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Mass Spectrometric Analysis
Published in Adorjan Aszalos, Modern Analysis of Antibiotics, 2020
The trimethylsilylated derivatives of cephalexin [226] and several penicillins [227] were examined by EI GC-MS. The potential for using these derivatives in a quantitative method was described. Using an internal standard, the correlation coefficient of cephalexin was 0.999, with a detection limit of 100 ng. The EI spectra of these derivatives are variable and highly dependent on the side chain at the 6-position. The molecular ions are generally weak. Several ions are related to the formation and subsequent fragmentation of a thiazolidine ring, and others are specific to the side chain. These latter ions were used for selected ion monitoring to determine the concentrations of individual components in a mixture. However, attempts to examine two cephalosporins, cephalothin and cephaloglycin, failed to produce gas chromatographic peaks with mass spectra consistent with their known structures. The methyl ester of PS-5 was prepared to obtain its high-resolution mass spectrum under EI conditions [228]. The elemental composition of several fragment ions were useful in determining the structure.
An Overview of Helminthiasis
Published in Venkatesan Jayaprakash, Daniele Castagnolo, Yusuf Özkay, Medicinal Chemistry of Neglected and Tropical Diseases, 2019
Leyla Yurttaș, Betül Kaya Çavușoğlu, Derya Osmaniye, Ulviye Acar Çevik
Levamisole (11) is a large-spectrum anthelmintic agent that is effective against ascardiasis and hookworm infections. It is a nicotinic receptor agonist and lead to spastic paralysis. The side effects of levamisole are mild and include nausea, headache, dizziness, skin rash and gastrointestinal disturbance. For the synthesis of levamisole, styrene oxide is initially reacted with ethanolamine followed by subsequent replacement of the hydroxyl groups using thionyl chloride to give 2-chloro-N-(2-chloroethyl)-2- phenylethan-1-amine. Acidic hydrolysis followed by reaction with thiourea led to a thiazolidine ring. The reaction of the latter molecule with thionyl chloride and alkaline treatment affords the racemic tetramizol, which is in turn separated into its dextro- and levo-isomers. Levamisole is the levo isomer of tetramizol (Akgün et al. 2013). The synthesis of Levamisole (11).
Microalgae and Cyanobacteria as a Potential Source of Anticancer Compounds
Published in Gokare A. Ravishankar, Ranga Rao Ambati, Handbook of Algal Technologies and Phytochemicals, 2019
A new hybrid thiazoline-containing alkaloid, laucysteinamide A, was isolated from Caldora penicillata collected from Lau Lau Bay Saipan, Northern Mariana Island (Zhang et al. 2017). This compound showed moderate cytotoxicity against H-460 human NSCLC cells (IC50=11 µM). In a separate study, three hapaindole-type alkaloids, namely hapalindole X, deschlorohapalindole 1 and 13-hydroxy dechlorofontonamide, were isolated from the extract of two cultured cyanobacteria, Westiellopsis sp. and Fischerellamuscicola (Kim et al. 2012a). Of the three compounds, hapalindole X displayed moderate cytotoxicity against HT-29 (colon), MCF-7 (breast), NCI-H460 (lung) and SF268 (CNS) cancer cells with IC50 values of 24.8, 35.4, 23.0 and 23.5 µM respectively. Recently, Acuna et al. (2018) tested another alkaloid compound isolated from Fischerella muscicola, hapalindole H, against PC-3 androgen-insensitive prostate cancer cells. The compound showed selective cytotoxicity against PC-3 prostate cancer cells (EC50=20 nM).
Are patents important indicators of innovation for Chagas disease treatment?
