157528-56-8Relevant articles and documents
Development of a Dual-Acting Antibacterial Agent (TNP-2092) for the Treatment of Persistent Bacterial Infections
Ma, Zhenkun,Lynch, Anthony Simon
, p. 6645 - 6657 (2016/08/05)
The clinical management of prosthetic joint infections and other persistent bacterial infections represents a major unmet medical need. The rifamycins are one of the most potent antibiotic classes against persistent bacterial infections, but bacteria can
The design and discovery of novel amide CCR5 antagonists
Pryde, David C.,Corless, Martin,Fenwick, David R.,Mason, Helen J.,Stammen, Blanda C.,Stephenson, Peter T.,Ellis, David,Bachelor, David,Gordon, David,Barber, Christopher G.,Wood, Anthony,Middleton, Donald S.,Blakemore, David C.,Parsons, Gemma C.,Eastwood, Rachel,Platts, Michelle Y.,Statham, Keith,Paradowski, Kerry A.,Burt, Catherine,Klute, Wolfgang
supporting information; scheme or table, p. 1084 - 1088 (2009/08/07)
The synthesis of a range of novel amine-containing structures and their primary potency as inhibitors of HIV-1 fusion via blocking of the CCR5 receptor is described. The development of the medicinal chemistry strategy and SAR's which led to the identification of the piperidine amide compounds 33 and 36 as excellent leads for further evaluation is described, along with key physicochemical data which highlighted their lead potential.
8-METHOXY-9H-ISOTHIAZOLO[5,4-B]QUINOLINE-3,4-DIONES AND RELATED COMPOUNDS AS ANTI-INFECTIVE AGENTS
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Page/Page column 70-71, (2010/11/25)
The invention provides compound and salts of Formula (I) and (II), disclosed herein, which includes compounds of Formula (A) and Formula (B) such compounds possess useful antimicrobial activity. The variables R2, R3, R5, R
INTERMEDIATES FOR THE PRODUCTION OF OPTICALLY ACTIVE CYCLOPROPYLAMINE DERIVATIVES AND PROCESS FOR THE PRODUCTION OF THE INTERMEDIATES
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Page/Page column 9-10, (2008/06/13)
The present invention provides intermediates needed for production of an optically active compound represented by formula (6), which enable the compound (6) to be readily synthesized in simple production steps without optical resolution, and also provides
QUINOLONE ANTIBACTERIAL AGENTS
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Page/Page column 87; 88; 120, (2010/02/12)
Compounds of formula (I) wherein A is formula (II), formula (III) or formula (IV), and B is formula (V), formula (VI), or formula (VII), can be used in a variety of applications including use as antibacterial agents.
ANTIBACTERIAL AMINOQUINAZOLIDINEDIONE DERIVATIVES
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Page/Page column 115; 116; 148, (2010/02/12)
Compounds of formula (I) wherein: A is Formula (II), Formula (III), or Formula (IV) and B is Formula (V), Formula (VI), or Formula (VII), can be used in a variety of applications including use as antibacterial agents.
A practical ex-chiral-pool synthesis of β-proline and homo-β-proline
Thomas, Christoph,Orecher, Florian,Gmeiner, Peter
, p. 1491 - 1496 (2007/10/03)
Starting from aspartic acid an efficient synthesis of enantiomerically pure β-proline and homo-β-proline is described. The key step of the synthesis includes formation of the 1,4-biselectrophile 6, followed by rearrangement via the aziridinium intermediate 7 and ring closure to give the pyrrolidinium salt 9a which can serve as a common precursor for both target compounds.
An Efficient Method for the Synthesis of (R)-3-(1-Amino-1-methylethyl)pyrrolidines for the Antiinfective Agent, PD 138312
Fedij, Victor,Lenoir, Edward A.,Suto, Mark J.,Zeller, James R.,Wemple, James
, p. 1131 - 1134 (2007/10/02)
Methylcerium dichloride has been found to undergo bis addition to nitriles to produce tertiary carbinamines with retention of optical purity at the ? position.This result is used in the development of a short, economical synthesis of the 1,8-naphthyridine antiinfective agent, PD 138312.
Process for chiral 3-(1-amino-1,1-bisalkylmethyl)-1-substituted-pyrrolidines
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, (2008/06/13)
The process for the preparation of chiral 3-(1-amino-1,1-bisalkylmethyl)-1-substituted-pyrrolidines used as key intermediates for the preparation of naphthyridine and quinolone antibacterial agents which comprises reacting readily available chiral 1-subst