128061-80-3Relevant academic research and scientific papers
Vasoactive thiomethyl-pyrimidines: Promising drug candidates with vascular activity
De Andrade, Audrey N.,Araújo, Alice V.,Barbosa, Hugo B.W.,Wanderley, Almir G.,Malta, Oscar L.,Dos Anjos, Janaína V.
, p. 1266 - 1273 (2017/06/06)
Pyrimidines and their derivatives are present in various biologically active molecules. Most of the synthetic methods employed to achieve the pyrimidinone ring consist of two stages: The synthesis of a Michael intermediate from an aldehyde and an "active
Synthesis of a 2,4,6-trisubstituted 5-cyano-pyrimidine library and evaluation of its immunosuppressive activity in a Mixed Lymphocyte Reaction assay
Stella, Alessandro,Van Belle, Kristien,De Jonghe, Steven,Louat, Thierry,Herman, Jean,Rozenski, Jef,Waer, Mark,Herdewijn, Piet
, p. 1209 - 1218 (2013/03/28)
A series of novel pyrimidine analogues were synthesized and evaluated for immunosuppressive activity in the Mixed Lymphocyte Reaction assay, which is well-known as the in vitro model for in vivo rejection after organ transplantation. Systematic variation of the substituents at positions 2, 4 and 6 of the pyrimidine scaffold led to the discovery of 2-benzylthio-5-cyano-6-(4- methoxyphenyl)-4-morpholinopyrimidine with an IC50 value of 1.6 μM in the MLR assay.
Novel pyrimidinone derivatives: Synthesis, antitumor and antimicrobial evaluation
Taher, Azza,Helwa, Amira Atef
experimental part, p. 521 - 530 (2012/06/01)
Starting from 6-aryl-4-oxo-2-thioxo-1,2,3,4-tetrahydropyrimidine-5- carbonitrile (4a-d), a series of mono- and dialkyl derivatives 5a-j and 6a, b was synthesized. Hydrazinolysis of 4a, b, d and 5d afforded the hydrazino derivatives 7a-c which were cyclised to give the triazolopyrimidinones 8a-c and the pyrimidotriazinones 9a-c through the reaction with formic acid and chloroacetyl chloride, respectively. Most of the newly synthesized compounds were evaluated for their in-vitro antitumor activity. Compounds 6a and b displayed promising anticancer activity against leukaemia, non-small cell lung, melanoma, and renal cancer. On the other hand, all compounds prepared were screened for their in-vitro antibacterial and antifungal activities. Compounds 5h and j showed significant activity against Staphylococcus aureus, while compounds 5e, 7c and 8c displayed moderate inhibitory activity against Candida albicans.
An efficient and facile synthesis of inhibitors for hepatitis C viral and anti-SARS agents: 4-aryl-5-cyano-1,6-dihydro-2-thiouracils
Rong, Liangce,Yin, Shan,Xia, Sheng,Tao, Shimin,Shi, Yanhui,Tu, Shujiang
experimental part, p. 983 - 993 (2012/08/07)
One-pot, multicomponent reaction for the synthesis of 4-aryl-5-cyano-1,6- dihydro-2-thiouracils via three-component from aromatic aldehydes, ethyl 2-cyanoacetate and S-benzylisothiourea hydrochloride (methyl carbamimidothioate sulfate) under methanol is d
A one pot regioselective synthesis of new functionalized derivatives of [1,2,41 Triazolo [4,3-α] pyrimidin-5 (lH)-one
Mahran, Asma M.,Nada, Afaf A.,Ragab
scheme or table, p. 225 - 237 (2011/06/19)
REACTION of 5-cyano-6-aryl-2-thiouracil 1A-C or its methylthio derivatives 2A-C with hydrazonoyl chlorides 3a-h led to the formation of 7-aryl-6-cyano-1,2,4-triazolo[4,3-a] pyrmidin-5(111)-one derivatives 8. The mechanism and the regioselectivity of the studied reactions were discussed with the help of the given X-ray crystallographic data .
Suitably functionalised pyrimidines as potential antimycotic agents
Agarwal, Nidhi,Raghuwanshi, Sandeep K.,Upadhyay,Shukla,Ram, Vishnu J.
, p. 703 - 706 (2007/10/03)
Various suitably functionalised pyrimidine derivatives have been synthesized to explore their potential as antimycotic agents. Some of the synthesized compounds 4c, 4d, 8a-e have shown highly significant in vitro antifungal activity against five human pathogenic fungi. (C) 2000 Elsevier Science Ltd. All rights reserved.
Glycosylation of 2-thiouracil derivatives. A synthetic approach to 3- glycosyl-2,4-dioxypyrimidines
Khodair,Ibrahim,El Ashry
, p. 433 - 444 (2007/10/03)
Reaction of 6-aryl-5-cyano-2-thiouracils 2a-d with glycosyl halides 4a,b under alkaline conditions gave the respective bisglycosylated derivatives 5a- h. However, their deacetylation with ammonia in methanol caused a cleavage of the S-glycosyl residue and gave the N-3 glycosylated analogues 6a-h.
Chemotherapeutic Agents. XII - Synthesis of Pyrimidines and Fused Pyrimidines as Leishmanicides and Herbicides
Ram, Vishnu Ji
, p. 893 - 905 (2007/10/02)
Various bicyclic (2, 3) and tricyclic (4, 5) heterocycles were prepared by the reaction of 1a, c with dihaloalkanes and polynitrohalobenzene separately.Electrophilic substitution on 1a-c with different alkyl halides yielded mono and dialkyl pyrimidines (6-20).Nucleophilic substitution reactions on 18 and 21 with amine and hydrazine separately yielded 22-31, 21a, b and 41c.Reaction of 25a with ethyl ethoxymethylenecyanoacetate and chloroacetyl chloride separately provided bicyclic compounds 32 and 33.Condensation-cyclization of 25a with formic, acetic and nitrous acid separately yielded 34a, b and 35.Reaction of 26a with ethylthioglycolate and thiourea separately provided 36a and 39.The latter was alkylated with methyl iodide to 40.An attempt to cyclize 29a and 30a with thionyl chloride provided bicyclic compounds 37a, b and an uncyclic product 38.Some of the compounds were screened for leishmanicidal and herbicidal activities and a few of them exhibited significant activity.
