33342-26-6Relevant academic research and scientific papers
Synthesis and bioactivity of phenyl substituted furan and oxazole carboxylic acid derivatives as potential PDE4 inhibitors
Lin, Yinuo,Ahmed, Wasim,He, Min,Xiang, Xuwen,Tang, Riyuan,Cui, Zi-Ning
, (2020/10/02)
In this present study, a series of 5-phenyl-2-furan and 4-phenyl-2-oxazole derivatives were designed and synthesized as phosphodiesterase type 4 (PDE4) inhibitors. In vitro results showed that the synthesized compounds exhibited considerable inhibitory ac
Synthesis and fungicidal activity of aryl carbamic acid-5-aryl-2- furanmethyl ester
Ying,Bao-Ju,Ling,Miao, Hong-Jian,Yan-Xia,Yang, Xin-Ling
, p. 3037 - 3042 (2011/07/31)
Chitin, a major structural component of insect cuticle and fungus cell wall but absent in plants and vertebrates, is regarded as a safe and selective target for pest control agents. Chitin synthesis inhibitors (CSIs) have been well-known as insect growth regulators (IGRs) but rarely found as fungicides in agriculture. To find novel CSIs with good activity, benzoylphenylurea, a typical kind of CSIs, was chosen as the lead compound and 26 novel aryl carbamic acid-5-aryl-2-furanmethyl esters were designed by converting the urea linkages of benzoylphenylureas to carbamic acid esters and changing the aniline parts into furanmethyl groups. The title compounds were synthesized and their structures confirmed by IR, 1H NMR, and elemental analysis. Preliminary insecticidal and fungicidal bioassays were carried out. The results indicated that the title compounds had no insecticidal effect on Culex pipiens pallens and Plutella xylostella Linnaeus, but most compounds exhibited good fungicidal activities against Corynespora cassiicola, Thanatephorus cucumeris, Botrytis cinerea, and Fusarium oxysporum. In particular, compounds V-4, V-6, V-7, and V-8 showed better activities against the four strains than those of the commercialized fungicides. The morphologic result suggested that compound V-21 had disturbed the cell wall formation of C. cassiicola. The results indicated that modification on the urea linkage of benzoylphenylurea was an effective way to discover new candidates for fungicides.
Palladium-catalysed direct arylation of heteroaromatics bearing unprotected hydroxyalkyl functions using aryl bromides
Roger, Julien,Pozgan, Franc,Doucet, Henri
experimental part, p. 696 - 710 (2010/06/19)
Heteroaromatics bearing unprotected hydroxyalkyl functions can be arylated using aryl or heteroaryl bromides, via palladium-catalysed carbonhydrogen bond activation/arylation. Good yields were generally obtained using 0.01-0.5 mol% of the air-stable palladium acetate complex as the catalyst. The nature of the base was found to be crucial for the selectivity of this reaction. Potassium acetate led to the direct arylation products whereas caesium car-bonate led to the formation of the ether. This procedure is certainly more atom-economic than other methods for the preparation of such compounds, as no protection/ deprotection sequence of the hydroxyalkyl function and no preparation of an organometallic derivative is required.
Potent and orally bioavailable noncysteine-containing inhibitors of protein farnesyltransferase
Augeri, David J.,Janowick, Dave,Kalvin, Douglas,Sullivan, Gerry,Larsen, John,Dickman, Daniel,Ding, Hong,Cohen, Jerry,Lee, Jang,Warner, Robert,Kovar, Peter,Cherian, Sajeev,Saeed, Badr,Zhang, Haichao,Tahir, Steve,Ng, Shi-Chung,Sham, Hing,Rosenberg, Saul H.
, p. 1069 - 1074 (2007/10/03)
Potent and orally bioavailable nonthiol-containing inhibitors of protein farnesyltransferase are described. Oral bioavailability was achieved by replacement of the pyridyl ether moiety of 1 with a 2-substituted furan ether to give 4. Potency was regained with 2,5-disubstituted furan ethers while maintaining the bioavailability inherent in 4. p-Chlorophenylfuran ether 24 is 0.7 nM in vitro (FTase) and is 32% bioavailable in the mouse, 30% bioavailable in rats, and 21% bioavailable in dogs.