Published in Expert Opinion on Therapeutic Patents, 2023
Andrea Pestana Caroli, Felipe R. P. Mansoldo, Veronica S. Cardoso, Celso Luiz Salgueiro Lage, Flavia L. Carmo, Claudiu T Supuran, Alane Beatriz Vermelho
The patent EP2225196A1 [55] corresponds to nitrile-containing inhibitors derivatives with action against cysteine peptidases from Trypanosoma cruzi, African trypanosomiasis, and Leishmaniasis. Some patents were lapsed or discontinued concerning the peptidases target, such as the US20090247471A1 [56]. A recent systematic review of the literature [57] about the efficacy of thiazolidine and its imidazolidine derivatives against amastigotes of Trypanosoma cruzi was published. It was demonstrated that the compound 2-Iminothiazolidin-4-one 18 was effective with better results than benznidazole against amastigotes which are prevalent in the chronic phase of CD. This compound’s action mechanism is probably the inhibition of cruzipain (cysteine peptidase) and structural modification in the parasite not yet identified. In this context, the patent WO2012119212A1 [58] proposes using imidazolidine and thiazolidine compounds to treat Chagas disease.
Synthesis, kinetic studies and in-silico investigations of novel quinolinyl-iminothiazolines as alkaline phosphatase inhibitors
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2023
Muhammad Naeem Mustafa, Pervaiz Ali Channar, Muhammad Sarfraz, Aamer Saeed, Syeda Abida Ejaz, Mubashir Aziz, Fatmah Ali Alasmary, Hanadi Yaqob Alsoqair, Hussain Raza, Song Ja Kim, Asad Hamad
The second class of compounds i.e. thiazoline moiety also possesses various pharmacological and therapeutic applications in the drug industries. These derivatives exhibit anti-allergic22, antibiotic23, anticonvulsant II24,25, antifungal III26, antihypertensive27, anti-HIV IV28, anti-inflammatory28, antimalarial, antipyretic, antirheumatic, antitumor29, analgesic30 and cytotoxic activities31. 3-Methylthiazolidine is appreciated for the inhibition of indole ethylamine N-methyltransferase (INMT)32 and beneficial for treatment of schizophrenia33. Bayer CropScience developed commercially available iminothiazoline insecticide Thiacloprid34. Moreover, 2-imino-3-(benzoylmethyl)thiazolidine is used to protect from γ-radiation35. Likewise, hydroxy thiazole carboxylate II was stated for the inhibition of HIF-α prolyl hydroxylase while PS-028 is selective GPIIb/IIIa antagonist36,37. Significantly, 2-Imino-1,3-thiazoline scaffolds V impede production of melanin in dose-dependent style, thus acting as whitening agent of skin38. Pifithrin-α VI is recognised iminothiazoline reversible inhibitor of p53-dependant gene transcription and p53-mediated apoptosis39. Thiazolines exhibit interesting applications such as insecticides, acaricides, and plant growth regulators in agriculture40. It also found in the natural products like mirabazoles, tantazoles and thiangazole, which show anti-HIV and anticancer activities41.
Synthesis and in vitro antiproliferative and antibacterial activity of new thiazolidine-2,4-dione derivatives
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2018
Nazar Trotsko, Agata Przekora, Justyna Zalewska, Grażyna Ginalska, Agata Paneth, Monika Wujec
New 5-substituted pyrazoline thiazolidine-4-one was tested for anticancer activity according to the NCI protocol. The most active compounds were the derivatives of 2-(2,4-dioxo-1,3-thiazolidin-5-ylidene)acetic acid, namely 5-{2-[5-(2-hydroxyphenyl)-3-(4-methoxyphenyl)-4,5-dihydro-1H-pyrazol-1-yl]-2-oxoethylidene}-1,3-thiazolidine-2,4-dione and 5-{2-[5-(2-hydroxyphenyl)-3-(naphthalen-2-yl)-4,5-dihydro-1H-pyrazol-1-yl]-2-oxoethylidene}-1,3-thiazolidine-2,4-dione. These derivatives displayed the highest inhibitory activity against leukaemia cells (HL-60 (TB)) and CNS cancer (SF-295)5.