59017-01-5Relevant academic research and scientific papers
Synthesis and in vitro bone cell activity of analogues of the cyclohexapeptide dianthin G
Amso, Zaid,Kowalczyk, Renata,Park, Young-Eun,Watson, Maureen,Lin, Jian-Ming,Musson, David S.,Cornish, Jillian,Brimble, Margaret A.
supporting information, p. 6231 - 6243 (2016/07/11)
The cyclohexapeptide natural product dianthin G promotes osteoblast (bone-forming cell) proliferation in vitro at nanomolar concentrations, and is therefore considered a promising candidate for the treatment of osteoporosis. An Nα-methyl amide bond scan of dianthin G was performed to probe the effect of modifying amide bonds on osteoblast proliferation. In addition, to provide greater structural diversity, a series of dicarba dianthin G analogues was synthesised using ring closing metathesis. Dianthin G and one novel dicarba analogue increased the number of human osteoblasts and importantly they did not increase osteoclast (bone-resorbing cell) differentiation in bone marrow cells.
Linear and cyclic dipeptides with antimalarial activity
Perez-Picaso, Lemuel,Rios, Maria Yolanda,Olivo, Horacio F.,Argotte-Ramos, Rocio,Rodriguez-Gutierrez, Maria
, p. 7048 - 7051,4 (2012/12/12)
Several natural and synthetic polypeptides possess important antimalarial activity. Shorter peptides with potent antimalarial activity have also been described, among them linear di-, tri-, tetra- and pentapeptides and their cyclic analogs. In an attempt
Efficient microwave assisted syntheses of 2,5-diketopiperazines in aqueous media
Perez-Picaso, Lemuel,Escalante, Jaime,Olivo, Horacio F.,Rios, Maria Yolanda
experimental part, p. 2836 - 2849 (2009/12/06)
Aqueous in situ one-pot N-Boc-deprotection-cyclization of Nα-Boc-dipeptidyltert-butyl and methyl esters under microwave irradiation afforded 2,5-diketopiperazines (DKPs) in excellent yields. This protocol is rapid, safe, environmentally friendly, and high
Acid-promoted reactions in 1-hydroxy, 1-dimethylaminomethyl and 1-methylene-4-arylmethyl-2,4-dihydro-1H-pyrazino[2,1-b]quinazoline-3,6-diones
Heredia, María Luisa,De la Cuesta, Elena,Avenda?o, Carmen
, p. 6163 - 6170 (2007/10/03)
The 1-dimethylaminomethyl or 1-methylene group of the title compounds was introduced through a Mannich or a tandem of Mannich-Hofmann reactions as the final step of a protocol that is shorter than other previously described for these precursors of N-acyliminium species. In these compounds, the acid-promoted intramolecular cyclizations of Pictet-Spengler-type were restricted to the N(2)-unsubstituted compounds, while their N(2)-methyl substituted analogues gave instead dimerization products. The cyclization was effective with 1-hydroxy-1,2-disubstituted compounds, which were obtained through addition of a Grignard reagent to 2H,4H-pyrazino[2,1-b]quinazoline-1,3,6-triones.
