Review
Pharmacology & Pharmacy
Jasmita Gill, Amit Sharma
Summary: Halofuginone, derived from a Chinese herb, has shown beneficial effects in treating various diseases such as parasitic diseases, cancer, fibrosis, and autoimmune disorders. Its mechanism of action involves inhibiting the prolyl-tRNA synthetase enzyme for its antiparasitic role.
DRUG DISCOVERY TODAY
(2022)
Review
Microbiology
Francisco Guerra, Elizabeth Winzeler
Summary: Phenotypic screening methods have been instrumental in identifying potential antimalarial drug candidates, but recent efforts are focused on target-based drug discovery.
CURRENT OPINION IN MICROBIOLOGY
(2022)
Article
Chemistry, Medicinal
Nicolas Chopin, Julien Bosson, Shinya Iikawa, Stephane Picot, Anne-Lise Bienvenu, Adeline Lavoignat, Guillaume Bonnot, Mickael Riou, Corinne Beauge, Vanaique Guillory, Christophe Biot, Guillaume Pilet, Matthieu Chesse, Elisabeth Davioud-Charvet, Mourad Elhabiri, Jean-Philippe Bouillon, Maurice Medebielle
Summary: A series of ferrocenyl-containing gamma-hydroxy-gamma-lactam tetramates were prepared through a ring opening-ring closure process in the presence of ferrocenyl alkylamines. These compounds exhibited good antiplasmodial activity and selective antiparasitic activity.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Review
Chemistry, Multidisciplinary
Atukuri Dorababu
Summary: Protozoal infections such as malaria and leishmania are increasingly prevalent, leading to a high death rate worldwide. The development of efficient anti-protozoal drugs with low toxicity remains a challenge, with research focusing on utilizing heterocyclic pharmacophores like quinoline bicycle for drug design. Efforts are ongoing to bring potent anti-protozoal agents to the clinical stage, considering the importance of structural features and safety index for clinical efficacy.
Article
Chemistry, Multidisciplinary
He-Ye Zhou, Chuan-Feng Chen
Summary: The exploration of macrocycle-based nonporous adaptive crystals has been a hot topic in the fields of supramolecular chemistry and crystal engineering. In this study, calix[3]acridan-based NACs were developed to separate industrially important 4-picoline from its isomer mixtures with a purity of over 93.8%.
CHEMICAL COMMUNICATIONS
(2022)
Article
Chemistry, Multidisciplinary
Anil Kumar, Manju Kandpal
Summary: New antibacterial ligand H(3)hmbpa-5 and its aluminium complexes Al(OPri)(Hhmbpa-5), Al(H(2)hmbpa-5)(Hhmbpa-5), and Al(H(2)hmbpa-5)(3) were synthesized and characterized. The ligand and complexes showed excellent antibacterial activity against Pseudomonas aeruginosa, Streptococcus aureus, Klebsiella pneumoniae, and Klebsiella pneumoniae.
JOURNAL OF CHEMISTRY
(2023)
Article
Chemistry, Applied
Sidika Cetinkaya, Sedat Yurdakal
Summary: Home prepared TiO2 photocatalysts were synthesized under different conditions and characterized. The results showed that the high selectivity of the home prepared samples was mainly attributed to the hydrophilicity of the TiO2 surface, which allowed desorption of valuable products instead of over-oxidation.
Article
Chemistry, Organic
Maurycy Prystupa, Tilo Sohnel, Jonathan Sperry
Summary: 3-Hydroxy-2,2'-bisindole undergoes dimerization-skeletal rearrangement processes under acid- and base-mediated conditions, forming polyheterocyclic ring systems with up to nine rings. The mechanistic rationale for these reactions suggests similarities with the reactivity of 3',3''-dihydroxytetraindole under similar conditions, providing insight into these chemical transformations.
