cas 47173-80-8, N-Boc-O-Benzyl-D-serine | Articles data

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Subtype-Specific Agonists for NMDA Receptor Glycine Binding Sites
A series of analogues based on serine as lead structure were designed, and their agonist activities were evaluated at recombinant NMDA receptor subtypes (GluN1/2A-D) using two-electrode voltage-clamp (TEVC) electrophysiology. Pronounced variation in subunit-selectivity, potency, and agonist efficacy was observed in a manner that was dependent on the GluN2 subunit in the NMDA receptor. In particular, compounds 15a and 16a are potent GluN2C-specific superagonists at the GluN1 subunit with agonist efficacies of 398% and 308% compared to glycine. This study demonstrates that subunit-selectivity among glycine site NMDA receptor agonists can be achieved and suggests that glycine-site agonists can be developed as pharmacological tool compounds to study GluN2C-specific effects in NMDA receptor-mediated neurotransmission.
Maolanon, Alex R.,Risgaard, Rune,Wang, Shuang-Yan,Snoep, Yoran,Papangelis, Athanasios,Yi, Feng,Holley, David,Barslund, Anne F.,Svenstrup, Niels,Hansen, Kasper B.,Clausen, Rasmus P.
p. 1681 - 1687
(2017/08/21)

A facile synthesis of the spiroindoline-based growth hormone secretagogue, MK-677
A facile and improved route for the synthesis of the orally active spiroindoline-based growth hormone secretagogue, MK-677 was described. The key step adopted the Fischer indole/reduction strategy. The preparation of the key intermediates N-protected piperidine carboxaldehyde 5 and the N-Boc-O-benzyl-d-serine (2) are also optimized.
Qi, Xian Liang,Yang, Er Qun,Zhang, Jun Tao,Wang, Tao,Cao, Xiao Ping
scheme or table
p. 661 - 664
(2012/07/03)

PYRROLOPYRROLONES ACTIVE AS KINASE INHIBITORS
Compounds represented by formula (I) wherein A, R1, R2, R3, and R4 are as defined in the specification, compositions thereof, and methods of use thereof.
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Page/Page column 33

(2010/11/28)

GROWTH HORMONE SECRETAGOGUES
This invention relates to novel compounds which are useful in the modulation of endogenous growth hormone levels in a mammal. The invention further relates to novel intermediates for use in the synthesis of said compounds, as well as novel processes employed in these syntheses. Also included are methods of treating a mammal which include the administration of said compounds.
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Page/Page column 109

(2010/02/07)

Synthesis and biophysical studies of modified oligonucleotides containing acyclic amino alcohol nucleoside analogs
Novel serine derivative of thymine was prepared and incorporated into oligonucleotides. These modified oligonucleotides were studied for their binding affinity with complementary DNA/RNA.
Ramasamy, Kanda S.,Stoisavljevic, Vesna
p. 1845 - 1861
(2007/10/03)

SPIRO-SUBSTITUTED AZACYCLIC DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS
The present invention relates to compounds of formula (I), wherein n is zero, 1, 2 or 3; R represents C 1-6 alkyl, C 1-6 alkoxy, hydroxy, halogen, cyano, trifluoromethyl SO 2 C 1-6 alkyl, NR. sup.a R b, NR a COR b or CONR a R b, where R a and R b are each H, C 1-4 alkyl, phenyl or trifluoromethyl; R. sup.1 represents phenyl optionally substituted by 1, 2 or 3 of C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-7 cycloalkyl, C 3-7 cycloalkylC 1-4 alkyl,--O(CH 2) p O--(where p is 1 or 2) , halogen, cyano, nitro, trifluoromethyl, trimethylsilyl, OR a, SR. sup.a, SOR a, SO 2 R a, NR a R b, NR a COR b, NR a CO 2 R b, COR a, CO 2 R a or CONR a R. sup.b ; naphthyl; benzhydryl; or benyl, where the naphthyl group or each phenyl moiety of benzyl and benzhydryl may be substituted by C 1-6 alkyl, C 1-6 alkoxy, halogen or trifluoromethyl; R 2 represents hydogen, a substituent as defined for R 1 or heteroaryl selected from indazolyl, thienyl, furanyl, pyridyl, thiazolyl, tetrazolyl and quinolinyl; wherein each heteroaryl may be substituted by C 1-6 alkyl, C 1-6 alkoxy, halogen or trifluoromethyl; R 3 and R 4 are each H or C 1-6 alkyl or R 3 and R 4 together are linked so as to form a C 1-3 alkylene chain; R 5 represents H, C 1-6 alkyl, C 3-7 cycloalkyl, C 3-7 cycloalkylC 1-4 alkyl, phenylC. sub.1-4 alkyl, CO 2 R a, CONR a R b, SOR a or SO 2 R a, wherein the phenyl moiety may be substituted by C. sub.1-6 alkyl, C 1-6 alkoxy, halogen or trifluoromethyl; X and Y are each H, or together represents =O; and Z represents a bond, O, S, SO, SO 2, NR 6, or--(CR 6 R 6)--where R 6 is H or C. sub.1-6 alkyl; or a pharmaceutically acceptable salt thereof. The compounds are of particular use in the treatment or prevention of pain, inflammation, migraine, emesis and postherpetic neuralgia. STR1
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(2008/06/13)

Amino acid nucleic acids: Synthesis and hybridization properties of a novel class of antisense oligonucleotides
Oligonucleotides containing novel phoshoramidite 12 were synthesized and studied for their hybridization properties for the first time. Interestingly, these modified oligonucleotides showed a remarkable resistance to exonuclease.
Ramasamy, Kanda S.,Seifert, Wilfried
p. 1519 - 1522
(2007/10/03)

Synthesis of the orally active spiroindoline-based Growth Hormone Secretagogue, MK-677
The preparation of the Merck Growth Hormone Secretagogue; MK-677 is described. A Fischer indole/reduction based strategy provides the novel spiroindoline nucleus of this potent compound. This optimized sequence necessitates the isolation of only one intermediate 10 and provides MK-677 in 48% overall yield from isonipecotic acid 3.
Maligres, Peter E.,Houpis, Ioannis,Rossen, Kai,Molina, Audrey,Sager, Jess,Upadhyay, Veena,Wells, Kenneth M.,Reamer, Robert A.,Lynch, Joseph E.,Askin, David,Volante,Reider, Paul J.,Houghton, Peter
p. 10983 - 10992
(2007/10/03)