Results 51 to 60 of about 178,765 (288)

Inhibition studies on a panel of human carbonic anhydrases with N1-substituted secondary sulfonamides incorporating thiazolinone or imidazolone-indole tails

Journal of Enzyme Inhibition and Medicinal Chemistry, 2018
Being the primary sulfonamide among the most efficient zinc binding group (ZBG) to design inhibitors for the metallo-enzymes carbonic anhydrases (CA, EC 4.2.1.1), herein, we propose an investigation on four physiologically important human (h) CAs (hCA I,
Fadi M. Awadallah, Silvia Bua, Walaa R. Mahmoud, Hossam H. Nada, Alessio Nocentini, Claudiu T. Supuran   +5 more
doaj   +1 more source

Escaping ESKAPE resistance: in vitro and in silico studies of multifunctional carbamimidoyl-tethered indoles against antibiotic-resistant bacteria

Royal Society Open Science, 2023
Combining the hybridization and repurposing strategies, six compounds from our in-house library and having a designed hybrid structure of MBX-1162, pentamidine and MMV688271 were repurposed as potential antibacterial agents.
Kanika Gulia, Ahmed H. E. Hassan, Justin R. Lenhard, Abdelbasset A. Farahat   +3 more
doaj   +1 more source

Diversity-Oriented Synthesis of Indole-Fused Polycyclic Scaffolds via Rhodium-Catalyzed NH-Indole-Directed C–H Coupling of 2‑Phenyl‑1H‑indoles with Propargylic Alcohol Derivatives [PDF]

Diversity-oriented synthesis strategy for the efficient assembly of indole-fused polycyclic scaffolds via rhodium-catalyzed NH-indole-directed C–H coupling with propargylic alcohol derivatives in a regioselective manner was developed.
Leipeng Lu (11675029), Guijiao Xiang (18313132), Yanqiao Wang (5024867), Xiaofeng Zhang (172446), Qiufeng Huang (1963807)   +4 more
core   +1 more source

Hydrogen-Bonding in the Structures of the Hydrated Proton-Transfer Compounds of Isonipecotamide with the Isomeric Indole-2- and Indole-3-Carboxylic Acids [PDF]

, 2011
The structures of two hydrated proton-transfer compounds of 4-piperidinecarboxamide (isonipecotamide) with the isomeric heteroaromatic carboxylic acids indole-2-carboxylic acid and indole-3-carboxylic acid, namely 4-carbamoylpiperidinium indole-2 ...
Urs D. Wermuth, Smith, Graham, Wermuth, Urs D., Wermuth, Urs, Graham Smith, Wermuth, Urs D   +5 more
core   +1 more source

A concise and regioselective synthesis of 6-bromo-5-methoxy-1H-indole-3-carboxylic acid and its derivatives: Strategic development toward core moiety of Herdmanine D [PDF]

, 2020
A concise, regioselective and highly efficient strategy for the construction of 6-bromo-5-methoxy-1H-indole-3-carboxylic acid has been developed through trifluoroacetylated indole driven hydrolysis. The developed protocol has the advantage of selectively
Pankaj Sharma (58141), Gunjan Kashyap (8393136), Sunita Bhagat (8393139), Nutan Sharma (181815)   +3 more
core   +1 more source

Gut microbiome and aging—A dynamic interplay of microbes, metabolites, and the immune system

FEBS Letters, EarlyView.
Age‐dependent shifts in microbial communities engender shifts in microbial metabolite profiles. These in turn drive shifts in barrier surface permeability of the gut and brain and induce immune activation. When paired with preexisting age‐related chronic inflammation this increases the risk of neuroinflammation and neurodegenerative diseases.
Aaron Mehl, Eran Blacher
wiley   +1 more source

Clinical Persistence of Chlamydia trachomatis Sexually Transmitted Strains Involves Novel Mutations in the Functional αββα Tetramer of the Tryptophan Synthase Operon

mBio, 2019
Clinical persistence of Chlamydia trachomatis (Ct) sexually transmitted infections (STIs) is a major public health concern. In vitro persistence is known to develop through interferon gamma (IFN-γ) induction of indoleamine 2,3-dioxygenase (IDO), which ...
Naraporn Somboonna, Noa Ziklo, Thomas E. Ferrin, Jung Hyuk Suh, Deborah Dean   +4 more
doaj   +1 more source

Modulation of Homer1 EVH1 domain internal dynamics by putative autism‐associated mutations

FEBS Letters, EarlyView.
The putative autism‐associated M65I and S97L variants of the EVH1 domain of the postsynaptic scaffold protein Homer1 do not exhibit substantial changes in their overall structure or partner binding. Both of them, but especially the M65I variant, show altered internal dynamics relative to the wild‐type domain on the μs‐ms timescale, indicated by the ...
Fanni Farkas, Brigitta Maruzs, Zsófia E. Kálmán, Tomas Klumpler, Gyula Batta, Bálint Péterfia, Zoltán Gáspári   +6 more
wiley   +1 more source

Indole Treatment Alleviates Intestinal Tissue Damage Induced by Chicken Coccidiosis Through Activation of the Aryl Hydrocarbon Receptor

Frontiers in Immunology, 2019
Indoles, as the ligands of aryl hydrocarbon receptor (AhR), have been shown to possess immune-modulating property in terms of the balancing between regulatory T cells (Treg) and T helper 17 cells (Th17) activities.
Woo H. Kim, Hyun S. Lillehoj, Wongi Min
doaj   +1 more source

Novel Hybrid Indole-Based Caffeic Acid Amide Derivatives as Potent Free Radical Scavenging Agents: Rational Design, Synthesis, Spectroscopic Characterization, In Silico and In Vitro Investigations

Metabolites, 2023
Antioxidant small molecules can prevent or delay the oxidative damage caused by free radicals. Herein, a structure-based hybridization of two natural antioxidants (caffeic acid and melatonin) afforded a novel hybrid series of indole-based amide analogues
Ahmed Elkamhawy, Na Kyoung Oh, Noha A. Gouda, Magda H. Abdellattif, Saud O. Alshammari, Mohammed A. S. Abourehab, Qamar A. Alshammari, Amany Belal, Minkyoung Kim, Ahmed A. Al-Karmalawy, Kyeong Lee   +10 more
doaj   +1 more source