Antimicrobial and antiurease activities of newly synthesized morpholine derivatives containing an azole nucleus
Yükleniyor...
Dosyalar
Tarih
2013
Dergi Başlığı
Dergi ISSN
Cilt Başlığı
Yayıncı
Springer Birkhauser
Erişim Hakkı
info:eu-repo/semantics/openAccess
Özet
2-[6-(Morpholin-4-yl)pyridin-3-ylamino]acetohydrazide (4) was obtained starting from 6-morpholin-4-ylpyridin-3-amine (2) via the formation of ester (3) and then converted to the corresponding Schiff bases (5, 6) with the reaction with aromatic aldehydes. The carbothioamide (9), obtained from the reaction of hydrazide with phenylisothiocyanate, was converted to the corresponding 1,2,4-triazole (11) and 1,3,4-thiadiazole (12) derivatives by the treatment with NaOH or H2SO4, respectively. The cyclocondenzation of 9 with 4-chlorophenacyl bromide or ethyl bromoacetate produced the corresponding 1,3-thiazole (10) or 1,3-thiazolidine derivatives (13), respectively. Antimicrobial and antiurease activities of newly synthesized compounds were investigated. Some of them were found to be active on M. smegmatis, and they displayed activity toward C. albicans and S. cerevisiae in high concentration. Compound 10 proved to be the most potent showing an enzyme inhibition activity with an IC50 = 2.37 +/- A 0.19 mu M.
Açıklama
Anahtar Kelimeler
Morpholine, 1,2,4-Triazole, 1,3,4-Oxadiazole, Mannich base, Antimicrobial activity, Antiurease activity
Kaynak
Medicinal Chemistry Research
WoS Q Değeri
N/A
Scopus Q Değeri
Q1
Cilt
22
Sayı
8
Künye
Bektaş, H., Ceylan, Ş., Demirbaş, N., Alpay-Karaoğlu, Ş., & Sökmen, B. B. (2013). Antimicrobial and antiurease activities of newly synthesized morpholine derivatives containing an azole nucleus. Medicinal Chemistry Research, 22(8), 3629-3639.
