Efficient discrimination of natural stereoisomers of chicoric acid, an HIV-1 integrase inhibitor
نویسندگان
چکیده
منابع مشابه
Chicoric acid analogues as HIV-1 integrase inhibitors.
The present study was undertaken to examine structural features of L-chicoric acid (3) which are important for potency against purified HIV-1 integrase and for reported cytoprotective effects in cell-based systems. Through a progressive series of analogues, it was shown that enantiomeric D-chicoric acid (4) retains inhibitory potency against purified integrase equal to its L-counterpart and fur...
متن کاملHuman immunodeficiency virus type 1 (HIV-1) integrase: resistance to diketo acid integrase inhibitors impairs HIV-1 replication and integration and confers cross-resistance to L-chicoric acid.
The diketo acids are potent inhibitors of human immunodeficiency virus (HIV) integrase (IN). Mutations in IN, T66I, S153Y, and M154I, as well as T66I-S153Y and T66I-M154I double mutations, confer resistance to diketo acids (D. J. Hazuda et al., Science 287:646-650, 2000). The effects of these IN mutations on viral replication, enzymatic activity, and susceptibility to other HIV inhibitors are r...
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BACKGROUND Two inhibitors of the HIV-1 integrase enzyme (INIs) are in late stage clinical development. To date, approximately 42 mutations within the HIV-1 integrase (IN) gene have been associated with INI drug resistance. Naturally occurring IN gene polymorphisms may have important implications for INI development. In this study, we evaluated clinical HIV-1 strains from INI-naive patients to d...
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Enantioselective total synthesis of the recently isolated, novel polyketide natural product (+)-integrasone has been accomplished from the readily available Diels-Alder adduct of cyclopentadiene and p-benzoquinone. An enzymatically desymmetrized epoxyquinone building block has been elaborated through a series of regio- , chemo- and stereocontrolled steps to the final bicyclic framework of the n...
متن کاملNatural Kaolin supported sulfuric acid as an efficient catalyst for the preparation of 1, 1-diacetates under solvent-free conditions
A facile and efficient method for the preparation of 1,1-diacetates of aldehydes is improved. The acidified kaolin with sulfuric acid (2 % w/w) catalyzed 1,1-diacetates formation from aldehydes in solvent-free conditions. Both aromatic and aliphatic aldehydes gave high yields (85-95 %) of the corresponding 1, 1-diacetates. Advantages of this method are the use of inexpensive and selective catal...
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ژورنال
عنوان ژورنال: Journal of Photochemistry and Photobiology B: Biology
سال: 2018
ISSN: 1011-1344
DOI: 10.1016/j.jphotobiol.2018.10.025