- Visible Light-Catalyzed Benzylic C-H Bond Chlorination by a Combination of Organic Dye (Acr+-Mes) and N-Chlorosuccinimide
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By combining "N-chlorosuccinimide (NCS)"as the safe chlorine source with "Acr+-Mes"as the photocatalyst, we successfully achieved benzylic C-H bond chlorination under visible light irradiation. Furthermore, benzylic chlorides could be converted to benzylic ethers smoothly in a one-pot manner by adding sodium methoxide. This mild and scalable chlorination method worked effectively for diverse toluene derivatives, especially for electron-deficient substrates. Careful mechanistic studies supported that NCS provided a hydrogen abstractor "N-centered succinimidyl radical,"which was responsible for the cleavage of the benzylic C-H bond, relying on the reducing ability of Acr?-Mes.
- Xiang, Ming,Zhou, Chao,Yang, Xiu-Long,Chen, Bin,Tung, Chen-Ho,Wu, Li-Zhu
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p. 9080 - 9087
(2020/08/14)
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- Synthesis and evaluation of a 2-benzothiazolylphenylmethyl ether class of histamine H4 receptor antagonists
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Synthesis and biological evaluation of a new class of histamine H4receptor ligands, distinct from the previously reported chemotypes, are described. A virtual screening of our corporate compound collection identified a hit with an undesired dual H3R/H4R activity. Chemical exploration led to the discovery of a more potent and selective 2-benzothiazolylphenylmethyl ether lead compound.
- Labeeuw, Olivier,Levoin, Nicolas,Billot, Xavier,Danvy, Denis,Calmels, Thierry,Krief, Stéphane,Ligneau, Xavier,Berrebi-Bertrand, Isabelle,Robert, Philippe,Lecomte, Jeanne-Marie,Schwartz, Jean-Charles,Capet, Marc
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p. 5263 - 5266
(2016/10/30)
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- Synthesis, antibacterial and antifungal activities of bifonazole derivatives
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Two series of chlorinated benzhydryl imidazole and triazole derivatives were synthesized and tested in vitro against representative strains of potent pathogenic bacteria (Staphylococcus aureus CIP 4.83, Escherichia hirae CIP 5855, Pseudomonas aeruginosa CIP 82118, Escherichia coli CIP 53126) and fungi (Aspergillus niger IP 1431.83, Candida albicans IP 48.72, Candida krusei IP 208.52, Trichophython rubrum IP 1657.86). Most of these compounds were devoid of any antimicrobial activity, but several of them inhibited T. rubrum with MIC values in the range of 0.125 to 32 μg/mL, similar or superior to those of bifonazole and clotrimazole, used as standard controls. The replacement of the imidazole ring with a triazole moiety in these compounds led to derivatives with less antifungal activity. A preliminary SAR was undertaken on the effect of the number and the position of chlorine atoms on the distribution of negative charge on the surface of some compounds on antifungal activity. Copyright
- El Hage, Salome,Lajoie, Barbora,Feuillolay, Catherine,Roques, Christine,Baziard, Genevieve
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experimental part
p. 402 - 410
(2012/01/11)
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- Design, synthesis, and structure-activity relationships of pyrazolo[3,4-d]pyrimidines: A novel class of potent enterovirus inhibitors
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A series of pyrazolo[3,4-d]pyrimidines were synthesized and their antiviral activity was evaluated in a plaque reduction assay. It is very interesting that this class of compounds provide remarkable evidence that they are very specific for human enteroviruses, in particular, coxsackieviruses. Some derivatives proved to be highly effective in inhibiting enterovirus replication at nanomolar concentrations. SAR studies revealed that the phenyl group at the N-1 position and the hydrophobic diarylmethyl group at the piperazine largely influenced the in vitro antienteroviral activity of this new class of potent antiviral agents. It was found that the pyrazolo[3,4-d]pyrimidines with a thiophene substituent, such as compounds 20-24, in general exhibited high activity against coxsackievirus B3 (IC50=0.063-0.089μM) and moderate activity against enterovirus 71 (IC50=0.32-0.65μM) with no apparent cytotoxic effect toward RD (rhabdomyosarcoma) cell lines (CC5025μ M).
- Chern, Jyh-Haur,Shia, Kak-Shan,Hsu, Tsu-An,Tai, Chia-Liang,Lee, Chung-Chi,Lee, Yen-Chun,Chang, Chih-Shiang,Tseng, Sung-Nien,Shih, Shin-Ru
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p. 2519 - 2525
(2007/10/03)
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- Biocidal benzylbiphenyl derivatives
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This invention concerns compounds of formula. stereochemically isomeric forms thereof, acid or base addition salts thereof, N-oxides thereof, or quaternary ammonium derivatives thereof, wherein the dotted line is an optional bond; X is a direct bond when the dotted line represents a bond, or X is hydrogen or hydroxy, when the dotted line does not represent a bond; R1, R2, R5and R6are each independently selected from hydrogen, halo, hydroxy, C1-4alkyl, C1-4alkyloxy, —SO3H, and the like; R3and R4are each independently selected from hydrogen, halo, hydroxy, C1-4alkyl, C1-4alkyloxy, nitro, amino, cyano, trifluoromethyl, or trifluoromethoxy;L is a radical of formula wherein A1is a direct bond or C1-6alkanediyl; A2is C2-6alkanediyl; and R7to R11are hydrogen, C1-6alkyl, aminoC1-6alkyl and the like; having biocidal properties; their preparation, compositions containing them and their use as a biocide.
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