Atividade antifúngica de imidas cíclicas contra Cryptococcus / Antifungal activity of cyclic imides Cryptococcus neoformans

A criptococose é uma infecção fúngica causada pela levedura Cryptococcus neoformans que acomete tanto hospedeiros normais quanto imunocomprometidos. Nos últimos anos, o número de cepas resistentes a váriso antifúngicos de uso clínico tem apresentado um vertiginoso crescimento. Neste contexto, é de fundamental importância a pesquisa de novas alternativas terapêuticas, através do estudo com produtos naturais, substâncias isoladas e sintéticas, como as imidas cíclicas. O presente trabalho teve como objetivo investigar a atividade antifúngica das imidas cíclicas frente a cepas de Cruptococcus neofornans. A triagem antifúngica foi realizada utilizando a técnica de difusão em meio sólido. Para a determinação da concentração inibitória mínima, foi empregada a técnica da microdiluição. Foram testadas naftalimidas, succimidas e maleimidas. Dentre estas substâncias, as maleimidas ... De acordo com os resultados , as maleimidas surgem como candidatas a antifúngicos por atuarem contra uma espécie de microorganismo que comumente causa infecções.

Preparation of a zinc porphyrinated nanofibrous membrane and its ammonia sensing property / 浙江大学学报·医学版

<p><b>OBJECTIVE</b>To prepare a zinc porphyrinated polyimide nanofibrous membrane for rapid detection of trace amount of ammonia.</p><p><b>METHODS</b>Zinc porphyrin chromophore was copolymerized into polyimide backbones and the according nanofibrous membrane was prepared by electrospinning technique. Ammonia detection was achieved by recording the color and spectral changes of the membrane before and after exposing to the target gas. The sensitivity, selectivity and detection limit of prepared membrane were further studied.</p><p><b>RESULTS</b>The obtained nanofibrous membrane preserved typical photophysical properties of zinc porphyrin chromophores. When exposed to ammonia, a dual chromo and spectrum responses of the nanofibrous membrane were observed. The binding affinity constant and the detection limit of zinc porphyrinated polyimide nanofibrous membrane calculated from surface plasmon resonance (SPR) analysis and UV-vis were 3.33 X10³ L/mol and 3.13 mg/m³, respectively.</p><p><b>CONCLUSION</b>The membrane prepared in this study exhibits good sensitivity, selectivity and reproducibility towards ammonia detection.</p>

Profile of susceptibility in vitro of Trichosporon asahii and Trichosporon inkin strains against cyclic imides

In vitro susceptibility testing of Trichosporon asahii (13 strains) and T. inkin (13 strains) against cyclic imides (succinimides, naphtalimides and maleimides) in concentrations of 200 to 6,25 μg/mL was performed according to the diffusion agar method. By the results obtained, the antifungal activity of the cyclic imides: 3,4-dichloro-N-phenyl-maleimide; 3,4-dichloro-N-phenyl-ethyl-maleimide and 3,4-dichloro-N-phenyl-propyl-maleimide (50 μg/mL) over T. asahii and T. inkin was important and it may be helpful in showing perspectives in a search for new antimicotic products.

O perfil de sensibilidade in vitro de Trichosporon asahii (13 cepas) e T. inkin (13 cepas) frente a imidas cíclicas (naftalimidas, succinimidas e maleimidas) nas concentrações de 6,25 a 200 μg/mL foi realizado pelo método de difusão em agar. Pelos resultados obtidos, a atividade antifúngica das imidas cíclicas: 3,4-dicloro-N-fenil-maleimida; 3,4-dicloro-N-fenil-etil-maleimida e 3,4-dicloro-N-fenil-propil-maleimida (50 μg/mL) sobre T. asahii e T. inkin foi importante e pode abrir perspectivas na busca de novos produtos antimicóticos.

Avaliação da sensibilidade de cepas de Malassezia furfur a imidas cíclicas / Sensibility of evaluation of Malassezia furfur strains at cyclic imides

Malassezia furfur (Pityrosporum orbiculare) é um fungo lipofílico, que está associado a pitiríase versicolor, foliculite, dermatite seborréica e atópica, fungemia e infecções sistêmicas. O tratamento é feito com soluções antimicóticas ou derivados imidazólicos, particularmente, o cetoconazol. Dentro das perspectivas de avaliação de novas alternativas para a terapêutica das infecções micóticas, determinou-se, nesse estudo, a atividade antifúngica de compostos imídicos. As imidas 3,4-dicloro-N-fenil-maleimida (6,3 µg/ml), 3,4-dicloro-N-benzil-maleimida (25 µg/ml) e 3,4-dicloro-N-fenil-propil-maleimida (20 µg/ml) foram os compostos que apresentaram melhor atividade inibitória contra as cepas de M. furfur...

Synthesis of dibenz [c,e] azepine-5,7-dione derivatives

Aminolysis of diphemic anhydride afforded the diphenamic acid derivatives [1a-f], which on cyclization of [1a-d] by acetic anhydride yielded the 6-substituted dibenz [c,e] azepine-5,7-diones [2a-d]. Potassium diphenimide was prepared and reacted with certain halogen compounds to produce [2d-m]. Hydrazinolysis of diphenimide produced exclusively the diphenamic acid hydrazide [4a], the acyl [4b-c] and arylidene [5a-e] derivatives of which were prepared. Structure of the final products was proved by microanalysis, spectral data and when necessary by unambiguous synthesis. Some of the newly synthesised compounds were screened for anticonvulsant and hypnotic activity

Morphine-like activity of substituted amides & imides of [D-Ala2, Met5]-enkephalin.

Six enkephalin analogues (N-substituted amides and imides of [D-Ala2, Met5]-enkephalin) were synthesized and tested for opioid activity. All the compounds, except one i.e., compound IV, showed analgesic activity which was much higher than Met-enkephalin and morphine in mice and inhibited electrically induced contractions of isolated guineapig ileum, [D-Ala2, Met5]-enkephalin-morpholide and [D-Ala2, Met5]-enkephalin-beta-Ala-amide were the most potent analgesics and nearly 6 and 500 times as active as morphine and Met-enkephalin respectively. Both the compounds were equipotent on the guineapig ileum preparation, whereas the beta-Ala-amide was about twice as active as the morpholide in the electrically stimulated mouse vas deferens preparation.

study on the effect of the sulphone group on imides

While n-substituted phthalimides can't undergo Perkin condensation, N-[P-tolylsulphonyl] phthalimide [Ib] react with P-nitrophenylacetic acid to give the benzal derivative [II] and with other active methylene compounds to give the anilide derivatives [IV]. With Grignard reagents [Ib] follow in some cases the normal lines as N-substituted phthalimides to give [X] and [XI]. While in other cases [Ib] gave abnormal products as [XII] and [XIII], With P,S[5] [one mole] [Ib] gives the expected monothione [Ic] which with amines gives N-substituted phthalimides [XIV]

A preliminary report on the antiarrhythmic action of some newly synthesized glutarimide compounds.

The effects of a new series of glutarimide compounds have been studied in acetylcholine induced auricular fibrillation in anaesthetized cats and epinephrine induced ventricular arrhythmmias in conscious pigeons. Some of the compounds showed varying degree of protective action against experimental arrhythmias. However these compounds were found to be less potent than quinidine. The mechanism of antiarrhythmic action has been discussed.