58550-82-6Relevant academic research and scientific papers
N1-benzenesulfonylgramine and N 1-benzenesulfonylskatole: Novel 5-HT6 receptor ligand templates
Pullagurla, Manik R.,Dukat, Ma?gorzata,Setola, Vincent,Roth, Bryan,Glennon, Richard A.
, p. 3355 - 3359 (2003)
1-Benzenesulfonyl-5-methoxy-N,N-dimethyltryptamine (3; Ki=2.3 nM) is a 5-HT6 receptor antagonist; removal of the 5-methoxy group (i.e., 6; Ki=4.1 nM) has little impact on receptor affinity. In the present study, it is shown that the aminomethyl portion of 6 can be shortened to gramine analogue 10a (Ki=3.1 nM); a related skatole derivative 11b (Ki=12 nM) also binds with high affinity indicating that the aminoethyl portion of the tryptamines is not required for binding. Compounds 10a and 11b represent members of novel classes of 5-HT6 antagonists.
A practical synthesis of indole-based heterocycles using an amidoaluminum-mediated strategy
Todd, Robert,Hossain, M. Mahmun
experimental part, p. 1846 - 1850 (2010/01/16)
A large number of biologically active compounds consist of an indole scaffolding. Because of this, chemists are continually searching for more efficient means through which to successfully synthesize the required alkaloids. In our recent effort to synthes
