Synthesis of New Methionine Derivatives for the Treatment of Paracetamol - Induced Hepatic Injury

The direct pharmacological properties of amino acids and the possibility of using them as carriers for other active pharmacological substances are well known. Methionine, being able to yield the methyl group, is very important in the treatment of hepatic diseases. Paracetamol acute poisoning causes liver injury in both humans and animals. The study is designed to synthesize some new methionine derivatives and to establish a possible correlation between the new structure and the pharmacological properties. To this end, acute experimental poisoning with PanadolВ® (paracetamol) was performed while, for the treatment of liver injury caused by this compound, two original synthesis derivatives of methionine, namely N-(m-nitrobenzoyl)- L-methionine and N-(m-aminobenzoyl)-L-methionine, were used. Male Wistar rats were administered PanadolВ® (paracetamol) per oral (7500 mg/kg). N-(m-nitrobenzoyl)-L-methionine (m-NBM) 50 mg/kg and N-(m-aminobenzoyl)-L-methionine (m-ABM) 50 mg/kg were given intraperitoneally, 30 minutes after PanadolВ® administration. Biochemical parameters such as SGOT, SGPT, serum bilirubin and glycemia were estimated to assess the liver function. PanadolВ® (paracetamol) poisoning produced an increase in serum transaminases, bilirubin and glicemia. These effects were reduced by treatment with m-NBM and especially m-ABM. These biochemical observations were supplemented by histopathological examination of liver sections. The results obtained with m-ABM were comparable with those reported on methionine, which is a recognised antidote in paracetamol poisoning

Electrocardiogram Features in Non-Cardiac Diseases: From Mechanisms to Practical Aspects

Alexandr Ceasovschih,1,2,* Victorița Șorodoc,1,2 Serghei Covantsev,3,* Anastasia Balta,1,2,* Jamol Uzokov,4,* Sergio E Kaiser,5 Abdallah Almaghraby,6 Cătălina Lionte,1,2 Cristian Stătescu,1,7 Radu A Sascău,1,7 Viviana Onofrei,1,8 Raluca Ecaterina Haliga,1,2,* Alexandra Stoica,1,2,* Cristina Bologa,1,2 Ștefan Ailoaei,7 Yusuf Ziya Şener,9 Nicholas G Kounis,10 Laurențiu Șorodoc1,2 1Faculty of Medicine, “Grigore T. Popa” University of Medicine and Pharmacy, Iasi, Romania; 2 2nd Internal Medicine Department, “Sf. Spiridon” Clinical Emergency Hospital, Iasi, Romania; 3Department of Research and Clinical Development, Botkin Hospital, Moscow, Russia; 4Department of Cardiology, Republican Specialized Scientific Practical Medical Center of Therapy and Medical Rehabilitation, Tashkent, Uzbekistan; 5Discipline of Clinical and Experimental Pathophysiology, Rio de Janeiro State University, Rio de Janeiro, Brazil; 6Department of Cardiology, Ibrahim Bin Hamad Obaidallah Hospital, Ras Al Khaimah, United Arab Emirates; 7Department of Cardiology, “Prof. Dr. George I.M. Georgescu” Cardiovascular Diseases Institute, Iasi, Romania; 8Department of Cardiology, “Sf. Spiridon” Clinical Emergency Hospital, Iasi, Romania; 9Department of Internal Medicine, Hacettepe University Faculty of Medicine, Ankara, Turkiye; 10Department of Internal Medicine, Division of Cardiology, University of Patras Medical School, Patras, Greece*These authors contributed equally to this workCorrespondence: Victorița Șorodoc, 2nd Internal Medicine Department, “Sf. Spiridon” Clinical Emergency Hospital, Independentei 1 Street, Iasi, 700106, Romania, Tel +40232 240 822, Email [email protected] Viviana Onofrei, Cardiology Department, “Sf. Spiridon” Clinical Emergency Hospital, Independentei 1 Street, Iasi, 700106, Romania, Email [email protected]: Despite the noteworthy advancements and the introduction of new technologies in diagnostic tools for cardiovascular disorders, the electrocardiogram (ECG) remains a reliable, easily accessible, and affordable tool to use. In addition to its crucial role in cardiac emergencies, ECG can be considered a very useful ancillary tool for the diagnosis of many non-cardiac diseases as well. In this narrative review, we aimed to explore the potential contributions of ECG for the diagnosis of non-cardiac diseases such as stroke, migraine, pancreatitis, Kounis syndrome, hypothermia, esophageal disorders, pulmonary embolism, pulmonary diseases, electrolyte disturbances, anemia, coronavirus disease 2019, different intoxications and pregnancy.Keywords: electrocardiography, electrocardiogram, features, non-cardiac diseases, EC

Enhanced antipyretic activity of new 2, 5-substituted 1, 3, 4-oxadiazoles encapsulated in alginate/gelatin particulated systems

cited By 4International audienceNew 1,3,4-oxadiazoles with pharmacological potential, derived from 5-nitroindazole, have been synthesized. Their chemical structure has been established by elemental and spectral analyses (FT-IR and 1H-NMR). The oxadiazoles presented low toxicity, one compound, either in a free form or loaded in polymeric microcapsules, also showing a remarkable antipyretic activity, similar to that of acetylsalicylic acid

