Potasiyel olarak aktif 2, 4-tiyazolidindion türevleri üzerinde sentez çalışmaları
Küçük Resim Yok
Tarih
2001
Yazarlar
Dergi Başlığı
Dergi ISSN
Cilt Başlığı
Yayıncı
Ege Üniversitesi
Erişim Hakkı
info:eu-repo/semantics/closedAccess
Özet
45 ÖZET Epilepsi en yaygın nörolojik hastalıklardan biridir. Serebral nöronların anormal deşarjlar yapması sonucu ortaya çıkan ve tekrarlanır, geçici ataklarla kendini gösteren bir hastalıktır. Epilepsi tedavisinde kullanılan ilaçların en iyi şekilde kullanılmalarına karşın, tutarıkları tamamıyla önlemede başarılı değildir. Bu nedenle yeni antiepileptik ilaçlara duyulan gereksinim özellikle vurgulanmaktadır. Bu çalışmada amacımız, potansiyel antikonvülzan olarak tasarlanan 2- (Z^Aö-tetrahidro-^-diokso-l,3-tiyazol-3-il)-/V-fenilasetamit bileşiğinin sentezinin gerçekleştirilmesidir. Bu amaçla kloroasetik asit ve tiyoüre, literatürde bildirilen yönteme göre tepkimeye sokularak 2,4-tiyazolidindion bileşiği elde edilmiştir. Daha sonra, elde edilen 2,4-tiyazolidindion, anilin ve 2-kloroasetil klorürün tepkimesiyle hazırlanan 2-kloro-N-fenilasetamit bileşiği ile, metanol ve sodyum metoksit varlığında 5 saat kaynatılmıştır. Reaksiyon ürünü, sütun kromatografisi ile saflaştırılmıştır. Elde edilmesi arzulanan bileşiğin yapısını tamamıyla desteklemeyen spektral analiz sonuçları, reaksiyon ürününün yapısını aydınlatmada yetersiz kalmıştır. Kesin yapının saptanabilmesi için daha ileri spektral analizler gereklidir
46 SUMMARY Epilepsy is one of the most common neurological diseases. It is a chronic and often progressive disorder characterized by recurrent transient attacks which are caused by an abnormal discharge of cerebral neurons. Despite the optimal use of available antiepileptic drugs, the treatment is not satisfactory in preventing seizures completely. Therefore, the need for safer and more effective new antiepileptic drugs is well known. In this study, our aim was to realize the synthesis of 2-(2,3,4,5-tetrahydro- 2,4-dioxo-1,3-thiazole-3-yl)-/V-phenylacetamide derivative which is designed as a potential anticonvulsant. For this purpose, chloroacetic acid and thiourea have been reacted to yield 2,4-thiazolidinedione, according to method reported in literature. Then, 2,4-thiazolidinedione and 2-chloro-A/-phenylacetamide, which was prepared from aniline and 2-chloroacetyl chloride, have been heated to reflux for five hours in the presence of methanol and sodium methoxyde. The product of the reaction has been purified by column chromatography. The results of spectral analyses (UV, IR, 1H NMR and EIMS), which have not completely supported the structure of the desired product, have failed for structure elucidation of the reaction product. Further detailed spectral analyses should be done to assign the exact structure.
46 SUMMARY Epilepsy is one of the most common neurological diseases. It is a chronic and often progressive disorder characterized by recurrent transient attacks which are caused by an abnormal discharge of cerebral neurons. Despite the optimal use of available antiepileptic drugs, the treatment is not satisfactory in preventing seizures completely. Therefore, the need for safer and more effective new antiepileptic drugs is well known. In this study, our aim was to realize the synthesis of 2-(2,3,4,5-tetrahydro- 2,4-dioxo-1,3-thiazole-3-yl)-/V-phenylacetamide derivative which is designed as a potential anticonvulsant. For this purpose, chloroacetic acid and thiourea have been reacted to yield 2,4-thiazolidinedione, according to method reported in literature. Then, 2,4-thiazolidinedione and 2-chloro-A/-phenylacetamide, which was prepared from aniline and 2-chloroacetyl chloride, have been heated to reflux for five hours in the presence of methanol and sodium methoxyde. The product of the reaction has been purified by column chromatography. The results of spectral analyses (UV, IR, 1H NMR and EIMS), which have not completely supported the structure of the desired product, have failed for structure elucidation of the reaction product. Further detailed spectral analyses should be done to assign the exact structure.
Açıklama
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Anahtar Kelimeler
Eczacılık ve Farmakoloji, Pharmacy and Pharmacology
