- A Mild Heteroatom (O -, N -, and S -) Methylation Protocol Using Trimethyl Phosphate (TMP)-Ca(OH) 2Combination
-
A mild heteroatom methylation protocol using trimethyl phosphate (TMP)-Ca(OH)2combination has been developed, which proceeds in DMF, or water, or under neat conditions, at 80 °C or at room temperature. A series of O-, N-, and S-nucleophiles, including phenols, sulfonamides, N-heterocycles, such as 9H-carbazole, indole derivatives, and 1,8-naphthalimide, and aryl/alkyl thiols, are suitable substrates for this protocol. The high efficiency, operational simplicity, scalability, cost-efficiency, and environmentally friendly nature of this protocol make it an attractive alternative to the conventional base-promoted heteroatom methylation procedures.
- Tang, Yu,Yu, Biao
-
-
- Synthesis and antifungal activity of nicotinamide derivatives as succinate dehydrogenase inhibitors
-
Thirty-eight nicotinamide derivatives were designed and synthesized as potential succinate dehydrogenase inhibitors (SDHI) and precisely characterized by 1H NMR, ESI-MS, and elemental analysis. The compounds were evaluated against two phytopath
- Ye, Yong-Hao,Ma, Liang,Dai, Zhi-Cheng,Xiao, Yu,Zhang, Ying-Ying,Li, Dong-Dong,Wang, Jian-Xin,Zhu, Hai-Liang
-
p. 4063 - 4071
(2014/05/20)
-
- Synthesis and antifungal activity of nicotinamide derivatives as succinate dehydrogenase inhibitors
-
Thirty-eight nicotinamide derivatives were designed and synthesized as potential succinate dehydrogenase inhibitors (SDHI) and precisely characterized by 1H NMR, ESI-MS, and elemental analysis. The compounds were evaluated against two phytopathogenic fungi, Rhizoctonia solani and Sclerotinia sclerotiorum, by mycelia growth inhibition assay in vitro. Most of the compounds displayed moderate activity, in which, 3a-17 exhibited the most potent antifungal activity against R. solani and S. sclerotiorum with IC50 values of 15.8 and 20.3 μM, respectively, comparable to those of the commonly used fungicides boscalid and carbendazim. The structure-activity relationship (SAR) of nicotinamide derivatives demonstrated that the meta-position of aniline was a key position contributing to the antifungal activity. Inhibition activities against two fungal SDHs were tested and achieved the same tendency with the data acquired from in vitro antifungal assay. Significantly, 3a-17 was demonstrated to successfully suppress disease development in S. sclerotiorum infected cole in vivo. In the molecular docking simulation, sulfur and chlorine of 3a-17 were bound with PHE291 and PRO150 of the SDH homology model, respectively, which could explain the probable mechanism of action between the inhibitory and target protein.
- Ye, Yong-Hao,Ma, Liang,Dai, Zhi-Cheng,Xiao, Yu,Zhang, Ying-Ying,Li, Dong-Dong,Wang, Jian-Xin,Zhu, Hai-Liang
-
p. 4063 - 4071
(2015/04/22)
-
- Synthesis and diuretic activity of pyrido[2,3-d]pyrimidones and related compounds
-
The synthesis of a series of pyrido[2,3-d]pyrimidine-4-one derivatives (7) and the results of a study of their potassium-sparing diuretic activity are described. Compounds 7 were prepared from 2-chloro-3-pyridinecarbonyl chloride, 1,2-dihydro-2-thioxo-3-pyridinecarbonyl chloride, 2-methylthio-3-pyridinecarbonyl chloride or 2-(p-chlorophenyl)thio-3-pyridinecarbonylchloride and different amines through the respective amides (4). Compounds 4 and 7 were assayed for diuretic and potassium-sparing activities. Although some of the compounds showed significant diuretic activity, a significant increase of the Na+/K+ index was only observed with 5-oxo-5H(1,3)thiazolo[3,2-a]pyrido[3,2-e]pyrimidine.
- Monge,Martinez-Merino,Cenarruzabeitia,et al.
-
-
- Pyridinethiones. IX Preparation of Ricinidine, Thioricinidine and Other 2(1H)-Pyridones and -thiones Related to Nicotinic acid
-
1(1H)-Pyridones and -thiones related to 1-substituted nicotinic acid derivatives have been prepared via the corresponding 1-substituted-3-formyl-2(1H)-pyridones and -thiones.A number of synthetic procedures for the interconversion of functional groups in these nicotinic acid derivatives are given i.e. preparation of the aldoximes, nitriles, carboxamides and carboxylic acids as well as the 3-hydroxyalkyl derivatives.The course of the basic peroxide oxidation of the 1-substituted-3-formyl-2(1H)-pyridinethiones is found to be very dependent upon the electronegativity ofthe 1-substituent.A preparation of ricinidine is also described.
- Becher, Jan,Johansen, Tea,Michael, Maged Aziz
-
-
