- Design, Synthesis, and Fungicidal Evaluation of Novel Pyrazole-furan and Pyrazole-pyrrole Carboxamide as Succinate Dehydrogenase Inhibitors
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The identification of novel succinate dehydrogenase (SDH) inhibitors represents one of the most attractive directions in the field of fungicide research and development. During our continuous efforts to pursue inhibitors belonging to this class, some structurally novel pyrazole-furan carboxamide and pyrazole-pyrrole carboxamide derivatives have been discovered via the introduction of scaffold hopping and bioisosterism to compound 1, a remarkably potent lead obtained by pharmacophore-based virtual screening. As a result of the evaluation against three destructive fungi, including Sclerotinia sclerotiorum, Rhizoctonia solani, and Pyricularia grisea, a majority of them displayed potent fungicidal activities. In particular, compounds 12I-i, 12III-f, and 12III-o exhibited excellent fungicidal activity against S. sclerotiorum and R. solani comparable to that of commercial SDHI thifluzamide and 1.
- Yao, Ting-Ting,Xiao, Dou-Xin,Li, Zhong-Shan,Cheng, Jing-Li,Fang, Shao-Wei,Du, Yong-Jun,Zhao, Jin-Hao,Dong, Xiao-Wu,Zhu, Guo-Nian
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p. 5397 - 5403
(2017/07/13)
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- Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors
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A series of novel pyrazol-furan carboxamide analogues were designed, synthesized and biologically evaluated for their Akt1 inhibitory activities, as well as anti-proliferative efficacies against HCT116 and OVCAR-8 cell lines. Most compounds exhibited mode
- Zhan, Wenhu,Xu, Lei,Dong, Xiaowu,Dong, Jun,Yi, Xiao,Ma, Xiaodong,Qiu, Ni,Li, Jia,Yang, Bo,Zhou, Yubo,Hu, Yongzhou
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supporting information
p. 47 - 58
(2016/05/11)
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- Substituted pyrazol ring derivative and application thereof
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The invention discloses a substituted pyrazol ring derivative. The substituted pyrazol ring derivative is shown as the general formula I. The invention further provides an optical isomer or salt acceptable agriculturally of the substituted pyrazol ring derivative. The substituted pyrazol ring derivative, the optical isomer or the salt acceptable agriculturally can be used for preparing bactericides (including agricultural and gardening bactericides), and therefore prevention and control over agricultural and gardening fungi are achieved.
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Paragraph 0065; 0066; 0067; 0068
(2016/10/09)
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- HETERO-FUSED CYCLIC COMPOUND
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A compound represented by the formula (I) or a salt thereof: wherein a ring Z is a 5 to 6-membered heteroaromatic ring having one or two heteroatoms in the ring; X1 is a hydrogen atom, a hydroxy group, a hydroxy C1-6 alkyl group, —B(OH)2, a boronate ester group, a cyclic boronate ester group, a boranyl group, a cyclic boranyl group, —BF3Mn1, —Sn(R12)(R13)(R14), a leaving group, a carboxy group, a formyl group, or —NR16R17; and X2 is a hydrogen atom or —CO2R18.
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Paragraph 0241; 0242
(2016/07/05)
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- Efficient synthesis and biological evaluation of proximicins A, B and C
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A quick and efficient synthesis and the biological evaluation of promising antitumor-antibiotics proximicins A, B and C are reported. The characteristic repetitive unit of these molecules, the methyl 4-Boc-aminofuran-2-carboxylate 15, was prepared in thre
- Brucoli, Federico,Natoli, Antonino,Marimuthu, Preethi,Borrello, Maria Teresa,Stapleton, Paul,Gibbons, Simon,Sch?tzlein, Andreas
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experimental part
p. 2019 - 2024
(2012/05/05)
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- Novel tricyclic pyrazole BRAF inhibitors with imidazole or furan central scaffolds
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V-RAF murine sarcoma viral oncogene homolog B1 (BRAF) is a serine/threonine-specific protein kinase that is mutated with high frequency in cutaneous melanoma, and many other cancers. Inhibition of mutant BRAF is an attractive therapeutic approach for the treatment of melanoma. A triarylimidazole BRAF inhibitor bearing a phenylpyrazole group (dimethyl-[2-(4-{5-[4-(1H-pyrazol-3-yl)-phenyl]-4-pyridin-4-yl-1H-imidazol-2-yl} -phenoxy)-ethyl]-amine, 1a) was identified as an active BRAF inhibitor. Based on this starting point, we synthesized a series of analogues leading to the discovery of 6-{2-[4-(4-methyl-piperazin-1-yl)-phenyl]-5-pyridin-4-yl-3H- imidazol-4-yl}-2,4-dihydro-indeno[1,2-c]pyrazole (1j), with nanomolar activity in three assays: inhibition of purified mutant BRAF activity in vitro; inhibition of oncogenic BRAF-driven extracellular regulated kinase (ERK) activation in BRAF mutant melanoma cell lines; and inhibition of proliferation in these cells.
- Niculescu-Duvaz, Dan,Niculescu-Duvaz, Ion,Suijkerbuijk, Bart M.J.M.,Ménard, Delphine,Zambon, Alfonso,Nourry, Arnaud,Davies, Lawrence,Manne, Helen A.,Friedlos, Frank,Ogilvie, Lesley,Hedley, Douglas,Takle, Andrew K.,Wilson, David M.,Pons, Jean-Francois,Coulter, Tom,Kirk, Ruth,Cantarino, Neus,Whittaker, Steven,Marais, Richard,Springer, Caroline J.
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experimental part
p. 6934 - 6952
(2010/11/03)
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- OXO-DIHYDROISOINDOLE SULFONAMIDE COMPOUNDS AS MODULATORS OF THE CCK2 RECEPTOR
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Certain oxo-dihydroisoindote sulfonamide compounds of Formula (I): wherein R1 and R2 are each independently fluoro or chloro; R3 is H or methyl; R4 is chloro or bromo; one of X and Y is a carbonyl and the other
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Page/Page column 18
(2008/12/04)
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- SULFONAMIDE COMPOUNDS
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Certain sulfonamide compounds are dual CCK1/CCK2 inhibitors useful in the treatment of CCK1/CCK2 mediated diseases.
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Page/Page column 24-25
(2010/10/20)
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- Heterobicyclic pyrazole derivatives as kinase inhibitors
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Bicyclo-pyrazoles of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in
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Page/Page column 21
(2008/06/13)
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- HETEROBICYCLIC PYRAZOLE DERIVATIVES AS KINASE INHIBITORS
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Bicyclo-pyrazoles of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in
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- Two Syntheses of Manoalide via Heteroatom-Assisted Alkyne Carbometallation
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Two approaches to the sesterterpenoid phospholipase A2 inhibitors seco-manoalide (3) and manoalide (1) are described based on carbometallation of propargylic alcohols to generate the functionalised C6-C7 trisubstituted alkene.Both syntheses also deploy the photooxidation of a furan in order to generate a 4-substituted 5-hydroxy-2(5H)-furanone moiety.
- Bury, Paul,Hareau, Georges,Kocienski, Philip,Dhanak, Dashyant
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p. 8793 - 8808
(2007/10/02)
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