Synthesis and antimicrobial activity of new amidic derivatives of 5-nitroindazol-1-yl acetic acid encapsulated into alginate/pectin particles

International audienceNew amidic compounds with biologic activity, derived from 5-nitroindazol-1-yl-acetic acid have been synthesised and their chemical structure was confirmed by elemental and spectral analysis (FT-IR, 1H-NMR, 13C-NMR and mass spectrometry). The incorporation of some of the amides into sodium alginate and pectin based microcapsules, prepared by polymer ionotropic gelation in OAV emulsion determined the augmentation of their antibacterial potential against bacterial strains

Drug-Polymer Conjugates with Tuberculostatic Activity, Based on Poly (N-Vinyl Pyrrolidone-alt-Itaconic Anhydride) and Novel Aminoacid Hydrazides

cited By 4International audienceNovel drug-polymer conjugates were prepared by chemical immobilization of hydrazides on poly (N-vinyl pyrrolidone-alt-itaconic anhydride) support. Hydrazides with tuberculostatic activity were synthesized as derivatives of N-(p-nitrobenzoyl)-L-glutamine. Elemental and spectral analysis confirmed the chemical structure of the newly synthesized compounds and the evaluation of biological activity showed an increase of the tuberculostatic effect and a lower toxicity by chemically linking the hydrazides onto co-polymer. © 2013 Copyright Taylor and Francis Group, LLC

Novel acyl derivatives of n-(p-aminobenzoyl)-l-glutamine encapsulated in polymeric nanocapsules with potential antitumoral activity

cited By 7International audienceNew compounds with antitumoral activity have been obtained, by synthesizing aminoacid derivatives with formyl or acetyl groups grafted on N-(p-aminobenzoyl)-L-glutaminc. The suggested chemical structure of the new compounds was confirmed by elemental and spectral analysis (FT-IR and 1H-NMR). The synthesized acyl derivatives have been encapsulated into polymeric nanocapsules, based on chitosan and sodium alginate. Similarly to a reference cytostatic drug (methotrexate), biological tests showed that all compounds and all loaded nanocapsules presented low toxicity and good antitumoral activity against Erlich ascetic tumour in mice

Double crosslinked chitosan and gelatin submicronic capsules entrapping aminoacid derivatives with potential antitumoral activity

cited By 6International audienceThe aim of the article was the synthesis of novel L-phenylalanine derivatives with biological activity and their immobilization into polymeric particles. Thus, new formyl, acetyl and p-methoxy derivatives of L-phenylalanine with antitumor activity were synthesized by reaction with p-nitrobenzoyl chloride, followed by the reduction of nitro group and acylation of the new formed amino group. The chemical structures of the obtained aminoacid derivatives were determined by FT-IR, NMR, MS and elemental analyses. The compounds were encapsulated into chitosan- and gelatin-based submicronic capsules, prepared by double crosslinking (ionic and covalent) in a O/W/O double emulsion. The varying parameter polymer/ionic crosslinker molar ratio was seen to influence particle size, morphology, swelling degree, thermal properties, as well as their capacity to incorporate and release the new active principles. The in vivo acute toxicity and antitumoral effect of aminoacid derivatives in free form or encapsulated were evaluated on rats. Drug encapsulation into polymeric systems was proven to enhance antitumoral activity against implanted Guerin's carcinoma. © Springer Science+Business Media, LLC 2012

Polyelectrolyte complex based nanocapsules carrying novel 5-nitroindazole thiazolidines with potential use in treating oral infections

International audienceThe aim of this research was the synthesis of novel 2,3-disubstituted 1,3 thiazolidines, derived from 5- nitroindazole with antimicrobial activity and their encapsulation into polymer nanocapsules. Starting from previously synthesised hydrazones, there have been obtained novel thiazolidines by reaction with thioglycolic acid. The envisaged chemical structures were confirmed by spectral and elemental analysis. Two of the obtained thiazolidines were encapsulated into cationic Eudragit E100 nanocapsules, obtained by nanoprecipitation. In order to enhance drug release characteristics and particle stability, Eudragit E100 nanocapsules were covered with anionic polysaccharide (sodium alginate), thus forming a complex polyelectrolyte based membrane. The obtained nanocapsules presented a slower and more controlled drug release. The synthesized active principles, in free state and encapsulated into polymer nanocapsules, were tested for their acute toxicity and their influence on the development of model bacterial strains (Staphylococcus mutans, Actinobacillus actinomycetemcomitans, Bacillus subtilis, Bacillus cereus, Salmonella enteritidis, Escherichia coli and Staphylococcus aureus)

OPTIMIZATION REACTION FOR OBTAINING SOME N-[P-(R)-BENZOYL]-L- GLUTAMINE DERIVATIVES WITH PHARMACEUTICAL ACTION

The conditions in which the obtaining reactions of some N-[p-(R)-Benzoyl]-L-Glutamine derivatives are made with the highest yield were established in this paper. Due to their antitumoral effects, the action of glutamine derivatives on the digestive enzymes has been evaluated