Abstract
Objective
As a result of adverse effects including drug-resistance, toxicity and low bioavailability, there has been a crucial need for novel anticancer agents. In this present study, some ...novel 2,5-disubstituted 1,3,4-oxadiazole derivatives bearing pyridine moiety were synthesized and their potential cytotoxic activities were examined.
Materials and methods
A series of seven new compounds of 2-(5-(3-(pyrimidin-2-yl)thio)propyl)-1,3,4-oxadiazol-2-yl)thio)-1-(4-substituted)ethan-1-one derivatives were synthesized by reacting 5-(3-(pyrimidin-2-yl)thio)propyl-1,3,4-oxadiazole-2-thiol and 4-substituted phenacyl bromide derivatives in acetone with potassium carbonate. The structures of the obtained compounds were elucidated using FT-IR,
1
H-NMR and MS spectral data and elemental analyses. In vitro cytotoxic activity of the compounds was evaluated by MTT assay.
Results
Among the tested compounds, compound
4a
was found to be the most active cytotoxic agent against A549 cells, in compared with cisplatin as standard drug.
Conclusions
It was determined that some of synthesized compounds had considerable anticancer activity against the A549 cell lines. Compound
4a
including phenyl moiety was the most active compound against the A549 cell line and was identified as a lead moiety. Besides, compound
4c
including 4-metoxy phenyl moiety exhibited cytotoxic activity against A549 cells. Consequently, compounds possess phenyl and 4-methoxy phenyl moieties have been determined to be important for cytotoxic activity of these compounds.
3-Amino-5-(4-chlorophenylamino)-4-cyanofuran-2-carboxamide (2) was used as the key molecule for preparation of various furopyrimidines 3-9 and formation of spiro-cycloalkane furopyrimidines 10, 11. ...Also, poly fused heterocyclic compounds 13-17 were prepared from compound 2. The synthesized compounds were screened for their antimicrobial activity.
3-Amino-5-(4-klorfenilamino)-4-cijanofuran-2-karboksamid (2) upotrebljen je kao ključni spoj za pripravu različitih furo-pirimidina 3-9 i spiro-cikloalkan furopirimidina 10 i 11. Fuzionirani heterociklički spojevi 13-17 pripravljeni su također polazeći iz spoja 2. Sintetizirani spojevi ispitani su na antimikrobno djelovanje.
This study was aimed at the synthesis of fused benzothiophene derivatives containing heterocyclic moiety. The reaction of the tetrahydrobenzobthiophene derivatives 1a,b with ...ethoxycarbonylisothiocyanate afforded the thiourea derivatives 2a,b. Cyclization of the latter products gave the annulated benzobthienopyrimidine derivatives 3a,b. Compounds 2a,b and 3a underwent a series of heterocyclization reactions through the reaction with some chemical reagents to give the new benzobthienopyrimidine derivatives 5a,b to 8a-c. Also, this work was extended to study the potential role of the novel synthesized thiourea derivative 2a and benzobthienopyrimidine derivatives 3a, 5b, 6a and 8b as antidepressant, sedative or analgesic agents at two doses (15 or 30 mg kg-1 body mass). Some compounds (2a, 3a and 5b) showed mild antidepressant activity in the forced-swimming test. No compound showed sedative effect. Visceral pain evoked by i.p. injection of acetic acid in mice was significantly inhibited by all compounds at a high doses.
U radu je opisana sinteza fuzioniranih derivata benzotiofena koji sadrže heterociklički ostatak bitan za farmakološko djelovanje. Tiourea derivati 2a,b dobiveni su reakcijom derivata tetrahidrobenzobtiofena 1a,b s etoksikarbonilizotiocijanatom. Iz njih su dalje priređeni anulirani derivati benzobtienopirimidina 3a,b. Spojevi 2a,b i 3a su reakcijama heterociklizacije prevedeni u benzobtienopirimidine 5a,b-8a-c. Ispitivano je antidepresivno, sedativno i analgetsko djelovanje novosintetiziranih derivata tiouree 2a i benzobtienopirimidina 3a, 5b, 6a i 8b u dvije doze (15 ili 30 mg kg-1 tjelesne mase). Spojevi 2a, 3a i 5b pokazali su blago antidepresivno djelovanje u testu forsiranog plivanja, dok sedativni učinak nije pokazao niti jedan ispitivani spoj. Visceralna bol inducirana i.p. injekcijom octene kiseline u miševa značajno je inhibirana sa svim spojevima, ali u visokim dozama.
3-Amino-5-(4-klorfenilamino)-4-cijanofuran-2-karboksamid (2) upotrebljen je kao ključni spoj za pripravu različitih furo-pirimidina 3-9 i spiro-cikloalkane furopirimidina 10 i 11. Fuzionirani ...heterociklički spojevi 13-17 pripravljeni su također polazeći iz spoja 2. Sintetizirani spojevi ispitani su na antimikrobno djelovanje.
