41175-39-7Relevant academic research and scientific papers
Synthesis and evaluation of 2-phenyl-1,4-butanediamine-based CCR5 antagonists for the treatment of HIV-1
Tallant, Matthew D.,Duan, Maosheng,Freeman, George A.,Ferris, Robert G.,Edelstein, Mark P.,Kazmierski, Wieslaw M.,Wheelan, Pat J.
, p. 1394 - 1398 (2011/04/16)
We describe the synthesis and potency of a novel series of N-substituted 2-phenyl- and 2-methyl-2-phenyl-1,4-diaminobutane- based CCR5 antagonists. Compounds 7a and 12f were found to be potent in anti-HIV assays and bioavailable in the low-dose rat PK model.
Therapeutic compounds: Patent evaluation of WO2011011652A1
Supuran, Claudiu T.
scheme or table, p. 1491 - 1495 (2012/05/20)
A series of sulfonamide derivatives, incorporating azabicyclo[3.2.1]octane and phenyl-propyl scaffolds, were prepared by a succession of original steps. The compounds are claimed to act as antagonists of the C-C chemokine receptor 5 (CCR5) involved in the
THERAPEUTIC COMPOUNDS
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, (2011/02/24)
The present invention relates to compounds of Formula (I) and (Ia) useful in the treatment of CCR5-related diseases and disorders, for example, the prevention or treatment of an HIV infection, and in the treatment of the resulting acquired immune deficien
Optimization of 1H-tetrazole-1-alkanenitriles as potent orally bioavailable growth hormone secretagogues
Hernandez, Andres S.,Swartz, Stephen G.,Slusarchyk, Dorothy,Yan, Mujing,Seethala, R. Krishna,Sleph, Paul,Grover, Gary,Dickinson, Kenneth,Giupponi, Leah,Harper, Timothy W.,Humphreys, W. Griffith,Longhi, Daniel A.,Flynn, Neil,Murphy, Brian J.,Gordon, David A.,Biller, Scott A.,Robl, Jeffrey A.,Tino, Joseph A.
, p. 2067 - 2072 (2008/12/21)
1H-Tetrazole-1-alkanenitrile SR-9g exhibits a >10-fold in vivo potency enhancement over the lead nitrile 1 and has acceptable oral bioavailability in rats and dogs. An enantiospecific synthesis of 1H-tetrazole-1-alkanenitrile nitriles 9 has been developed.
A convenient synthesis of 3-arylbutanolides and 3-arylbutenolides
Gu, Jian-Xin,Holland, Herbert L.
, p. 3305 - 3315 (2007/10/03)
A series of 3-aryl-substituted butenolides and butanolides has been prepared in a common short synthetic sequence from the corresponding aryl aldehydes. The 3-arylbutanolides are prepared by cyclisation of 3-aryl-3- cyano-1-propanols, obtained by selectiv
Total synthesis of the spermidine alkaloid (+)-(9S,13S)-isocyclocelabenzine
Schultz, Katja,Hesse, Manfred
, p. 14189 - 14198 (2007/10/03)
An asymmetric synthesis of the spermidine alkaliod (+)-isocyclocelabenzine (1a) is reported using (3S)-3-amino-3-phenylpropanoic acid as the chiral building block. The 1,2,3,4-tetrahydroisoquinolin-1-one fragment 9 was synthesized by a modified Bischler-Napieralski reaction. The resulting C(13)-epimers were separated by semi-preparative HPLC. The relative configuratoin of the naturally occurring alkaloid was determined by an X-ray crystal structure analysis, which enabled us to determine the absolute configuration of natural (+)-1a at both chiral centers to be (9S) and (13S).
