Synthesis of Phenoxyphenyl Pyridine and Pyrazine Carboxamides. Activity against Cydia pomonella (L.) Eggs

Abstract

Several N-(4-phenoxyphenyl)pyridinecarboxamides and N-(4-phenoxyphenyl)pyrazinecarboxamides were synthesized from commercially available material, and their ovicidal activities against Cydia pomonella (L.) were tested. Some of the tested products showed a moderate activity when <24-h-old eggs were sprayed using a Potter tower. A significant increase in the length of the development period of the eggs was also observed in many cases. A clear correlation between both effects was noticed: the products that produced higher mortality also produced higher increase of the length of the development. These results seem to confirm our hypothesis that these compounds could be defined as a juvenile hormone analogues.

Structure and Function of Hemoglobin Confined Inside Silica Nanotubes

“…To further probe the effect of confinement on protein structure and activity, reversible binding of n-donor liquid-based ligands, such as pyridine and its derivatives, were investigated using cyclic voltammetry (CV). Pyridine is selected because it is an important precursor in several pharmaceutical- and agrochemical-based products . Figure b shows the CV of Hb/GC and SNT-Hb/GC in pyridine, C 5 H 5 N (0.1 M of C 5 H 5 N in 0.1 M PBS, pH 7.0).…”

“…Pyridine is selected because it is an important precursor in several pharmaceutical-45 and agrochemical-based products. 46 Figure 6b shows the CV of Hb/GC and SNT-Hb/GC in pyridine, C 5 H 5 N (0.1 M of C 5 H 5 N in 0.1 M PBS, pH 7.0). The Hb/GC electrode showed no pronounced peak in the measured voltage range, suggesting electroinactivity.…”

Discovery and Biophysical Evaluation of First Low Nanomolar Hits Targeting CYP125 of M. tuberculosis

“…For surface plasmon resonance (SPR) spectroscopy guided identification of CYP125 binders, we started with a hand‐picked selection of 132 compounds from our in‐house CYP inhibitor library focusing on structural diversity. The library contained compounds designed for inhibition of human steroidal P450 enzymes, especially CYP17, CYP11B1/2, and CYP19 . These inhibitors are privileged to interact with P450 enzymes because of their nitrogen‐containing heterocycles, which enable coordination to the iron(II) center of heme .…”

“…As the library compounds were originally designed for the inhibition of human steroidogenic enzymes, it was important to compare their activities toward human steroidogenic and hepatic enzymes as well as bacterial CYP enzymes (Table ). Most compounds from our library were active in the nanomolar range against their respective target . From our 14 heme binders, we selected five on the basis of their LE scores to be the most promising hits (i.e., compounds C24 , C60 , C127 , C128 , and C130 ) for further selectivity evaluation.…”

“…Compounds for testing [i.e., LP10 , econazole ( Eco ), and choleste‐3‐en‐4‐one ( CHN )] were purchased from commercial suppliers and were used without further purification. Procedures for the synthesis of library compounds were previously reported . Detailed information can be found in Section S6 of the Supporting Information.…”