- A one-pot synthesis of functionalized ethyl 1,3-thiazole-5-carboxylates from thioamides or thioureas and 2-chloro-1,3-dicarbonyl compounds in an ionic liquid
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A simple one-pot synthesis of functionalized ethyl 1,3-thiazole-5- carboxylates from the reaction of 2-chloro-1,3-dicarbonyl compounds with thioureas or thioamides in the presence of 1-butyl-3-methylimidazolium trifluoromethanesulfonate is described. Grap
- Yavari, Issa,Sayyed-Alangi, S. Zahra,Hajinasiri, Rahimeh,Sajjadi-Ghotbabadi, Hadi
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- Discovery of Novel Thiazole Carboxamides as Antifungal Succinate Dehydrogenase Inhibitors
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To contribute molecular diversity for novel fungicide development, a series of novel thiazole carboxamides were rationally designed, synthesized, and characterized with the succinate dehydrogenase (SDH) as target. Bioassay indicated that compound 6g showed the similar excellent SDH inhibition as that of Thifluzamide with IC50 of 0.56 mg/L and 0.55 mg/L, respectively. Some derivatives displayed improved in vitro fungicidal activities against Rhizoctonia cerealis and Sclerotinia sclerotiorum with EC50 of 1.2-16.4 mg/L and 0.5-1.9 mg/L. Surprisingly, 6g showed promising in vitro fungicidal activities against R. cerealis and S. sclerotiorum with EC50 of 6.2 and 0.6 mg/L, respectively, which was superior to Thifluzamide with the EC50 of 22.1 and 4.4 mg/L, respectively. Additionally, compounds 6c and 6g displayed excellent in vivo fungicidal activities against S. sclerotiorum on Brassica napus L. leaves with protective activity of 75.4% and 67.3% at 2.0 mg/L, respectively, while Thifluzamide without activity at 5.0 mg/L. Transcriptomic analysis of S. sclerotiorum treated with 6g by RNA sequencing indicated the down-regulation of succinate dehydrogenase gene SDHA and SDHB, and the inhibition of the TCA-cycle.
- Guo, Xiaofeng,Zhao, Bin,Fan, Zhijin,Yang, Dongyan,Zhang, Nailou,Wu, Qifan,Yu, Bin,Zhou, Shuang,Kalinina, Tatiana A.,Belskaya, Nataliya P.
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- SPECIFIC CARBOXAMIDES AS KCNQ2/3 MODULATORS
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The invention relates to specific carboxamides of formula (I) as KCNQ2/3 modulators, to processes for their preparation, to medicaments comprising these compounds and to the use of these compounds in the preparation of medicaments.
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Page/Page column 43
(2014/06/23)
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- Optimization of brain penetrant 11β-hydroxysteroid dehydrogenase type i inhibitors and in vivo testing in diet-induced obese mice
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11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) has been widely considered by the pharmaceutical industry as a target to treat metabolic syndrome in type II diabetics. We hypothesized that central nervous system (CNS) penetration might be required to see efficacy. Starting from a previously reported pyrimidine compound, we removed hydrogen-bond donors to yield 3, which had modest CNS penetration. More significant progress was achieved by changing the core to give 40, which combines good potency and CNS penetration. Compound 40 was dosed to diet-induced obese (DIO) mice and gave excellent target engagement in the liver and high free exposures of drug, both peripherally and in the CNS. However, no body weight reduction or effects on glucose or insulin were observed in this model. Similar data were obtained with a structurally diverse thiazole compound 51. This work casts doubt on the hypothesis that localized tissue modulation of 11β-HSD1 activity alleviates metabolic syndrome.
- Goldberg, Frederick W.,Dossetter, Alexander G.,Scott, James S.,Robb, Graeme R.,Boyd, Scott,Groombridge, Sam D.,Kemmitt, Paul D.,Sj?gren, Tove,Gutierrez, Pablo Morentin,Deschoolmeester, Joanne,Swales, John G.,Turnbull, Andrew V.,Wild, Martin J.
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p. 970 - 986
(2014/03/21)
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- SPECIFIC CARBOXAMIDES AS KCNQ2/3 MODULATORS
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The invention relates to specific carboxamides, to processes for their preparation, to medicaments comprising these compounds and to the use of these compounds in the preparation of medicaments.
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Paragraph 0304
(2014/06/11)
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- PDE4 INHIBITORS SELECTIVE FOR THE LONG FORM OF PDE4 FOR TREATING INFLAMMATION AND AVOIDING SIDE EFFECTS
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The present invention relates to compounds which are inhibitors of phosphodiesterase-4 (PDE4) useful for the treatment and prevention of stroke, myocardial infarct, cardiovascular inflammatory diseases and disorders and central nervous system disorders, t
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Page/Page column 124
(2010/07/10)
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- ARYL GPR120 RECEPTOR AGONISTS AND USES THEREOF
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Aryl GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.
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Page/Page column 73-74
(2010/05/13)
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- THIAZOLIOPYRIMIDINES AND THEIR USE AS INHIBITORS OF PHOSPHATIDYLINOSITOL-3 KINASE
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Thiazolopyrimidines of formula (I): wherein W represents a thiazole ring; R1 and R2 form, together with the N atom to which they are attached, a group of the following formula (IIa): in which A is a ring system; m is 0, 1 or 2; Rsup
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Page/Page column 33; 46-47
(2009/01/24)
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- FUSED HETEROCYCLIC COMPOUND AND USE THEREOF
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The present invention relates to wherein each symbol is as defined in the specification. The compound has a superior mineral corticoidreceptorantagonistic action and is useful as an agent for the prophylaxis or treatment of hypertension, cardiac failure and the like, a compound having a fused heterocycle, or a prodrug thereof, or a salt thereof; and an agent for the prophylaxis or treatment of hypertension, cardiac failure and the like.
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Page/Page column 335
(2008/06/13)
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- 2-AMINOMETHYLTHIAZOLE-5-CARBOXAMIDES AS PROTEIN KINASE MODULATORS
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This invention concerns novel thiazole compounds. Methods of using these compounds for the treatment, prevention and management of various diseases or disorders, as well as pharmaceutical compositions of these compounds, are also disclosed.
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Page/Page column 28-29
(2008/06/13)
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- Herbicidal thiazolecarboxamide derivatives
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Herbicidal thiazolecarboxamide derivatives of the formula STR1 in which n represents the numbers 0 or 1, A represents in each case optionally substituted alkyl, aryl, heteroaryl, arylamino or heteroarylamino, R1 represents hydrogen, halogen or alkyl, R2 represents hydrogen, halogen or alkyl, R3 represents hydrogen, halogen, alkyl or halogenoalkyl, R4 represents hydrogen, halogen, alkyl or halogenoalkyl, R5 represents hydrogen, halogen, alkyl, nitro or amino, R6 represents hydrogen, halogen, alkyl halogenoalkyl, alkoxy, halogenoalkoxy, alkylthio, halogenoalkylthio or alkoxycarbonyl, and R7 represents hydrogen, halogen, alkyl, nitro or amino
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