48144-44-1Relevant academic research and scientific papers
Novel compounds having treatment of immune diseases and use therof
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Paragraph 0086-0092, (2016/11/24)
The present invention relates to a novel compound capable of effectively treating and preventing immune disease and to a use thereof. The novel compound of the present invention suppresses the production of inflammatory cytokines and increases activities of regulatory T cells having immune regulatory ability. In addition, the compound of the present invention controls over an excessive immune response by inhibiting the production of autoantibodies and differentiation of osteoclasts, thereby being able to be used for treating immune diseases induced by regulatory anomalies of various immune response such as autoimmune disease, inflammatory diseases, and transplant rejection.(a) Cell toxicity effect control(MTT assay)(AA) Normal mouse cell(b) Autoantibody production immune reaction control(c) Inflammatory cytokine production control(d) Inflammatory gene expression controlCOPYRIGHT KIPO 2016
Regioselective synthesis of pyrimido[1,2-a][1,3,5]triazin-6-ones via reaction of 1-(6-oxo-1,6-dihydropyrimidin-2-yl)guanidines with triethylorthoacetate: Observation of an unexpected rearrangement
Sachdeva, Nikhil,Dolzhenko, Anton V.,Keung Chui, Wai
scheme or table, p. 4586 - 4596 (2012/07/28)
A novel thermal rearrangement, involving pyrimidine ring opening and subsequent ring closure leading to recyclization of the system, was identified in the reaction of (6-oxo-1,6-dihydropyrimidin-2-yl)guanidines 3 (where NR 1R2 = NH2, NH alkyl, NH aralkyl, NHCH 2Ph(R)) with triethyl orthoacetate, affording 4-substituted-2-methyl- 6H-pyrimido[1,2-a][1,3,5]triazin-6-ones 6 and their ring opened products. However, no such rearrangement was observed with (6-oxo-1,6-dihydropyrimidin-2- yl)guanidines 3 bearing a tertiary amino or anilino substituent (i.e. where NR1R2 = N(CH3)2, indoline, morpholino, NHAr). As expected, 2-substituted-4-methyl-6H-pyrimido[1,2-a][1,3,5] triazin-6-ones 4 were obtained as the final products. Experimental structural determination and theoretical studies were carried out to get an understanding of the observed thermal rearrangement. In addition, an attempt to obtain similar pyrimido[1,2-a][1,3,5]triazin-6-ones using N,N-dimethylacetamide dimethyl acetal (DMA-DMA) as one carbon inserting synthon had furnished triazine ring annulated product 14 bearing N,N-dimethyl enamino substituent at position 4 as a result of further reaction with a second molecule of DMA-DMA.
