Benzoxazin-4-ones as novel, easily accessible inhibitors for rhomboid proteases
نویسندگان
چکیده
منابع مشابه
Novel easily accessible glucosidase inhibitors: 4-hydroxy-5-alkoxy-1,2-cyclohexanedicarboxylic acids.
Glycosidases are very important enzymes involved in a variety of biochemical processes with a special importance to biotechnology, food industry, and pharmacology. Novel structurally simple inhibitors derived from cyclohexane-1,2-dicarboxylic acids were synthesized and tested against several fungal glycosidases from Aspergillus oryzae and Penicilliumcanescens. The presence of at least two carbo...
متن کاملFacile synthesis and herbicidal evaluation of 4H-3,1-benzoxazin-4-ones and 3H-quinazolin-4-ones with 2-phenoxymethyl substituents.
Series of 4H-3,1-benzoxazin-4-ones and 3H-quinazolin-4-ones with phenoxy-methyl substituents were rationally designed and easily synthesized via one-pot N-acylation/ring closure reactions of anthranilic acids with 2-phenoxyacetyl chlorides to yield the 4H-3,1-benzoxazin-4-ones, and subsequently substituted with amino derivatives to obtain the 3H-quinazolin-4-ones. The herbicidal evaluation was ...
متن کاملGeneral and Modular Strategy for Designing Potent, Selective, and Pharmacologically Compliant Inhibitors of Rhomboid Proteases
Rhomboid-family intramembrane proteases regulate important biological processes and have been associated with malaria, cancer, and Parkinson's disease. However, due to the lack of potent, selective, and pharmacologically compliant inhibitors, the wide therapeutic potential of rhomboids is currently untapped. Here, we bridge this gap by discovering that peptidyl α-ketoamides substituted at the k...
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Complexes of 3-[{3-(3'-bromo phenyl)}-prop-2-enoyl]-4-hydroxy-6-methyl-2H-chromen-2-one with Cu(II), Ni(II), Fe(II), Co(II) and Mn(II) have been synthesized and characterized using elemental analysis, IR spectra and conductivity measurements. These studies revealed that they are having octahedral geometry of the type [ML2 (H2O)2]. In-vitro antimicrobial activity of all synthesized compounds and...
متن کاملMicrowave Irradiation Promoted Reactions of Benzoxazin-4-Ones with Primary Amines. Preparation of 4(2=3H)-Quinazolinones
An efficient synthesis of 3-substituted or 2,3-disubstituted 4(3H)-quinazolinones from benzoxazin-4-ones and primary amines under microwave irradiation in unsealed vessels is described.
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ژورنال
عنوان ژورنال: Bioorganic & Medicinal Chemistry Letters
سال: 2018
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2017.12.056