- Neutrophil-Selective Fluorescent Probe Development through Metabolism-Oriented Live-Cell Distinction
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Human neutrophils are the most abundant leukocytes and have been considered as the first line of defence in the innate immune system. Selective imaging of live neutrophils will facilitate the in situ study of neutrophils in infection or inflammation events as well as clinical diagnosis. However, small-molecule-based probes for the discrimination of live neutrophils among different granulocytes in human blood have yet to be reported. Herein, we report the first fluorescent probe NeutropG for the specific distinction and imaging of active neutrophils. The selective staining mechanism of NeutropG is elucidated as metabolism-oriented live-cell distinction (MOLD) through lipid droplet biogenesis with the help of ACSL and DGAT. Finally, NeutropG is applied to accurately quantify neutrophil levels in fresh blood samples by showing a high correlation with the current clinical method.
- Gao, Min,Lee, Sun Hyeok,Park, Sang Hyuk,Ciaramicoli, Larissa Miasiro,Kwon, Haw-Young,Cho, Heewon,Jeong, Joseph,Chang, Young-Tae
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supporting information
p. 23743 - 23749
(2021/10/14)
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- Zinc mediated straightforward access to diacylpyrroles
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In this article, we report the preparation of various 2,4- and 2,5-diacylpyrroles via two zinc-mediated acylation reactions of non-protected pyrroles.
- Faye, Djiby,Mbaye, Mbaye Diagne,Coufourier, Sébastien,Lator, Alexis,Dieng, Samba Yandé,Gaillard, Sylvain,Renaud, Jean-Luc
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p. 492 - 499
(2017/05/19)
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- Reactions of nitrilium salts with indole and pyrrole and their derivatives in the synthesis of imines, ketones and secondary amines
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Abstract Reactions of N-methyl- and N-ethyl-nitrilium salts with indole and pyrrole and their derivatives yield imines or imine salts in good yields. The related imines are obtained from the salts after careful basification and hydrolysis of the imine salts or the imines by heating with aqueous base give the related ketones in good yields. Alternatively, the imine salts can be reduced using sodium borohydride in methanol to give the related secondary amines.
- Giles, Robert G.,Heaney, Harry,Plater, M. John
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p. 7367 - 7385
(2015/08/24)
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- Synthesis and in vitro antitumor activity of 1-(3-dimethylamino)propyl indolin-2-one derivatives
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A series of 1-(3-dimethylaminopropyl)indolin-2-one derivatives were designed and synthesized based on the structural features of TMP-20, LK-B030, and BX-517. These newly synthesized derivatives were evaluated for in vitro activity against five human cancer cell lines and three HUVECs. Results revealed that all of the target compounds 1a-h generally show potent activity against these cancer cell lines and higher selectivity on VEGF- and bFGF-stimulated HUVECs than HUVEC. In particular, 1f (IC50s: 1.10-1.47 μM) is 1.8-6.0-fold more potent than sunitinib against MDA-MB-231, A549, HL-60 and K-562, and 1.6-2.8-fold more potent than LK-B030 against MDA-MB-231 and A549.
- Lv, Kai,Wang, Li-Li,Zhou, Xin-Bo,Liu, Ming-Liang,Liu, Hong-Ying,Zheng, Zhi-Bing,Li, Song
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p. 1723 - 1729
(2013/07/26)
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- Antimalarial activity of natural and synthetic prodiginines
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Prodiginines are a family of linear and cyclic oligopyrrole red-pigmented compounds. Herein we describe the in vitro antimalarial activity of four natural (IC50 = 1.7-8.0 nM) and three sets of synthetic prodiginines against Plasmodium falciparum. Set 1 compounds replaced the terminal nonalkylated pyrrole ring of natural prodiginines and had diminished activity (IC 50 > 2920 nM). Set 2 and set 3 prodiginines were monosubstituted or disubstituted at either the 3 or 5 position of the right-hand terminal pyrrole, respectively. Potent in vitro activity (IC50 = 0.9-16.0 nM) was observed using alkyl or aryl substituents. Metacycloprodiginine and more potent synthetic analogues were evaluated in a P. yoelii murine patent infection using oral administration. Each analogue reduced parasitemia by more than 90% after 25 (mg/kg)/day dosing and in some cases provided a cure. The most favorable profile was 92% parasite reduction at 5 (mg/kg)/day, and 100% reduction at 25 (mg/kg)/day without any evident weight loses or clinical overt toxicity.
