Category: 72002-30-3

Hashimoto, Tadashi published the artcileSyntheses and biological activities of substance P analogs containing L– and D-homoglutamine and L– and D-pyrohomoglutamic acid at positions 5 and 6, HPLC of Formula: 72002-30-3, the publication is Bulletin of the Chemical Society of Japan (1987), 60(3), 1207-9, database is CAplus.

Six title substance P (SP) analogs were prepared by the solid-phase method on a benzylhydrylamine resin. The smooth muscle contractile activities of these analogs were compared with the activity of SP on isolated guinea pig ileum and trachea. The potency of [D-Hgn⁵,Hgn⁶]-SP (Hgn = homoglutamine residue) was as high as that of SP in the guinea pig ileum assay. The replacements of both Gln residues at positions 5 and 6 with the Hgn-D-Hgn sequence brought a drastic decrease in activity. The D-pyroHgu-Hgn-Phe-Phe-Gly-Leu-Met-NH₂ (pyroHgu = pyrohomoglutamic acid) analog possessed the highest potency among the 6 analogs.

Bulletin of the Chemical Society of Japan published new progress about 72002-30-3. 72002-30-3 belongs to piperidines, auxiliary class Piperidine,Chiral,Carboxylic acid,Amide, name is (R)-6-Oxopiperidine-2-carboxylic acid, and the molecular formula is C6H9NO3, HPLC of Formula: 72002-30-3.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Sklavounos, Constantine published the artcileD-α-Aminoadipic acid from cephalosporin C, Computed Properties of 72002-30-3, the publication is Organic Preparations and Procedures International (1984), 16(3-4), 165-9, database is CAplus.

The title compound (I) ([α]_D²⁵ = -25.7°, 2% 6N HCl) was prepared by deacylating cephalosporin C via the imino chloride and imino ether to give Me D-α-aminoadipate which was converted to lactam by treatment of base, crystallized, and hydrolyzed to I.

Organic Preparations and Procedures International published new progress about 72002-30-3. 72002-30-3 belongs to piperidines, auxiliary class Piperidine,Chiral,Carboxylic acid,Amide, name is (R)-6-Oxopiperidine-2-carboxylic acid, and the molecular formula is C11H8O3, Computed Properties of 72002-30-3.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Mitchell, Robin E. published the artcileSynthesis of amino acid conjugates to 2-imino-3-methylene-5-carboxypyrrolidine and 2-imino-3-methylene-6-carboxypiperidine, Recommanded Product: (R)-6-Oxopiperidine-2-carboxylic acid, the publication is Bioorganic & Medicinal Chemistry Letters (2010), 20(6), 1910-1912, database is CAplus and MEDLINE.

The four stereomers of 2-imino-3-methylene-5-(carboxy-L-valyl)pyrrolidine, a bacterial metabolite that is inhibitory to the fire blight bacterium Erwinia amylovora, were synthesized and compared for antibacterial activity. Several alternative amino acid conjugates with L,L-stereochem. were also prepared, and the synthesis was extended to 3-methylenepiperidine-6-L-carboxylic acid and a selection of 2-imino-3-methylenepiperidine-6-L-carboxy-L-amino acid conjugates. All synthetic amino acid conjugates (L,L-stereomers) were inhibitory to the growth of E. amylovora. The likely participation of the conjugated iminomethylene moiety as a Michael acceptor is implicated.

Bioorganic & Medicinal Chemistry Letters published new progress about 72002-30-3. 72002-30-3 belongs to piperidines, auxiliary class Piperidine,Chiral,Carboxylic acid,Amide, name is (R)-6-Oxopiperidine-2-carboxylic acid, and the molecular formula is C6H9NO3, Recommanded Product: (R)-6-Oxopiperidine-2-carboxylic acid.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Giannini, Giuseppe published the artcileST7612AA1, a Thioacetate-ω(γ-lactam carboxamide) Derivative Selected from a Novel Generation of Oral HDAC Inhibitors, Quality Control of 72002-30-3, the publication is Journal of Medicinal Chemistry (2014), 57(20), 8358-8377, database is CAplus and MEDLINE.

A systematic study of medicinal chem. aimed at identifying a new generation of HDAC inhibitors, through the introduction of a thiol zinc-binding group and of an amide-lactam in the ω-position of the polyethylene chain of the vorinostat scaffold, allowed the selection of a new class of potent pan-HDAC inhibitors (pan-HDACis). Simple, highly versatile, and efficient synthetic approaches were used to synthesize a library of these new derivatives, which were then submitted to a screening for HDAC inhibition as well as to a preliminary in vitro assessment of their antiproliferative activity. Mol. docking into HDAC crystal structures suggested a binding mode for these thiol derivatives consistent with the stereoselectivity observed upon insertion of amide-lactam substituents in the ω-position. ST7612AA1 I, selected as a drug candidate for further development, showed an in vitro activity in the nanomolar range associated with a remarkable in vivo antitumor activity, highly competitive with the most potent HDAC inhibitors, currently under clin. trials. A preliminary study of PK and metabolism is also illustrated.

Journal of Medicinal Chemistry published new progress about 72002-30-3. 72002-30-3 belongs to piperidines, auxiliary class Piperidine,Chiral,Carboxylic acid,Amide, name is (R)-6-Oxopiperidine-2-carboxylic acid, and the molecular formula is C6H9NO3, Quality Control of 72002-30-3.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem