65627-09-0Relevant articles and documents
Novel inhibitors of bacterial two-component systems with gram positive antibacterial activity: Pharmacophore identification based on the screening hit closantel
Hlasta, Dennis J.,Demers, James P.,Foleno, Barbara D.,Fraga-Spano, Stephanie A.,Guan, Jihua,Hilliard, Jamese J.,Macielag, Mark J.,Ohemeng, Kwasi A.,Sheppard, Cheryl M.,Sui, Zhihua,Webb, Glenda C.,Weidner-Wells, Michele A.,Werblood, Harvey,Barrett, John F.
, p. 1923 - 1928 (1998)
This SAR study has shown that the salicylanilide is the pharmacophore for inhibition of the bacterial two-component system. Hydrophobic substituents improve the potency of inhibitors in this series; however, hydrophobicity is not the sole determinant for inhibition; structural and electronic requirements also exist. Closantel (1) was found to inhibit a two- component system and to have antibacterial activity against drug resistant S. aureus and E. faecium.
Concise enantioselective synthesis of (+)-sertraline and (-)-CP-52002 using proline catalysis
Kalshetti, Rupali,Venkataramasubramanian,Kamble, Sanjay,Sudalai, Arumugam
supporting information, p. 1053 - 1055 (2016/02/16)
A short enantioselective synthesis of (+)-sertraline and its C4 epimer (-)-CP-52002 with an overall yield of 30%, respectively, as its hydrochloride has been described. The key steps are the proline catalyzed Mannich reaction of acetaldehyde and acid catalyzed intramolecular Friedel-Crafts' alkylation reaction of olefin proceeding with high optical purities.
One-pot synthesis of gem-difluorostyrenes from benzyl bromide via olefination of phosphonium ylide with difluorocarbene
Deng, Xiao-Yun,Lin, Jin-Hong,Xiao, Ji-Chang
, p. 116 - 120 (2015/11/10)
A new approach for the synthesis of gem-difluorostyrenes from benzyl bromide is described. Quaternization of triphenylphosphine with benzyl bromide to give phosphonium salts, deprotonation of the corresponding phosphonium salts to produce phosphonium ylide, and the subsequent olefination of phosphonium ylide with difluorocarbene generated from difluoromethylene phosphobetaine (Ph3P+CF2CO2-) by decarboxylation can occur smoothly in one-pot, furnishing the final gem-difluorostyrenes in good yields.