- Papireddy, Kancharla,Smilkstein, Martin,Kelly, Jane Xu,Shweta,Salem, Shaimaa M.,Alhamadsheh, Mamoun,Haynes, Stuart W.,Challis, Gregory L.,Reynolds, Kevin A.
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experimental part
p. 5296 - 5306
(2011/10/02)
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- Bu3SnH-mediated radical cyclisation onto azoles
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Alkyl radicals have been cyclised onto pyrroles, imidazoles and pyrazoles, and acyl radicals cyclised onto pyrroles, using Bu3SnH-, (TMS)3SiH- and Bu3GeH-mediated aromatic homolytic substitution for the synthesis of bicyclic N-heterocycles. The reactions yield intermediate π-radicals that lose hydrogen in the?rearomatisation step of the aromatic homolytic substitution. Mechanistic studies of these rearomatisation steps indicate aromatic homolytic substitution in which the initiator or breakdown products from the inhibitor are responsible for the H-abstraction step.
- Allin, Steven M.,Barton, William R.S.,Russell Bowman,Bridge (née Mann), Emma,Elsegood, Mark R.J.,McInally, Tom,McKee, Vickie
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p. 7745 - 7758
(2008/12/21)
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- NOVEL PYRROLE DERIVATIVES WITH ANGIOTENSIN II ANTAGONIST ACTIVITY
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Compounds which may be represented by the general formula (I) shown below and in which: R1 is a group independently selected from among: CHO, -COOH, -CH2OH R2 is hydrogen or a linear or branched C1-C6 alkyl group R3 is hydrogen or a halogen group selected from among Cl and Br R4 is a linear or branched C3-C5 alkyl group and the pharmaceutically acceptable salts thereof such as the sodium or potassium salt. The compounds exhibit potent and selective All antagonist activity and are useful for the treatment of any disorders in which elevated synthesis of All or overexpression of the AT1 receptor may play a primary pathological role, as in the case of arterial hypertension, congestive cardiac insufficiency, platelet aggregation and disorders associated therewith such as for example myocardial and cerebral infarction, renal ischaemia, venous and arterial thrombosis, peripheral vasculopathy, pulmonary hypertension, diabetes mellitus, diabetic neuropathy, glaucoma and diabetic retinopathy.
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Page/Page column 12-13
(2010/02/14)
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- Vilsmeier-Haack preparation of 2-acylpyrroles using bis(trichloromethyl) carbonate and N,N-dimethylacylamines
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A series of 2-acylpyrroles were synthesized by using bis(trichloromethyl) carbonate and N,N-dimethylacylamines as Vilsmeier-Haack reagents under mild conditions in good yields.
- Shi,Su,Shan
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p. 1019 - 1021
(2007/10/03)
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- Synthesis of some diethylphosphono substituted 3H-pyrrolizines
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The preparation of various alkyl substituted monophosphonate 3H-pynolizines via a tandem Michael □ Horner-Emmons reaction is reported. These products were prepared from tetraethyl ethylidene gem-bisphosphonate and corresponding 2-acylpyrroles.
- Loussouarn,Servant,Guervenou,Sturtz
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p. 275 - 285
(2007/10/03)
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- N-(lower alkyl)-2-(3'ureidobenzyl)pyrrolidines
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N-(lower alkyl)-2-(3'-ureidobenzyl)pyrrolidines and N-(lower alkyl)-2-(3'-ureidobenzyl)-5-(lower alkyl)pyrrolidines are useful for lowering intraocular pressure in mammals, for example, in the treatment of glaucoma.
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- THE FORMATION OF ACYLAMINO-DERIVATIVES OF INDOLES AND PYRROLES BY REACTIONS WITH NITRILIUM SALTS
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N-Methylnitrilum fluoroborates are prepared rapidly by warming trimethyloxonium fluoroborate wiht a slight excess of the nitrile, subsquent addition of indoles and pyrroles at low temperatures (-50 deg C to -20 deg C) gives iminium salts (and hence ketones) in high yields.
- Eyley, Stephen C.,Giles, Robert G.,Heaney, Harry
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p. 4649 - 4652
(2007/10/02)
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