3770-22-7Relevant academic research and scientific papers
INHIBITORS OF HISTONE DEACETYLASE USEFUL FOR THE TREATMENT OR PREVENTION OF HIV INFECTION
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Page/Page column 31, (2020/02/23)
The present invention relates to Compounds of Formula (I): Formula (I) and pharmaceutically acceptable salts or prodrug thereof, wherein R1, R2, R3, Ra, Rb, A and B are as defined herein. The present invention also relates to compositions comprising at least one compound of Formula (I), and methods of using the compounds of Formula (I) for treating or preventing HIV infection in a subject.
Does the Exception Prove the Rule? A Comparative Study of Supramolecular Synthons in a Series of Lactam Esters
Weck,Nauha,Gruber
, p. 2899 - 2911 (2019/05/10)
In this paper a series of simple lactam esters and carboxylic acids is studied with respect to their overall conformation and hydrogen bonding patterns. In total, eight lactams featuring Nα-substitution have been synthesized. Additionally, the molecular structures of related lactam esters have been considered. The length of the amide bonds does not seem to be majorly influenced by different substituents unless the electron withdrawing N-Boc-protection group is introduced, resulting in a higher susceptibility toward hydrolytic ring opening. As known from other lactams, the Nα ester moiety of the title compounds can be in an axial or equatorial conformation. Smaller ester groups were found to prefer equatorial positions, while larger ones occupy axial sites. N-substitution seems to promote axial conformations of the respective Nα group, with enantholactams being the only studied exception. In addition to the two common amide packing motifs, i.e., the R2 2 (8) amide dimer (NH···O/NH···O) and the C(4) amide chain, a third graph-set was found: the R2 2(8) NH···O/CH···O=C heterodimer. In general, there seems to be a tendency for medium-sized lactams as well as lactams with small esters to form R2 2 (8) amide dimers. Larger esters and enantholactam esters lead to C(4) amide chains. In this respect the formation of R2 2(8) N - H···O/C-H···O=C heterodimers should be seen as a remarkable exception.
An Efficient Two-Step Preparation of α-, β-, γ- or δ-Amino Acids from 2-Pyrazinones, 2-Hydroxypyrimidines or 2-Pyridones Respectively
Zacharie, Boulos,Abbott, Shaun D.,Baigent, Christopher B.,Doyle, Christopher,Yalagala, Ravi Shekar
, p. 6486 - 6493 (2018/11/23)
A practical and efficient two-step procedure is reported for the preparation of a variety of α-, β-, γ- and δ-amino acids from 2-pyridone, 2-pyrazinone or 2-hydroxypyrimidine and derivatives. The procedure is amenable to scale-up and in most cases no chromatographic purification of the product is required. This approach is useful, especially in the synthesis of amino acids or deuterated amino acids that are not obtained by other methods.
Lactams as prostanoid receptor ligands. Part 4: 2-Piperidones as selective EP4 receptor agonists
Elworthy, Todd R.,Brill, Emma R.,Caires, Christopher C.,Kim, Woongki,Lach, Leang K.,Tracy, Jahari Laurant,Chiou, San-San
, p. 2523 - 2526 (2007/10/03)
2-Piperidones were prepared bearing heptanoic acid or a thioether heptanoic acid at the 1-position as well as appropriately substituted at the 6-position to mimic the structure of prostaglandins. The stereochemical purity at the 6-position was determined to be ≥95% ee for an advanced synthetic intermediate. The 2-piperidones were identified as potent agonists at the EP4 prostanoid receptor. They displayed a high affinity (K i 5-130 nM) at EP4 and subtype selectivity.
