- Amine-Functionalized Polylactide-PEG Copolymers
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The formation of halogenated carboxylic acid intermediate followed by a ring-closing reaction led to amino-functionalized asymmetrical lactide monomer. PEG-based functional diblock and triblock polylactides were synthesized via a controlled ring-opening p
- Arlcan, Mehmet Onur,Erdo?an, Sezgi,Mert, Olcay
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- Buchwald-Hartwig versus Microwave-Assisted Amination of Chloroquinolines: En Route to the Pyoverdin Chromophore
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The reaction of 2-chloro-6,7-dimethoxy-3-nitroquinoline with a series of amines and aminoalkanoates under basic microwave-mediated conditions and under Buchwald-Hartwig amination conditions is reported. The microwave irradiation favored the reaction with amines, resulting in yields of up to 80percent, whereas amino acid functionalization gave yields comparable to those of Buchwald-Hartwig amination. tert-Butyl (2 R)-4-[(6,7-dimethoxy-3-nitroquinolin-2-yl)amino]-2-hydroxybutanoate was successfully cyclized to the pyoverdin chromophore, a subunit of siderophores.
- Altevogt, Luca,Baro, Angelika,Bilitewski, Ursula,Freund, Marcel,Laschat, Sabine,Lin, Yulin,Rudolf, Richard,Seubert, Philipp
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supporting information
p. 1177 - 1181
(2020/07/20)
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- Design of novel antibiotics that bind to the ribosomal acyltransfer site
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The structure of neamine bound to the A site of the bacterial ribosomal RNA was used in the design of novel aminoglycosides. The design took into account stereo and electronic contributions to interactions between RNA and aminoglycosides, as well as a ran
- Haddad, Jalal,Kotra, Lakshmi P.,Llano-Sotelo, Beatriz,Kim, Choonkeun,Azucena Jr., Eduardo F.,Liu, Meizheng,Vakulenko, Sergei B.,Chow, Christine S.,Mobashery, Shahriar
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p. 3229 - 3237
(2007/10/03)
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- Enantioselective Syntheses of (S)- and (R)-3-Hydroxypyrrolidin-2-ones via Lactate Dehydrogenase Catalysed Reductions of 4-Benzyloxycarbonylamino-2-oxobutanoic Acid
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The first examples of the BS- and SE-lactate dehydrogenase catalysed reductions of an α-keto acid incorporating a nitrogen containing function in the side chain are described: (S)- and (R)-benzyloxycarbonylamino-2-hydroxybutanoic acids were prepared in good yield and excellent enantioselectivities and were converted to the (S)- and (R)-3-hydroxypyrrolidin-2-ones respectively.
- Bentley, Jonathan M.,Wadsworth, Harry J.,Willis, Christine L.
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p. 231 - 232
(2007/10/02)
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- 4-O-(2,3,5-Trideoxy-5-amino-α-D-pentofuranosyl)-6-O-aminoglycosyl-1,3-diaminocyclitois, methods for their preparation, pharmaceutical formulations thereof and their use as antibacterial agents
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4-O-(2,3,5-Trideoxy-5-amino-α-D-pentofuranosyl)-6-O-aminoglycosyl-1,3-diaminocyclitols and 1-N-substituted derivatives thereof are described together with methods for their preparation and their use as antibacterial agents. Preferred are 1-N-(ω-amino-α-hydroxyalkanoyl)-[4-O-(2,3,5-trideoxy-5-amino-α-D-pentofuranosyl)-6-O-garosaminyl-2-deoxystreptamines], particularly the 1-N-(S-β-amino-α-hydroxypropionyl) derivatives, which are broad spectrum antibacterial agents.
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