- Design of novel tripyridinophane-based Eu(iii) complexes as efficient luminescent labels for bioassay applications
-
In this work, the development of highly luminescent europium(iii) complexes in water solution is reported, including their syntheses, analyses of their photophysical properties and applications in bioassays. Three Eu(iii) complexes are derived from new li
- Bourrier, Emmanuel,Faure, Pamela,Galaup, Chantal,Lamarque, Laurent,Leygue, Nadine,Picard, Claude,Zwier, Jurriaan M.
-
supporting information
p. 182 - 195
(2021/12/29)
-
- Does targeting Arg98 of FimH lead to high affinity antagonists?
-
Bacterial resistance has become an important challenge in the treatment of urinary tract infections. The underlying resistance mechanisms can most likely be circumvented with an antiadhesive approach, antagonizing the lectin FimH located at the tip of fim
- Toma?i?, Tihomir,Rabbani, Said,Jakob, Roman P.,Reisner, Andreas,Jakopin, ?iga,Maier, Timm,Ernst, Beat,Anderluh, Marko
-
-
- Photocatalytic Oxidative Iodination of Electron-Rich Arenes
-
A visible-light-mediated oxidative iodination of electron-rich arenes has been developed. 2.5 mol% of unsubstituted anthraquinone as photocatalyst were used in combination with elementary iodine, trifluoroacetic acid and oxygen as the terminal oxidant. The iodination proceeds upon irradiation in non- or weakly-electron donating solvents (DCM, DCE and benzene) wherein a spectral window in strongly coloured iodine solutions can be observed at around 400 nm. The method provides good to excellent yields (up to 98%) and shows excellent regioselectivity and good functional group tolerance (triple bonds, ketone, ester, amide). Moreover, the photo-iodination was also upscaled to a 5 mmol scale (1.1 g). Mechanistic investigations by intermediate trapping and competition experiments indicate a photocatalytic arene oxidation and the subsequent reaction with iodine as a likely mechanistic pathway. (Figure presented.).
- Narobe, Rok,Düsel, Simon J. S.,Iskra, Jernej,K?nig, Burkhard
-
supporting information
p. 3998 - 4004
(2019/07/17)
-
- WATER-SOLUBLE TRIAZAPYRIDINOPHANE-BASED COMPLEXING AGENTS AND CORRESPONDING FLUORESCENT LANTHANIDE COMPLEXES
-
The invention relates to complexing agents of formula (I) in which A1, A2, A3 and R1 are as defined in the description. The invention also relates to lanthanide complexes obtained from said complexing agents. The invention can be used for marking biological molecules.
- -
-
Paragraph 0081
(2019/01/04)
-
- Noncovalent Inhibitors of Mosquito Acetylcholinesterase 1 with Resistance-Breaking Potency
-
Resistance development in insects significantly threatens the important benefits obtained by insecticide usage in vector control of disease-transmitting insects. Discovery of new chemical entities with insecticidal activity is highly desired in order to develop new insecticide candidates. Here, we present the design, synthesis, and biological evaluation of phenoxyacetamide-based inhibitors of the essential enzyme acetylcholinesterase 1 (AChE1). AChE1 is a validated insecticide target to control mosquito vectors of, e.g., malaria, dengue, and Zika virus infections. The inhibitors combine a mosquito versus human AChE selectivity with a high potency also for the resistance-conferring mutation G122S; two properties that have proven challenging to combine in a single compound. Structure-activity relationship analyses and molecular dynamics simulations of inhibitor-protein complexes have provided insights that elucidate the molecular basis for these properties. We also show that the inhibitors demonstrate in vivo insecticidal activity on disease-transmitting mosquitoes. Our findings support the concept of noncovalent, selective, and resistance-breaking inhibitors of AChE1 as a promising approach for future insecticide development.
