Investigating the Ligand‐Binding Properties of N‐arylbenzimidazoles as Novel Elastase Inhibitors
A series of novel N‐[(3,5‐dimethylphenyl)methyl]‐1H‐benzimidazole derivatives is designed, synthesized, and evaluated for inhibitory activity against elastase. Several compounds demonstrate an antielastase activity, including the N‐(2‐bromophenyl)‐2‐(6‐chloro‐1‐(3,5‐dimethylbenzyl)‐1H‐benzo[d]imidazol‐2‐ylthio)acetamide, showing the greatest potency ...
Giovanna Pitasi +6 more
wiley +1 more source
Experimental pharmacological research regarding some new quinazolin-4-ones derivatives [PDF]
A series of new compounds with quinazolin-4-one structure, synthesized by the Pharmaceutical Chemistry Department of the Faculty of Pharmacy of the University of Medicine and Pharmacy “Carol Davila” Bucharest, was studied.
Bratu, Mihaela +8 more
core +1 more source
Structural systematics and conformational analyses of a 3x3 isomer grid of fluoro-N-(pyridyl)benzamides: physicochemical correlations, polymorphism and isomorphous relationships [PDF]
An isomer grid of nine fluoro-N-(pyridyl)benzamides (Fxx) (x = para-/meta-/ortho-) has been examined to correlate structural relationships between the experimental crystal structure and ab initio calculations, based on the effect of fluorine (Fx) and
Allen +43 more
core +1 more source
A Facile Protocol for C(sp2)–C(sp3) Bond Formation Reactions Toward Functionalized E3 Ligase Ligands
A robust C(sp2)–C(sp3) decarboxylative coupling strategy enables access to new CRBN ligands and degraders with improved physicochemical properties. This synthetic approach is expanding the chemical space beyond C(sp2)–N linkages, fine‐tuning proteolysis‐targeting chimera activities and unlocking previously inaccessible degrader chemotypes.
Anita Maksutova +15 more
wiley +1 more source
A fluorinated quinuclidine benzamide named LMA 10203 acts as an agonist of insect nicotinic acetylcholine receptors [PDF]
In the present study, we take advantage of the fact that cockroach dorsal unpaired median neurons express different nicotinic acetylcholine receptor subtypes to demonstrate that simple quinuclidine benzamides such as the 2-fluorinated benzamide LMA 10203,
B. Bodereau-Dubois +4 more
core +3 more sources
In this study, a series of twenty-two 5-chloro-2-hydroxy-N-[2-(arylamino)-1-alkyl-2-oxoethyl]benzamides and ten 4-chloro-2-hydroxy-N-[2-(arylamino)-1-alkyl-2-oxoethyl]benzamides is described.
Jirina Stolarikova +6 more
doaj +1 more source
2-Bromo-N-(dibenzylcarbamothioyl)benzamide [PDF]
The 2-bromo-benzoyl group in the title compound, C(22)H(19)BrN(2)OS, adopts an E conformation with respect to the thiono S atom across the N-C bond. In the crystal structure, the mol-ecule is stablized by N-H⋯O inter-molecular hydrogen bonds, forming a one-dimensional chain along the b axis.
Mohd Faizal Md Nasir +4 more
openaire +3 more sources
Pesticide Contamination in the Hair of Children From Colonia San Juan, a Rural Community in Paraguay
Hair analysis in children from a rural community in Paraguay reveals exposure to organophosphates, pyrethroids, neonicotinoids, fungicides, herbicides, and endocrine disruptors, highlighting the urgent need for stricter environmental protections and preventive health measures. ABSTRACT Chronic exposure to pesticides can cause carcinogenic, reproductive,
Stela Benitez Leite +5 more
wiley +1 more source
Structural systematic studies and conformational analyses of a 3x3 isomer grid of fluoro-N-(pyridyl)benzamides; physicochemical correlations, polymorphism and isomorphous relationships [PDF]
The effect of fluorine and pyridine N atom substitution patterns on molecular structure and conformation is probed in a 3 3 isomer grid (Scheme 1) of fluoro-N-(pyridyl)benzamides (Fxx) (C12H9N2OF, x = para-/meta-/ortho-) to evaluate and correlate ...
Gallagher, John F., Mocilac, Pavle
core
Design, Synthesis and Evaluation of N-pyrazinylbenzamides as Potential Antimycobacterial Agents
Three series of N-(pyrazin-2-yl)benzamides were designed as retro-amide analogues of previously published N-phenylpyrazine-2-carboxamides with in vitro antimycobacterial activity. The synthesized retro-amides were evaluated for in vitro growth inhibiting
Jan Zitko +7 more
doaj +1 more source

