84225-86-5Relevant academic research and scientific papers
Discovery of Cyclic Boronic Acid QPX7728, an Ultrabroad-Spectrum Inhibitor of Serine and Metallo-β-lactamases
Hecker, Scott J.,Reddy, K. Raja,Lomovskaya, Olga,Griffith, David C.,Rubio-Aparicio, Debora,Nelson, Kirk,Tsivkovski, Ruslan,Sun, Dongxu,Sabet, Mojgan,Tarazi, Ziad,Parkinson, Jonathan,Totrov, Maxim,Boyer, Serge H.,Glinka, Tomasz W.,Pemberton, Orville A.,Chen, Yu,Dudley, Michael N.
supporting information, p. 7491 - 7507 (2020/08/21)
Despite major advances in the β-lactamase inhibitor field, certain enzymes remain refractory to inhibition by agents recently introduced. Most important among these are the class B (metallo) enzyme NDM-1 of Enterobacteriaceae and the class D (OXA) enzymes
BORONIC ACID DERIVATIVES AND THERAPEUTIC USES THEREOF
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Paragraph 0184, (2019/11/12)
Disclosed herein are antimicrobial compounds, compositions, pharmaceutical compositions, the use and preparation thereof. Some embodiments relate to boronic acid derivatives and their use a therapeutic agents.
BORONIC ACID DERIVATIVES AND THERAPEUTIC USES THEREOF
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Paragraph 0200, (2018/02/28)
Disclosed herein are antimicrobial compounds compositions, pharmaceutical compositions, the method of use and preparation thereof. Some embodiments relate to boronic acid derivatives and their use as therapeutic agents, for example, β-lactamase inhibitors (BLIs).
BORONIC ACID DERIVATIVES AND THERAPEUTIC USES THEREOF
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Paragraph 0266, (2016/02/28)
Disclosed herein are antimicrobial compounds compositions, pharmaceutical compositions, the use and preparation thereof. Some embodiments relate to boronic acid derivatives and their use as therapeutic agents.
BORONIC ACID DERIVATIVES AND THERAPEUTIC USES THEREOF
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Paragraph 0246, (2016/10/04)
Disclosed herein are antimicrobial compounds compositions, pharmaceutical compositions, the use and preparation thereof. Some embodiments relate to boronic acid derivatives and their use as therapeutic agents.
BORONIC ACID DERIVATIVES AND THERAPEUTIC USES THEREOF
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Paragraph 0253, (2015/12/08)
Disclosed herein are antimicrobial compounds compositions, pharmaceutical compositions, the use and preparation thereof. Some embodiments relate to boronic acid derivatives and their use as therapeutic agents.
Synthetic access to optically active isoflavans by using allylic substitution
Takashima, Yuji,Kaneko, Yuki,Kobayashi, Yuichi
experimental part, p. 197 - 207 (2010/03/03)
A general approach to the (S)- and (R)-isoflavans was invented, and efficiency of the method was demonstrated by the synthesis of (S)-equol ((S)-3), (R)-sativan ((R)-4), and (R)-vestitol ((R)-5). The key step is the allylic substitution of (S)-6a (Ar1=2,4-(MeO)2C6H3) and (R)-6b (Ar1=2,4-(BnO)2C6H3) with copper reagents derived from CuBr·Me2S and Ar2-MgBr (7a, Ar2=4-MeOC6H4; 7b, 2,4-(MeO)2C6H3; 7c, 2-MOMO-4-MeOC6H3), furnishing anti SN2′ products (R)-8a and (S)-8b,c with 93-97% chirality transfer in 60-75% yields. The olefinic part of the products was oxidatively cleaved and the Me and Bn groups on the Ar1 moieties was then removed. Finally, phenol bromide 9a and phenol alcohols 9b,c underwent cyclization with K2CO3 and the Mitsunobu reagent to afford (S)-3 and (R)-4 and -5, respectively.
BENZAMIDO-DERIVATIVES
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, (2008/06/13)
Novel therapeutically active compounds of the formula wherein R1 and R2 are the same or different and each represents a hydrogen atom, a halogen atom, a cyano group, a lower alkyl group or an acyl group, R3 is a lower alkyl group; an alkenyl group; or a b
Potential neuroleptic agents. 3. Chemistry and antidopaminergic properties of substituted 6-methoxysalicylamides
de Paulis,Kumar,Johansson,Raemsby,Florvall,Hall,Angeby-Moeller,Ogren
, p. 1263 - 1269 (2007/10/02)
A series of substituted 6-methoxysalicylamides were synthesized from their corresponding 2,6-dimethoxybenzamides by demethylation of one methoxy group with boron tribromide. Substituted 6-methoxysalicylamides having a lipophilic aromatic substituent in the 3-position para with respect to the methoxy group, e.g. a bromo or an iodo atom or an ethyl or a propyl group, and having an (S)-N-(1-alkyl-2-pyrrolidinyl)methyl moiety as the side chain were found to be potent blockers of [3H]spiperone binding in vitro and potent inhibitors of the apomorphine syndrome in the rat. Similar to remoxipride but in contrast to haloperidol, some of the substituted salicylamides show a 10-20 fold separation between the dose that inhibits hyperactivity and that which inhibits stereotypy. It was concluded that, besides the requirement of a lipophilic substitutent in the position para to the methoxy group for antidopamine activity in vivo, the formation of a coplanar six-membered pseudoring involving the amide moiety and the methoxy group is a structural requirement for activity in vitro.
