Category: 161370-66-7

Teno, Naoki published the artcileSynthesis and evaluation of tripeptidic plasmin inhibitors with nitrile as warhead, Category: iodides-buliding-blocks, the publication is Journal of Peptide Science (2012), 18(10), 620-625, database is CAplus and MEDLINE.

Plasmin is best known as the key mol. in the fibrinolytic system, which is critical for clot lysis and can initiate matrix metalloproteinase (MMP) activation cascade. Along with MMP, plasmin is suggested to be involved in physiol. processes that are linked to the risk of carcinoma formation. Plasmin inhibitors could be perceived as a promising new principle in the treatment of diseases triggered by plasmin. On the basis of the peptidic sequence derived from the synthetic plasmin substrate, a series of peptidic plasmin inhibitors possessing nitrile as warhead were prepared and evaluated for their inhibitory activities against plasmin and other serine proteases, plasma kallikrein and urokinase. The most potent peptidic inhibitors with the nitrile warhead exhibit potency toward plasmin (IC₅₀ = 7.7-11 μM) and are characterized by their selectivity profile against plasma kallikrein and urokinase. The results and mol. modeling of the peptidic inhibitor complexed with plasmin reveal that the P2 residue makes favorable contacts with the open binding pocket comprising the S2 and S3 subsites of plasmin.

Journal of Peptide Science published new progress about 161370-66-7. 161370-66-7 belongs to iodides-buliding-blocks, auxiliary class Chiral,Iodide,Amine,Aliphatic hydrocarbon chain,Ester,Amide, name is (S)-tert-Butyl 2-((tert-butoxycarbonyl)amino)-4-iodobutanoate, and the molecular formula is C12H14O2, Category: iodides-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Iodide,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Qu, Wenchao published the artcilePreparation and characterization of L-[5-¹¹C]-glutamine for metabolic imaging of tumors, Application In Synthesis of 161370-66-7, the publication is Journal of Nuclear Medicine (2012), 53(1), 98-105, database is CAplus and MEDLINE.

Recently, there has been a renewed interest in the study of tumor metabolism above and beyond the Warburg effect. Studies on cancer cell metabolism have provided evidence that tumor-specific activation of signaling pathways, such as the upregulation of the oncogene myc, can regulate glutamine uptake and its metabolism through glutaminolysis to provide the cancer cell with a replacement of energy source. Methods: We report a convenient procedure to prepare L-[5-¹¹C]-glutamine. The tracer was evaluated in 9L and SF188 tumor cells (glioma and astrocytoma cell lines). The biodistribution of L-[5-¹¹C]-glutamine in rodent tumor models was investigated by dissection and PET. Results: By reacting ¹¹C-cyanide ion with protected 4-iodo-2-amino-butanoic ester, the key intermediate was obtained in good yield. After hydrolysis with trifluoroacetic and sulfonic acids, the desired optically pure L-[5-¹¹C]-glutamine was obtained (radiochem. yield, 5% at the end of synthesis; radiochem. purity, >95%). Tumor cell uptake studies showed maximum uptake of L-[5-¹¹C]-glutamine reached 17.9% and 22.5% per 100 μg of protein, resp., at 60 min in 9L and SF188 tumor cells. At 30 min after incubation, more than 30% of the activity appeared to be incorporated into cellular protein. Biodistribution in normal mice showed that L-[5-¹¹C]-glutamine had significant pancreas uptake (7.37 percentage injected dose per g at 15 min), most likely due to the exocrine function and high protein turnover within the pancreas. Heart uptake was rapid, and there was 3.34 percentage injected dose per g remaining at 60 min after injection. Dynamic small-animal PET studies in rats bearing xenografted 9L tumors and in transgenic mice bearing spontaneous mammary gland tumors showed a prominent tumor uptake and retention. Conclusion: The data demonstrated that this tracer was favorably taken up in the tumor models. The results suggest that L-[5-¹¹C]-glutamine might be useful for probing in vivo tumor metabolism in glutaminolytic tumors.

Journal of Nuclear Medicine published new progress about 161370-66-7. 161370-66-7 belongs to iodides-buliding-blocks, auxiliary class Chiral,Iodide,Amine,Aliphatic hydrocarbon chain,Ester,Amide, name is (S)-tert-Butyl 2-((tert-butoxycarbonyl)amino)-4-iodobutanoate, and the molecular formula is C13H24INO4, Application In Synthesis of 161370-66-7.

Referemce:
https://en.wikipedia.org/wiki/Iodide,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Clausen, Rasmus P. published the artcileThe Glutamate Receptor GluR5 Agonist (S)-2-Amino-3-(3-hydroxy-7,8-dihydro-6H-cyclohepta[d]isoxazol-4-yl)propionic Acid and the 8-Methyl Analogue: Synthesis, Molecular Pharmacology, and Biostructural Characterization, HPLC of Formula: 161370-66-7, the publication is Journal of Medicinal Chemistry (2009), 52(15), 4911-4922, database is CAplus and MEDLINE.

The design, synthesis, and pharmacol. characterization of a highly potent and selective glutamate GluR5 agonist is reported. (S)-2-Amino-3-((RS)-3-hydroxy-8-methyl-7,8-dihydro-6H-cyclohepta[d]isoxazol-4-yl)propionic acid (I) is the 8-Me analog of (S)-2-amino-3-(3-hydroxy-7,8-dihydro-6H-cyclohepta[d]isoxazol-4-yl)propionic acid (II). I displays an improved selectivity profile compared to II. A versatile stereoselective synthetic route for this class of compounds is presented along with the characterization of the binding affinity of I to ionotropic glutamate receptors (iGluRs). Functional characterization of I at cloned iGluRs using a calcium imaging assay and voltage-clamp recordings show a different activation of GluR5 compared to (S)-glutamic acid, kainic acid, and (S)-2-amino-3-(3-hydroxy-5-tert-butyl-4-isoxazolyl)propionic acid as previously demonstrated for II. An X-ray crystallog. anal. of II and computational analyses of II and I bound to the GluR5 agonist binding domain (ABD) are presented, including a watermap anal., which suggests that water mols. in the agonist binding site are important selectivity determinants.

Journal of Medicinal Chemistry published new progress about 161370-66-7. 161370-66-7 belongs to iodides-buliding-blocks, auxiliary class Chiral,Iodide,Amine,Aliphatic hydrocarbon chain,Ester,Amide, name is (S)-tert-Butyl 2-((tert-butoxycarbonyl)amino)-4-iodobutanoate, and the molecular formula is C13H24INO4, HPLC of Formula: 161370-66-7.

Referemce:
https://en.wikipedia.org/wiki/Iodide,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com