141108-78-3Relevant academic research and scientific papers
Thiazolidin-5-imine Formation as a Catalyst-Free Bioorthogonal Reaction for Protein and Live Cell Labeling
Bi, Xiaobao,Yin, Juan,Rao, Chang,Balamkundu, Seetharamsing,Banerjee, Biplab,Zhang, Dingpeng,Zhang, Dawei,Dedon, Peter C.,Liu, Chuan-Fa
supporting information, p. 7790 - 7793 (2019/01/14)
A previously undescribed reaction involving the formation of a thiazolidin-5-imine linkage was developed for bioconjugation. Being highly specific and operating in aqueous media, this simple condensation reaction is used to chemoselectively label peptides, proteins, and living cells under physiological conditions without the need to use toxic catalysts or reducing reagents.
DIAMINE CROSSLINKING AGENTS, CROSSLINKED ACIDIC POLYSACCHARIDES AND MEDICAL MATERIALS
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Paragraph 0387-0391, (2017/01/26)
The invention provides a diamine crosslinking agent for acidic polysaccharides consisting of a diamine compound having a primary amino group at both terminals and an ester or thioester bond in the molecule, wherein the number of atom in the linear chain between at least one of the amino groups and the carbonyl carbon in the ester or thioester is 1 to 5; in particular, a diamine crosslinking agent for acidic polysaccharides which is represented by the general formula (I) below: [the symbols in the formula are as described in the specification]; a crosslinked acidic polysaccharide obtained by forming crosslinks by amide bonding between the amino groups in the diamine crosslinking agent and carboxyl groups in an acidic polysaccharide; and a medical material including the crosslinked product.
Development of dual-acting agents for thromboxane receptor antagonism and thromboxane synthase inhibition. 3. Synthesis and biological activities of oxazolecarboxamide-substituted ω-phenyl-ω-(3-pyridyl)alkenoic acid derivatives and related compounds
Takeuchi, Kumiko,Kohn, Todd J.,True, Timothy A.,Mais, Dale E.,Wikel, James H.,Utterback, Barbara G.,Wyss, Virginia L.,Jakubowski, Joseph A.
, p. 5362 - 5374 (2007/10/03)
A novel series of oxazolecarboxamide-substituted ω-phenyl-ω-(3- pyridyl)alkenoic acid derivatives was discovered as potent dual-acting agents to block the TXA2 receptor and to inhibit the thromboxane synthase (TRA/TSI). Synthesis, structure-activity relationship (SAR), and in vitro and in vivo pharmacology of this series of compounds are described. Modification of the series revolved around the oxazole moiety to increase the hydrophilicity of the compounds and to correlate the biological activity with lipophilicity of the compounds. The most potent in the series was (E)-7-[4- [4-[[(4-cyclohexylbutyl)amino]carbonyl]-2-oxazolyl]phenyl]-7-(3-pyridyl)hept- 6-enoic acid (14) with K(d) = 9.9 ± 0.4 nM for the thromboxane receptor antagonism and IC50 = 55.0 ± 17.9 nM for thromboxane synthase inhibition. The compound 14 was a selective TRA/TSI which exhibited desirable characteristics for oral activity, 'shunt' effect to elevate PGI2 level, and absence of agonist activity.
Synthesis and analgesic activity of new dermorphin analogues
Naqvi, T.,Dhawan, V. C.,Haq, W.,Raghubir, R.,Patnaik, G. K.,et al.
, p. 445 - 450 (2007/10/02)
Synthesis and analgesic activity of five new heptapeptides structurally related to dermorphin (DM): Tyr-D-Ala-Phe-Gly-Tyr-Pro-Ser-NH.C3H7(i) (21), Tyr-D-Ala-Phe-Gly-Tyr-Pro-Gly-NH.C3H7(i) (22), Tyr-D-Ala-Phe-Gly-Tyr-Pro-Ser-NH.CH2.C6H5 (23), Tyr-D-Ala-Phe
