103871-32-5Relevant academic research and scientific papers
Structure-activity dependency of new bacterial tryptophanyl tRNA synthetase inhibitors
Witty, David R.,Walker, Graham,Bateson, John H.,O'Hanlon, Peter J.,Cassels, Robert
, p. 1375 - 1380 (2007/10/03)
Analogues of the aminoacyl tRNA synthetase inhibitor, indolmycin, have been synthesised in which the side chain methyl group is replaced by a wide range of substituents. Their antibacterial and enzyme inhibitory potency is related to steric properties and
Indole and indazole derivatives, for the treatment and prophylaxis of cerebral disorders, their preparation and their use
-
, (2008/06/13)
Compounds of formula (I) : [in which R1 and R2 are each hydrogen or various organic groups, pis 0, 1, 2 or 3, U is -CO- or -CH(OR3)- where R3 is hydrogen or a hydroxy-protecting group, V is an optionally unsaturated aliphatic hydrocarbon group and W is a nitrogen-containing group] are useful in the treatment and prophylaxis of dementia especially of the Alzheimer's type.
New Total Synthesis of (+/-)-Indolmycin
Dirlam, John P.,Clark, David A.,Hecker, Scott J.
, p. 4920 - 4924 (2007/10/02)
A convergent total synthesis of the antibiotic (+/-)-indolmycin (1) is presented.N-Carbobenzoxy-3-(1-chloroethyl)indole (12) is prepared in three steps from indole-3-carboxaldehyde (9).Alkylation of the lithium anion of 2-(dimethylamino)-4(5H)-oxazolone (4) with chloride (12) provides a mixture of the (+/-)-2-dimethylamino derivative of indolmycin (13) and its diastereomer (14) in a ratio of 2.2:1.Amine exchange is effected by treatment of 13 with methylamine, affording (+/-)-1 in five steps from commercially available 9.Efforts to extend this technology toward an asymmetric synthesis of (-)-1 are described.
