26226-72-2Relevant articles and documents
Selective cyclooxygenase inhibition and ulcerogenic liability of some newly prepared anti-inflammatory agents having thiazolo[4,5-d]pyrimidine scaffold
Bakr, Rania B.,Ghoneim, Amira A.,Azouz, Amany A.
, (2019)
Novel candidates of thiazolo[4,5-d]pyrimidines (9a-l)were synthesized and their structures were elucidated by spectral and elemental analyses. All the novel derivatives were screened for their cyclooxygenase inhibitory effect, anti-inflammatory activity and ulcerogenic liability. All the new compounds exhibited anti-inflammatory activity, especially 1-(4-[7-(4-nitrophenyl)-5-thioxo-5,6-dihydro-3H-thiazolo[4,5-d]pyrimidin-2-ylideneamino]phenyl)ethanone (9g)was the most active derivative with 57%, 88% and 88% inhibition of inflammation after 1, 3 and 5h, respectively. Furthermore, this derivative 9g recorded higher anti-inflammatory activity than celecoxib which showed 43%, 43% and 54% inhibition after 1, 3 and 5h, sequentially. Moreover, the target derivatives 9a-l demonstrated moderate to high potent inhibitory action towards COX-2 (IC50 = 0.87–3.78 μM), in particular, the derivatives 9e (IC50 = 0.92 μM), 9g (IC50 = 0.87 μM)and 9k (IC50 = 1.02 μM)recorded higher COX-2 inhibitory effect than the selective COX-2 inhibitor drug celecoxib (IC50 = 1.11 μM). The in vivo potent compounds (9e, 9g and 9k)caused variable ulceration effect (ulcer index = 5–12.25)in comparison to that of celecoxib (ulcer index = 3). Molecular docking was performed to the most potent COX-2 inhibitors (9e, 9g and 9k)to explore the binding mode of these derivatives with Cyclooxygenase-2 enzyme.
New 4-(2-Furyl)-1,4-dihydronicotinonitriles and 1,4,5,6-Tetrahydronicotinonitriles: Synthesis, Structure, and Analgesic Activity
Aksenov, N. A.,Aksenova, I. V.,Bibik, E. Yu.,Dotsenko, V. V.,Frolov, K. A.,Krivokolysko, D. S.,Krivokolysko, S. G.,Pankov, A. A.,Samokish, A. A.,Vasilin, V. K.,Venidiktova, Yu. S.
, p. 1646 - 1660 (2021/11/01)
Abstract: A series of new hybrid molecules containing 2-furyl and partially saturated pyridine fragments was obtained based on the reaction of cyanothioacetamide with furfural and 1,3-dicarbonyl compounds. The resulting compounds were tested in vivo for analgesic activity (rats) in the orofacial trigeminal pain test. Some the tested compounds showed an antinociceptive effect, superior to that of the reference drug (metamizole sodium).
Ethyl benzoate bearing pyrrolizine/indolizine moieties: Design, synthesis and biological evaluation of anti-inflammatory and cytotoxic activities
Attalah, Khalid M.,Abdalla, Ashraf N.,Aslam, Akhmed,Ahmed, Muhammad,Abourehab, Mohammed A.S.,ElSawy, Naser A.,Gouda, Ahmed M.
, (2019/11/26)
Two new series of ethyl benzoate bearing pyrrolizine and indolizine moieties 8–11 were synthesized and evaluated for their anti-inflammatory and anticancer activities. Among these derivatives, compounds 9a, 10b and 11b displayed in vivo anti-inflammatory