4,6-Diamino-1H-pirimidin-2-tion (1) upotrebljen je kao ishodni spoj u sintezi derivata pirimidina 2-5. Spoj 5 je cikliziran u pirimido2,1-b1,3tiazin derivat 6, koji je kondenziran s ...p-klorbenzaldehidom u spoj 7. Produkt 7 je u reakciji s hidroksilaminom dao izoksazol4,5-dtiazino2,3-apirimidin 8. Spoj 8b je u reakciji s 2-kloretil metil eterom dao spoj 9. Slično je spoj 3 reagirao s kloroctenom kiselinom i dao tiazol3,2-apirimidin 10, koji je kondenziran s p-klorbenzaldehidom u produkt 11. Spoj 11 je kondenzacijom s hidroksilaminom dao izoksazol4,5-dtiazolo2,3-apirimidin 12. Spoj 12b je s 2-kloretil metil eterom dao produkt 13. Biološka evaluacija pokazuje da neki od sintetiziranih produkata imaju antimikrobno djelovanje.
U radu je opisana sinteza fuzioniranih derivata benzotiofena koji sadrže heterociklički ostatak bitan za farmakološko djelovanje. Tiourea derivati 2a,b dobiveni su reakcijom derivata ...tetrahidrobenzobtiofena 1a,b s etoksikarbonilizotiocijanatom. Iz njih su dalje priređeni anulirani derivati benzobtienopirimidina 3a,b. Spojevi 2a,b i 3a prevedeni su reakcijama heterociklizacije u benzobtienopirimidine 5a,b-8a-c. Ispitivano je antidepresivno, sedativno i analgetsko djelovanje novosintetiziranih derivata tiouree 2a i benzobtienopirimidina 3a, 5b, 6a i 8b u dvije doze (15 ili 30 mg kg1 tjelesne mase). Spojevi 2a, 3a i 5b pokazali su blago antidepresivno djelovanje u testu forsiranog plivanja, dok sedativni učinak nije pokazao niti jedan ispitivani spoj. Visceralna bol inducirana i.p. injekcijom octene kiseline u miševa značajno je inhibirana sa svim spojevima, ali u visokim dozama.
A síndrome de Asperger éuma perturbação caraterizada pelo compromisso da interação social e um padrão de comportamentos estereotipados. Estes incluem comportamentos repetitivos, irritabilidade, ...agressividade, hiperatividade e desatenção. O tratamento dos sintomas comportamentais constitui um desafio, com escassos estudos acerca da eficácia das diferentes abordagens terapêuticas. Este artigo é a primeira descrição do uso bem‑sucedido de palmitato de paliperidona mensal no tratamento de sintomas comportamentais num adulto com síndrome de Asperger.
Objetivo: Evaluar el efecto protector del extracto acuoso de Cymbopogon citratus (DC) Stapf, ante el daño inducido por las radiaciones UVC. Material y Métodos: Para evaluar si el extracto acuoso de ...C. citratus era capaz de inducir roturas de cadenas en el ADN, moléculas de plásmido pBluescript SK II fueron tratadas con diferentes concentraciones del extracto (0,01 - 4,0 mg/mL), en los tiempos de exposición: 30, 60 y 90 min. El efecto fotoprotector fue evaluado aplicando el extracto vegetal antes, durante, y después de la irradiación del ADN plasmídico con 200 J/m² de UVC. La actividad enzimática de T4 endonucleasa V fue empleada para detectar formación de CPDs. Las formas superenrollada y relajada de las moléculas de plásmido fueron separadas electroforéticamente en gel de agarosa. Adicionalmente, se midió la transmitancia del extracto acuoso a la DO de 254 nm. Resultados: Ninguna de las concentraciones evaluadas resultó genotóxica con 30 min de tratamiento. Las concentraciones ≥ 2 mg/mL indujeron roturas de cadenas a los 90 min de incubación. El extracto de C. citratus a concentraciones ≥ 0,5 mg/mL protegió al ADN frente a las radiaciones UVC. Conclusiones: En nuestras condiciones experimentales, el extracto acuoso de C. citratus protege al ADN frente a la genotoxicidad inducida por la luz UVC, previniendo la generación de CPDs, pero no es capaz de eliminarlas una vez formadas.
Nutrition related diseases. Inborn errors of purine-pyrimidine metabolism
This paper constitutes a thematic review on inborn errors of purine-pyrimidine metabolism.
Purines and pyrimidines are ...nitrogenous non protein substances, with low molecular
weight, biologically active, that perform essential functions in life transmission and in
body functioning. These conditions result in chronic diseases that might be treated with
appropriate therapies including gen therapy -that may provide a definitive cure. Although
diet is used as adjuvant therapy to prevent some manifestations of gout, it plays no relevant
part in the treatment of these conditions.
El presente trabajo es una revisión temática sobre los errores congénitos
en el metabolismo de las pirimidinas y purinas, que son sustancias nitrogenadas no proteicas,
de bajo peso molecular, biológicamente activas, que desempeñan funciones esenciales
en la transmisión de la vida y en el funcionamiento del organismo. Las consecuencias
de estos trastornos son enfermedades crónicas, pasibles de tratamientos adecuados,
incluyendo en algunos de ellos la posibilidad de la terapia génica, con la solución
definitiva del proceso.
Excepto como coadyuvante para prevenir algunas de las manifestaciones de la gota, la
dieta no constituye un aspecto relevante en el tratamiento de estos trastornos.
Yeast based supplements for animal feeding Cantoni, C. (Milan Univ. (Italy). Dipartimento di Scienze e Tecnologie Veterinarie per la Sicurezza Alimentare)
Archivio Veterinario Italiano (Italy),
(May 2005), Letnik:
56, Številka:
3-4
Journal Article
A brief review on the yeast products for animal nutrition is here reported
Viene fornita una rassegna sui preparati a base di lievito commercializzati
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