Publisher SummaryThis chapter provides the basic synthesis paths routes for the manufacture of propaquizafop, with a listing of the main raw materials and intermediates used in the synthesis of propaquizafop. Propaquizafop is commercially known as Agil or Shogun, and it belongs to the quinoxalin...

Propaquizafop is an herbicide with demonstrated hepatocarcinogenic activity in rodents. A rodent-specific mode of action (MOA) in the liver via activation of peroxisome proliferator-activated receptor α (PPARα) has been postulated based on existing data. Experience with PPARα-inducing pharmac...

Diazomethylation esterified all tested acidic indoles without appreciable loss. A group of ten methyl ester derivatives were obtained in crystalline form. These were used to test the relative values of four gas chromatographic substrates. Quantitative comparisons led to the selection of Versamid...

S-nitrosylation, regulated by S-nitrosoglutathione reductase (GSNOR), is considered as an important route for nitric oxide (NO)-modulated stress tolerance in plants. However, genetic evidence for the GSNOR-mediated integrated regulation of S-nitrosylation and plant stress response remains elusiv...

The present work was aimed at exploring a series of R/S-3,4-dihydro-2,2-dimethyl-6-halo-4-(phenylaminothiocarbonylamino)-2H-1-benzopyrans structurally related to (±)-cromakalim and differently substituted at the 4- and 6-positions. The biological effects of these putative activators of ATP-sens...

A series of substituted tricyclic 4,4-dimethyl-3,4-dihydrochromeno[3,4-d]imidazole derivatives have been synthesized and their mPGES-1 biological activity has been disclosed in detail. Structure-activity relationship (SAR) optimization provided inhibitors with excellent mPGES-1 potency and low t...

A simple, efficient, and eco-friendly synthetic protocol has been developed for the synthesis of pyranoxanthenes via one pot three-component reaction. This reaction is between aromatic aldehyde, 2,2-dimethylchroman-7-ol and 1,3-cyclohexanedione by using molecular iodine in AcOH as a reaction med...

The current therapeutic arsenal for toxoplasmosis is restricted to drugs non-specific to the parasite which cause important side effects. Development of more efficient and specific anti-Toxoplasma compounds is urgently needed. Imidazo[1,2-b]pyridazines designed to inhibit the calcium-dependent p...

We herein report two hydrochloride crystals obtained by slow diffusion of acetone into methanol solution of 2-(imidazo[1,2-a]pyridin-2-yl)-2-oxoacetic acid radical which was acidified with different concentration of hydrochloric acid. The relationship between magnetic properties and crystal-stac...

Electrochemical oxidative selenylation of imidazo[1,2–a]pyridines has been developed. The reaction proceeds in an undivided electrochemical cell equipped with glassy carbon electrodes employing LiClO4 as a supporting electrolyte. This approach is environmentally benign by using shelf-stable dis...

A series of 11-aryl-11H-indeno[1′,2′:4,5]imidazo[1,2-a]pyridines was obtained via AlCl3-promoted, dehydrative cyclization of the corresponding aryl(2-arylimidazo[1,2-a]pyridin-3-yl)methanols in moderate to good yields. The synthesized compounds can be considered as conformationally restricted,...

Examples of 2,2′-, 2,3′-, and 2,7′-biindolyls have been prepared by the reaction of indoles with indolin-2-ones and phosphoryl chloride or trifluoromethanesulfonic anhydride. In certain conditions terindolyls can also be formed and those described contain combinations of the above linkages.

Isatin is a well acknowledged pharmacophore in many clinically approved drugs used for treatment of cancer. 3-Hydrazinoindolin-2-one, as a derivative of isatin, represents a pharmacophore of an important class of biologically active pharmaceutical agents by virtue of their diverse biological act...

The synthesis, structure–activity relationships (SAR) and structural data of a series of indolin-2-one inhibitors of RET tyrosine kinase are described. These compounds were designed to explore the available space around the indolinone scaffold within RET active site. Several substitutions at di...

Diabetic complications and their detrimental effects caused by sugar derived substances, have been the serious issue for the last few years and have yet not been fully combated. The key point of the present study is to synthesize some newer chemical entities which can eradicate such ailments to ...

The intramolecular cyclization of 2′-aminochalcones derived from 2- and 4-pyridinecarboxaldehydes was carried out in the presence of Amberlyst®-15/AcOH media. Unexpectedly, the reaction proceeded through a 5-exo process turning into an alternative approach for the synthesis of 2-(pyridinylmethy...

New series of oxindol-based heterocyclic entities (2–11) have been designed and synthesized using indolin-2-one derivatives as key materials (1a–d). The chemical structures of the new synthesized compounds were characterized by FTIR, 1HNMR, 13CNMR, MS spectroscopy and elemental analyses. Three...

In the current study, twenty-two compounds based upon 3-hydroxy-3-(2-oxo-2-phenylethyl)indolin-2-one nucleus were designed, synthesized and in vitro evaluated for HIV-1 RT inhibition and anti-HIV-1 activity. Compounds 3d, 5c and 5e demonstrated encouraging potency against RT enzyme as well as HI...

First ever synthesis of functionalized 5,7-dihydro-6H-dibenzo[d,f][1,3]diazepin-6-ones (6, 9) has been developed through base induced ring transformation of 2H-pyran-2-one-3-carbonitriles with indolin-2-ones. A protocol for alkenylating indolin-2-ones by 2H-pyran-2-one-3-carbonitriles has also b...

We have previously described the identification of indolin-2-one-5-carboxamides as potent PAK4 inhibitors. This study expands the structure-activity relationships on our original series by presenting several modifications in the lead compounds, 2 and 3. A series of novel derivatives was designed...