- Knutsson, Sofie,Engdahl, Cecilia,Kumari, Rashmi,Forsgren, Nina,Lindgren, Cecilia,Kindahl, Tomas,Kitur, Stanley,Wachira, Lucy,Kamau, Luna,Ekstr?m, Fredrik,Linusson, Anna
-
supporting information
p. 10545 - 10557
(2019/01/04)
-
- New Approach to 1,4-Benzoxazin-3-ones by Electrochemical C?H Amination
-
1,4-Benzoxazin-3-ones are important structural motifs in natural products and bioactive compounds. Usually, the synthesis of benzoxazinones requires transition-metal catalysts and pre-functionalized substrates such as aryl halides. However, the anodic C?H
- Wesenberg, Lars Julian,Herold, Sebastian,Shimizu, Akihiro,Yoshida, Jun-Ichi,Waldvogel, Siegfried R.
-
supporting information
p. 12096 - 12099
(2017/09/13)
-
- Super Aryl-Extended Calix[4]pyrroles: Synthesis, Binding Studies, and Attempts To Gain Water Solubility
-
We describe the synthesis of unprecedented calix[4]pyrrole receptors featuring “super aryl extended” (SAE) cavities. We elaborated the aromatic cavity provided by the αααα-isomer of para-tetraiodo-meso-phenyl calix[4]pyrrole by installing ethynyl-aryl sub
- Escobar, Luis,Aragay, Gemma,Ballester, Pablo
-
supporting information
p. 13682 - 13689
(2016/09/13)
-
- A potent and selective small-molecule inhibitor for the lymphoid-specific tyrosine phosphatase (LYP), a target associated with autoimmune diseases
-
Lymphoid-specific tyrosine phosphatase (LYP), a member of the protein tyrosine phosphatase (PTP) family of signaling enzymes, is associated with a broad spectrum of autoimmune diseases. Herein we describe our structure-based lead optimization efforts with
- He, Yantao,Liu, Sijiu,Menon, Ambili,Stanford, Stephanie,Oppong, Emmanuel,Gunawan, Andrea M.,Wu, Li,Wu, Dennis J.,Barrios, Amy M.,Bottini, Nunzio,Cato, Andrew C. B.,Zhang, Zhong-Yin
-
p. 4990 - 5008
(2013/07/26)
-
- CALCIUM-SENSING RECEPTOR-ACTIVE COMPOUNDS
-
A compound of general formula I their use as calcium receptor-active compounds for the prophylaxis, treatment or amelioration of physiological disorders or diseases associated with disturbances of CaSR activity, such as hyperparathyroidism, pharmaceutical
- -
-
-
- 4,4-(disubstituted) cyclohexan-1-one monomers and related compounds
-
This invention relates to derivatives of 4,4-(disubstituted)cyclohexan-1-ones and related compounds which are useful for treating allergic and inflammatory diseases.
- -
-
-
- Applicability of Hammett Equation to the Kinetics of Acid-catalysed Esterification of meta- and para-Substituted Phenoxyacetic Acids by Methanol
-
Rate constants have been determined for the acid-catalysed esterification of meta- and para-substituted phenoxyacetic acids by methanol, with hydrogen chloride as catalyst.The applicability of the Hammett equation to the rate data has been examined.The para-substituted benzoic acids react slower than the corresponding para-substituted phenoxyacetic acids.The probable cause of this behaviour is discussed.
- Baliah, V.,Gurumurthy, R.
-
p. 629 - 631
(2007/10/02)
-
- Influence of meta- and para-Substituents on the Kinetics of Esterification of Phenoxyacetic Acids by Methanol
-
The influence of meta- and para- substituents on the kinetics of acid-catalysed esterification of phenoxyacetic acids is discussed.In the case of para Cl, Br and I substituents, d-orbital resonance is suggested to explain the observed behaviour.The possibility of protonation of the methoxy oxygen in the acid medium employed is indicated to explain the slower rate of reaction of m- and p-methoxyphenoxyacetic acids.
- Baliah, V.,Gurumurthy, R.
-
p. 1082 - 1083
(2007/10/02)
-