439919-48-9Relevant academic research and scientific papers
Synthesis and in vivo evaluation of bicyclic gababutins
Blakemore, David C.,Bryans, Justin S.,Carnell, Pauline,Carr, Christopher L.,Chessum, Nicola E.A.,Field, Mark J.,Kinsella, Natasha,Osborne, Simon A.,Warren, Andrew N.,Williams, Sophie C.
scheme or table, p. 461 - 464 (2010/04/05)
Synthesis of a number of bicyclic five-membered ring derivatives of gabapentin led to the identification of two compounds, (-)-(11A) and (20A) which both had an excellent level of potency against α2δ and were profiled in an in vivo model of neu
Synthesis and in vivo evaluation of 3,4-disubstituted gababutins
Blakemore, David C.,Bryans, Justin S.,Carnell, Pauline,Field, Mark J.,Kinsella, Natasha,Kinsora, Jack K.,Meltzer, Leonard T.,Osborne, Simon A.,Thompson, Lisa R.,Williams, Sophie C.
scheme or table, p. 248 - 251 (2010/04/02)
A range of 3,4-alkylated five-membered ring derivatives of gabapentin were synthesised. One compound (21) had an excellent level of potency against α2δ and was profiled in in vivo models of pain and anxiety.
Inhibition of Pseudomonas aeruginosa biofilm formation with bromoageliferin analogues
Huigens III, Robert W.,Richards, Justin J.,Parise, Gina,Ballard, T. Eric,Zeng, Wei,Deora, Rajendar,Melander, Christian
, p. 6966 - 6967 (2008/02/06)
Two analogues of the marine natural product bromoageliferin have been synthesized and subsequently assayed for the ability to inhibit the formation of Pseudomonas aeruginosa biofilms. Both compounds inhibited the ability of Pseudomonas aeruginosa strains
Orally active PDE4 inhibitor with therapeutic potential
Ochiai, Hiroshi,Ohtani, Tazumi,Ishida, Akiharu,Kishikawa, Katuya,Yamamoto, Susumu,Takeda, Hiroshi,Obata, Takaaki,Nakai, Hisao,Toda, Masaaki
, p. 555 - 571 (2007/10/03)
Based on the promising results obtained by the clinical trial of Ariflo, further optimization of the spatial arrangement of the three pharmacophores (the carboxylic acid moiety, nitrile moiety and 3-cyclopentyloxy-4-methoxyphenyl moiety) in the
Stereoselective Total Synthesis of Racemic (3S,4R/3R,4S)- and a Diastereoisomeric Mixture of (6E,10Z)-3,4,7,11-Tetramethyltrideca-6,10-dienal (Faranal); The Trail Pheromone of the Pharaoh's Ant
Baker, Raymond,Billington, David C.,Ekanayake, Neelakanthie
, p. 1387 - 1393 (2007/10/02)
Racemic (3S,4R/3R,4S)-faranal has been synthesised by a convergent, stereospecific route which employed the addition of alkylcopper complexes to terminal acetylenes, to generate two trisubstituted double bonds, and a Diels-Alder reaction to establish the relative stereochemistry of the C-3, C-4 methyl groups.A diastereoisomeric mixture of faranals, enriched in the (3S,4S/3R,4R)-enantiomeric pair , has been synthesised by a somewhat shorter route via an intermediate diester, obtained from electrochemical dimerisation of ethyl crotonate.
A Total Synthesis of (+/-)-Faranal, the True Trail Pheromone of Pharaoh's Ant, Monomorium pharaonis
Knight, David W.,Ojhara, Bol
, p. 955 - 960 (2007/10/02)
A relatively short total synthesis of the true trail pheromone of Pharaoh's ant, (+/-)-faranal is reported.The carbon skeleton was assembled by a Wittig condensation between (Z)-6-methyloct-5-en-2-one (4) and the 5-carboxypentylphosphonium salt (15).The ketone (4) was prepared in 'one-pot' and in a stereoselective manner using vinyl cuprate chemistry, while the relative stereochemistry of the two methyl substituents in the phosphonium salt (15) was established by using the Diels-Alder adduct (16) of buta-1,3-diene and maleic anhydride, which, after reduction and oxidative cleavage of the resulting cis-1,2-dimethylcyclohex-4-ene (18), gave only meso-3,4-dimethyladipic acid (19); this in turn was converted into the salt (15) in six straight-forward steps.
Prostacyclin compounds
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, (2008/06/13)
Prostacyclin derivatives of formula (I): STR1 (wherein R1 represents a hydrogen atom or a lower alkyl group; R2 represents an alkenyl group having from 8 to 12 carbon atoms; and n represents an integer of from 1 to 8, inclusive) and
