- SELECTIVE FLUORESCENT PROBE FOR ALDEHYDE DEHYDROGENASE
-
High aldehyde dehydrogenase 1A1 (ALDH1A1) activity has emerged as a reliable marker for the identification of both normal and cancer stem cells. Herein, is presented AlDeSense, a turn-on green fluorescent probe for aldehyde dehydrogenase 1A1 (ALDH1A1) and Ctrl-AlDeSense, a matching non-responsive reagent. AlDeSense exhibits a 20-fold fluorescent enhancement when treated with ALDH1A1. Through the application of surface marker antibody staining, tumorsphere assays, and assessment of tumorigenicity, the disclosed results show that cells exhibiting high AlDeSense signal intensity have properties of cancer stem cells. Herein, is also reported the development of a red congener, red-AlDeSense. Importantly, red-AlDeSense represents one of only a few examples of a turn-on sensor in the red region using the d-PeT quenching mechanism.
- -
-
Paragraph 0282
(2020/07/14)
-
- The preparation of two, preclinical amino-quinazolinediones as antibacterial agents
-
This paper describes the synthesis of two amino-quinazolinediones which are potent gyrase/topoisomerase inhibitors and useful as antibacterial agents. The early scale-up work to prepare a chiral side chain on multigram scale and two different amino-quinaz
- Beylin, Vladimir,Boyles, David C.,Curran, Timothy T.,Macikenas, Dainius,Parlett IV, Roger V.,Vrieze, Derek
-
p. 441 - 449
(2012/12/31)
-
- Synthesis of mono- and di-substituted 2,4,5-trifluorobenzoic acid synthons, key precursors for biologically active 6-fluoroquinolones
-
In the search for new potent antiparasitical fluoroquinolones, a QSAR analysis by molecular connectivity led to the design of R5 (Me or Et)/R8 (MeO, Me or Et)-substituted analogs of the most powerful antibacterial or antiparasitical
- Anquetin, Guillaume,Greiner, Jacques,Vierling, Pierre
-
p. 8394 - 8404
(2007/10/03)
-
- Pyridonecarboxylic acid derivatives or salts thereof and antibacterial agents containing the same as the active ingredient
-
A novel pyridonecarboxylic acid derivative or its salt exhibiting satisfactory antibacterial activities, intestinal absorption, metabolic stability, and reduced side effects, in particular, phototoxicity and cytotoxicity, as well as an antibacterial agent
- -
-
-
- Pyridonecarboxylic acid derivatives substituted by a bicyclic amino group as antibacterials
-
This invention relates to a N1 -(halogenocyclopropyl)-substituted pyridonecarboxylic acid derivative represented by the following formula (I): STR1 wherein X1 is a halogen atom or a hydrogen atom; X2 is a halogen atom; R1 is a hydrogen atom, a hydroxyl group, a thiol group, a halogenomethyl group, an amino group, an alkyl group or an alkoxy group which may have a substituent group; R2 is a group represented by the following formula (II): STR2 wherein R3 and R4 are independently a hydrogen atom or an alkyl group and n is an integer of 1 or 2; A is a nitrogen atom or a partial structure of the following formula (III): STR3 wherein X3 is a hydrogen atom, a halogen atom, a cyano group, an amino group, an alkyl group, a halogenomethyl group, an alkoxyl group or a halogenomethoxyl group which may have a substituent group; and R is a hydrogen atom, a phenyl group, an acetoxymethyl group, a pivaloyloxymethyl group, an ethoxycarbonyl group, a choline group, a dimethylaminoethyl group, a 5-indanyl group, a phthalidynyl group, a 5-alkyl-2-oxo-1,3-dioxol-4-ylmethyl group, a 3-acetoxy-2-oxobutyl group, an alkyl group, an alkoxymethyl group or a phenylalkyl group, and provides a heterocyclic compound useful as antibacterial drugs.
- -
-
-
- Spiro compound
-
The present invention relates to spiro compounds of general formula I: STR1 wherein the substituents are herein below defined. The present invention relates to antibacterial spiro compounds which are of value as drugs for humans, veterinary drugs or drugs for use in fish culture or as preservatives, and to antibacterial compositions containing one or more of the same compounds as active ingredients.
- -
-
-
- Quinolonecarboxylic acid derivatives and their preparation
-
Quinolonecarboxylic acid derivatives of the following formula, STR1 wherein R indicates straight or branched lower alkyl, R1 indicates cycloalkyl having 3 to 6 carbon atoms, straight or branched lower alkyl, halogenoalkyl, alkenyl, hydroxyalkyl
- -
-
-