JOURNAL OF ORGANIC CHEMISTRY
(2021)
Article
Multidisciplinary Sciences
Cristina C. Clement, Angelo D'Alessandro, Sangeetha Thangaswamy, Samantha Chalmers, Raquel Furtado, Sheila Spada, Giada Mondanelli, Federica Ianni, Sarah Gehrke, Marco Gargaro, Giorgia Manni, Luisa Carlota Lopez Cara, Peter Runge, Wanxia Li Tsai, Sinem Karaman, Jorge Arasa, Ruben Fernandez-Rodriguez, Amanda Beck, Antonio Macchiarulo, Massimo Gadina, Cornelia Halin, Francesca Fallarino, Mihaela Skobe, Marc Veldhoen, Simone Moretti, Silvia Formenti, Sandra Demaria, Rajesh K. Soni, Roberta Galarini, Roccaldo Sardella, Gregoire Lauvau, Chaim Putterman, Kari Alitalo, Ursula Grohmann, Laura Santambrogio
Summary: 3-hydroxy-L-kynurenamine (3-HKA) is a metabolite deriving from a lateral pathway of tryptophan catabolism. The authors identify 3-HKA as a biogenic amine with anti-inflammatory properties, showing its protective effects against psoriasis and nephrotoxic nephritis in mice.
NATURE COMMUNICATIONS
(2021)
Article
Parasitology
Pongpisid Koonyosying, Somdet Srichairatanakool, Saruda Tiwananthagorn, Nattawooti Sthitmatee
Summary: Babesiosis is a parasitic infectious disease caused by Babesia, which can be transmitted via tick bites. Currently, there are limited drugs available for the treatment of this disease, and drug resistance is increasing. This study evaluated the inhibitory efficacy of an iron chelator and antimalarial drugs against Babesia bovis infection in vitro.
VETERINARY PARASITOLOGY
(2023)
Article
Chemistry, Applied
Mathias Pickl, Markus Ebner, Samantha Gittings, Pere Clapes, Wolfgang Kroutil
Summary: Although optical pure amino alcohols are highly demanded, their synthesis remains challenging due to the requirement of elaborate protection strategies. This study presents a multi-enzymatic methodology that allows the synthesis of enantioenriched 1,3-amino alcohols from commodity chemicals. By utilizing a Type I aldolase and enzymatic transamination, both diastereomers of the 1,3-amino alcohol motif were accessible, resulting in the desired amino alcohols with high enantioselectivity.
ADVANCED SYNTHESIS & CATALYSIS
(2023)
Article
Agriculture, Multidisciplinary
Ruichen Gao, Zhimin Li
Summary: This study utilized a biocatalytic approach to achieve efficient production of HMB by rational design and optimization of reaction conditions, overcoming the limitations of traditional chemical synthesis and fermentation methods.
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
(2021)
Review
Biochemistry & Molecular Biology
Roberta Ettari, Santo Previti, Carla Di Chio, Maria Zappala
Summary: Malaria is a serious global public health issue, with chemotherapy being the only current treatment method due to lack of effective vaccine. However, the resistance to antimalarial drugs poses a challenge to the current therapeutic regimen. Therefore, the search for new drug targets is a pressing priority.
CURRENT MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Dickson Mambwe, Constance M. Korkor, Amanda Mabhula, Zama Ngqumba, Cleavon Cloete, Malkeet Kumar, Paula Ladeia Barros, Meta Leshabane, Dina Coertzen, Dale Taylor, Liezl Gibhard, Mathew Njoroge, Nina Lawrence, Janette Reader, Diogo Rodrigo Moreira, Lyn-Marie Birkholtz, Sergio Wittlin, Timothy J. Egan, Kelly Chibale
Summary: Iterative medicinal chemistry optimization led to the discovery of a highly potent compound 23 with metabolic stability and selectivity, displaying activity against multiple stages of malaria and showing in vivo efficacy in mice.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Physical
Hisakazu Miyamoto, Hiroki Takahashi
Summary: The title compounds, 3-(p-phenylphenyl)-3-hydroxy-N-isopropyl-4,4-dimethylazetidin-2-one (2d) and 3-phenyl-3-hydroxy-N-isopropyl-4,4-dimethylazetidin-2-one (2a), were synthesized by photoreaction of N,N-diisopropyl(p-phenylphenyl)glyoxylamide 1d and N,N-diisopropylphenylglyoxylamide 1a, respectively, in solution. The formation of the compounds was confirmed by various spectroscopic techniques and X-ray diffraction. The crystal structures of compounds 2d and 2a belong to the orthorhombic and monoclinic systems, with space groups Pna2(1) and P2(1)/c, respectively.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
