103127-53-3Relevant articles and documents
Fluorinated Olefinic Lactams: The Case of Amino Acids - Preparation and Mechanistic Studies
Bartoszak-Adamska, El?bieta,Go?dyn, Mateusz,Koroniak, Henryk,Koroniak-Szejn, Katarzyna,Salamon-Krokosz, Katarzyna,Siod?a, Tomasz
, (2022/03/17)
Herein, we report the synthesis of analogues of amino acids with a monofluorovinyl moiety. Interestingly, we have found that cyclization of the obtained products proceeds easily in all cases. The cyclization process has not previously been observed at this reaction stage, and such fluorinated lactams derived from phenylalanine, valine, alanine have not been described before.
METHODS OF TREATING LIVER FIBROSIS USING CALPAIN INHIBITORS
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Paragraph 0342, (2020/01/24)
Disclosed herein are methods of treating liver fibrosis by administering calpain inhibitors to subjects in need thereof.
CALPAIN MODULATORS AND THERAPEUTIC USES THEREOF
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Paragraph 0398, (2019/10/23)
Small molecule calpain modulator compounds, including their pharmaceutically acceptable salts, can be included in pharmaceutical compositions. The compounds can be useful in inhibiting calpain, or competitive binding with calpastatin, by contacting them with CAPN1, CAPN2, and/or CAPN9 enzymes residing inside a subject. The compounds and composition can also be administered to a subject in order to treat a fibrotic disease or a secondary disease state or condition of a fibrotic disease.
Membrane-active antimicrobial poly(amino-modified alkyl) β-cyclodextrins synthesized: Via click reactions
Yamamura, Hatsuo,Nonaka, Miho,Okuno, Shingo,Mitsuhashi, Ryogo,Kato, Hisato,Katsu, Takashi,Masuda, Kazufumi,Tanimoto, Koichi,Tomita, Haruyoshi,Miyagawa, Atsushi
, p. 509 - 518 (2018/03/26)
The emergence of drug-resistant bacteria has led to the high demand for new antibiotics. In this report, we investigated membrane-active antimicrobial β-cyclodextrins. These contain seven amino-modified alkyl groups on a molecule, which act as functional
A rapid and efficient one-pot method for the reduction of N-protected α-amino acids to chiral α-amino aldehydes using CDI/DIBAL-H
Ivkovic, Jakov,Lembacher-Fadum, Christian,Breinbauer, Rolf
supporting information, p. 10456 - 10460 (2015/11/10)
N-Protected amino acids can be easily converted into chiral α-amino aldehydes in a one-pot reaction by activation with CDI followed by reduction with DIBAL-H. This method delivers Boc-, Cbz- and Fmoc-protected amino aldehydes from proteinogenic amino acids in very good isolated yields and complete stereointegrity.
Synthesis of proline analogues as potent and selective cathepsin S inhibitors
Kim, Mira,Jeon, Jiyoung,Song, Jiyeon,Suh, Kwee Hyun,Kim, Young Hoon,Min, Kyung Hoon,Lee, Kwang-Ok
, p. 3140 - 3144 (2013/06/26)
Cathepsin S is a potential target of autoimmune disease. A series of proline derived compounds were synthesized and evaluated as cathepsin S inhibitors. We discovered potent cathepsin S inhibitors through structure-activity relationship studies of proline analogues. In particular, compound 19-(S) showed promising in vitro/vivo pharmacological activities and properties as a selective cathepsin S inhibitor.
Synthesis and cytotoxicity evaluation of diastereoisomers and N-terminal analogues of tubulysin-U
Shankar, P. Sreejith,Bigotti, Serena,Lazzari, Paolo,Manca, Ilaria,Spiga, Marco,Sani, Monica,Zanda, Matteo
, p. 6137 - 6141 (2013/10/22)
Tubulysins are potent anti-mitotic natural compounds and a scalable and efficient synthetic route for generation of its analogues has been developed and extended to the synthesis of diastereoisomers and N-terminal analogues of tubulysin-U. Structure-activ
HETEROCYCLIC AMIDE COMPOUNDS AND PHARMACEUTICAL USE OF THE SAME
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, (2008/06/13)
Heterocyclic amide compounds of the formula (I) STR1 wherein each symbol is as defined in the specification, pharmacologically acceptable salts thereof, pharmaceutical compositions thereof and pharmaceutical use thereof. The heterocyclic amide compounds and pharmacologically acceptable salts thereof of the present invention have superior inhibitory activity against chymase groups in mammals inclusive of human, and can be administered orally or parenterally. Therefore, they are useful as chymase inhibitors and can be effective for the prophylaxis and treatment of various diseases caused by chymase, such as those caused by angiotensin II.
Synthesis and Stereoselective Reactions of 2-(Pyrrol-1-yl)alkanals and 2-(pyrrol-1-yl)alkan-1-ones
Kashima, Choji,Maruyama, Tatsuya,Fujioka, Yoko,Harada, Kazuo
, p. 1041 - 1046 (2007/10/02)
2-(2,5-Dimethylpyrrol-1-yl)alkanals, 2-(pyrrol-1-yl)alkanals, and 2-(2,5-dimethylpyrrol-1-yl)alkan-1-ones were prepared.The reactions of these compounds with Grignard and hydride reagents proceeded stereoselectively to give the corresponding 2-(pyrrol-1-yl)alcohols, which were converted into 2-aminoalcohols, such as norephedrine and ephedrine, by cleavage of the pyrrole ring.