197370-13-1Relevant articles and documents
Synthesis and Study of Head-to-Tail Regioregular Poly(alkyl thiophene-3-carboxylates)
Amarasekara, Ananda S.,Pomerantz, Martin
, p. 2255 - 2258 (2003)
Regioregular head-to-tail poly(alkyl thiophene-3-carboxylates) have been prepared by very careful formation of the mono-Grignard reagent from alkyl 2,5-dibromothiophene-3-carboxylates (-40°C, 1 h) followed by nickel-catalyzed polymerization. The spectral properties are reported along with the molecular weights.
An insight into the pharmacophores of phosphodiesterase-5 inhibitors from synthetic and crystal structural studies
Chen, Gong,Wang, Huanchen,Robinson, Howard,Cai, Jiwen,Wan, Yiqian,Ke, Hengming
, p. 1717 - 1728 (2008)
Selective inhibitors of cyclic nucleotide phosphodiesterase-5 (PDE5) have been used as drugs for treatment of male erectile dysfunction and pulmonary hypertension. An insight into the pharmacophores of PDE5 inhibitors is essential for development of second generation of PDE5 inhibitors, but has not been completely illustrated. Here we report the synthesis of a new class of the sildenafil derivatives and a crystal structure of the PDE5 catalytic domain in complex with 5-(2-ethoxy-5-(sulfamoyl)-3-thienyl)-1-methyl-3-propyl-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one (12). Inhibitor 12 induces conformational change of the H-loop (residues 660-683), which is different from any of the known PDE5 structures. The pyrazolopyrimidinone groups of 12 and sildenafil are well superimposed, but their sulfonamide groups show a positional difference of as much as 1.5 A. The structure-activity analysis suggests that a small hydrophobic pocket and the H-loop of PDE5 are important for the inhibitor affinity, in addition to two common elements for binding of almost all the PDE inhibitors: the stack against the phenylalanine and the hydrogen bond with the invariant glutamine. However, the PDE5-12 structure does not provide a full explanation to affinity changes of the inhibitors. Thus alternatives such as conformational change of the M-loop are open and further structural study is required.
Synthesis and molecular properties of isomeric thienoisoindigo
Cao, Jian,Chen, Yaorong,Hong, Wenjing,Ren, Xiancheng,Wang, Chang-Cheng,Wang, Hua-Chun,Xu, Yun-Xiang
supporting information, p. 13218 - 13225 (2021/10/14)
Three isomers of thienoisoindigo (TII) are prepared by changing the ring-fusion mode or the amide arrangement of lactam units, namely, 5,10-dihexyl-5,10-dihydrodithieno[3,2-c:3′,2′-h][2,6]naphthyridine-4,9-dione (TVTDA), 4,10-dihexyldithieno[3,2-c:3′,2′-h
SELECTIVE INHIBITORS OF CLINICALLY IMPORTANT MUTANTS OF THE EGFR TYROSINE KINASE
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Page/Page column 143, (2019/01/21)
The present invention provides compounds of Formula (I) or a subgeneric structure or species thereof, or a pharmaceutically acceptable salt, ester, solvate, and/or prodrug thereof, and methods and compositions for treating or ameliorating abnormal cell pr
Palladium-catalyzed intramolecular C-H arylation of 2-halo-: N -Boc- N -arylbenzamides for the synthesis of N-H phenanthridinones
Hu, Quan-Fang,Gao, Tian-Tao,Shi, Yao-Jie,Lei, Qian,Yu, Luo-Ting
, p. 13879 - 13890 (2018/04/25)
A palladium catalyzed synthesis of N-H phenanthridinones was developed via C-H arylation. The protocol gives phenanthridinones regioselectively by one-pot reaction without deprotection. It exhibits broad substrate scope and affords targets in up to 95% yields. Importantly, it could be applied for the less reactive o-chlorobenzamides.
