Synthesis and characterization of new heterocyclic compounds with potential antituberculosis activity and their immobilization on polymer supports

cited By 4International audienceNew biologically active compounds, obtained by synthesizing new hydrazides derived from benzoxazolyl-2mercaptoformic acid, respectively benzoxazolyl-2-mercaptoacetic acid, have been chemically immobilized onto poly(maleic anhydride-alt-vinyl acetate) supports, forming drug-polymer conjugates with controlled delivery. The reaction products were characterized by elemental and spectral analyses (FT-IR, 1H-NMR). Toxicological and tuberculostatic activity tests recommend certain reaction products as therapeutic candidates with pharmacological application

Polymer conjugates with potential biological activity based on new derivatives of 2-mercaptobenzoxazole-synthesis and characterization

cited By 1International audienceNew potentially biologically active compounds derived from 2-mercapto-benzoxazole were synthesized and coupled on polymeric support of poly (maleic anhydride-alt-vinyl acetate) for the preparation of polymer-drug conjugates with controlled drug release. All compounds were characterized by elemental and spectroscopy (FT-IR, 1H-NMR) analysis. The toxicological tests recommend the products for further laboratory screening. [Figure not available: see fulltext.] © 2013 Versita Warsaw and Springer-Verlag Wien

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

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

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