)benzene-1,4-di-amine () were deprotonated by tri-ethyl-amine, forming the counter-ion EtNH, which inter-acts an N-H⋯O hydrogen bond with the ligand. The Zn atoms have a distorted trigonal-pyramidal () and distorted tetra-hedral () geometries with a coord-ination number of four, coordinating with the ligands N and O atoms.
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