103678-36-0Relevant articles and documents
Novel highly selective inhibitors of ubiquitin specific protease 30 (USP30) accelerate mitophagy
Kluge, Arthur F.,Lagu, Bharat R.,Maiti, Pranab,Jaleel, Mahaboobi,Webb, Michael,Malhotra, Jyoti,Mallat, Ashley,Srinivas, P. Akhila,Thompson, James E.
, p. 2655 - 2659 (2018)
Mitophagy is one of the processes that cells use to maintain overall health. An E3 ligase, parkin, ubiquitinates mitochondrial proteins prior to their degradation by autophagasomes. USP30 is an enzyme that de-ubiquitinates mitochondrial proteins; therefore, inhibiting this enzyme could foster mitophagy. Herein, we disclose the structure–activity relationships (SAR) within a novel series of highly selective USP30 inhibitors. Two structurally similar compounds, MF-094 (a potent and selective USP30 inhibitor) and MF-095 (a significantly less potent USP30 inhibitor), serve as useful controls for biological evaluation. We show that MF-094 increases protein ubiquitination and accelerates mitophagy.
USP30 INHIBITORS
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Page/Page column 22, (2018/12/13)
The application relates to phenyl- or naphthylsulfonamide derivatives of the structural formula (I). The compounds are described as inhibitors of USP30 (ubiquitin specific peptidase 30) useful for the treatment of conditions involving mitochondrial defects including neurodegenerative diseases such as Alzheimer's and Parkinson's or a neoplastic disease such as leukemia.
Alpha-amino acrylate microbicide and preparation method and application thereof
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, (2017/10/13)
The invention provides an alpha-amino acrylate microbicide and a preparation method and application thereof. The alpha-amino acrylate microbicide has a specific chemical structure formula shown as a formula I, and the formula I is shown in the description. The alpha-amino acrylate microbicide has the advantages that by utilizing the design principle of pesticide molecules, a medical leading compound with anti-coronavirus activity is performed with structure modification of agricultural plant virus-resisting activity, a series of alpha-amino acrylate derivatives is designed and synthesized, and particularly, the alpha-amino acrylate derivative containing piperidine ring is synthesized; the known compound is used as a positive reference compound to systematically screen the biology activity; a plurality of high-efficiency anti-virus leading molecules are provided for the developing of new pesticides, and the positive meaning is realized for the reduction application of the pesticide and the protection of environment ecology.
An improved method of amide synthesis using acyl chlorides
Zhang, Li,Wang, Xiao-jun,Wang, Jing,Grinberg, Nelu,Krishnamurthy, DhileepKumar,Senanayake, Chris H.
supporting information; experimental part, p. 2964 - 2966 (2009/08/07)
A simple, mild and highly efficient condition for amide synthesis from acyl chlorides has been developed to minimize hydrolysis, racemization and other side reactions. This method should expand capabilities in the peptide coupling area.
DIOXACYCLOALKANE COMPOUND HAVING RENIN-INHIBITORY ACTIVITY
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, (2008/06/13)
Dioxacycloalkane compounds of the formula [1] STR1 wherein A is STR2 wherein W is STR3 X is--CO--or--SO 2--; Y is--CH. sub.2--,--O--or--NR 25--; and R 1 is an aralkyl which may be substituted by lower alkoxy;R 2 is a hydrogen atom or a lower alkyl;R 3 is--(CH 2)d-SR 26 or STR4 R. sup.4 and R 5 are each a hydrogen atom or a lower alkyl; and E is--C(R. sup.29)(R 30)--or--CH 2 CH 2--, pharmaceutically acceptable salts thereof, intermediates for producing said compounds, and methods for producing said intermediates. The compounds of the formula [1] have a strong inhibitory activity against renin and show continuous hypotensive action by oral administration. They are useful as hypotensive agents or therapeutic agents for heart failure.
N-Acylated α-Amino Acids as Novel Oral Delivery Agents for Proteins
Leone-Bay, Andrea,Santiago, Noemi,Achan, Douglas,Chaudhary, Kiran,DeMorin, Frenel,et al.
, p. 4263 - 4269 (2007/10/03)
A series of N-acylated α-amino acids were synthesized and shown to improve the oral delivery of two protein drugs, salmon calcitonin (sCT) and interferon-α.Forty-five compounds in this series were tested in vivo in rats and primates.A significant positive
The Alkylation of Menthyl Hippurate and Some Related Materials: A Reinvestigation.
McIntosh, John M.,Thangarasa, Rasiah,Foley, Nancy K.,Ager, David J.,Froen, Diane E.,Klix, Russell C.
, p. 1967 - 1974 (2007/10/02)
Benzylation of chiral esters of N-acyglycines using various bases and additives was examined.No C-alkylation was observed with one equivalent of base.Diastereoselectivities were dependent on the amount of additive, the nature of the N-acyl group, and the chiral ester.A model to account for the degree and sense of the stereoselectivity is proposed.
