In order to discover new compounds with good fungicidal activities, 32 pyrazole derivatives were designed and synthesized. The structures of the target compounds were confirmed by 1H-NMR, 13C-NMR, and high-resolution electrospray ionization mass spectrometry (HR-ESI-MS), and their fungicidal activities against Botrytis cinerea, Rhizoctonia solani Kuhn, Valsa mali Miyabe et Yamada, Thanatephorus...

The reaction of the cyanoacetylhydrazine (1) with α-bromoketones (2a-c) gave the hydrazide-hydrazone derivatives 3a-c. The latter compounds underwent ready cyclization when heated in sodium ethoxide to form the 1,3,4-oxadiazine derivatives 4a-c. The reaction of 3a with hydrazines gave the 1,3,4-triazine derivatives 7a,b. Compounds 3a-c and 7a,b underwent some heterocyclizations when treated wit...

Pyrazoles are an important class of five membered heterocyclic compounds; are widely found as the core structure in a large variety of compounds that possess important agrochemical and pharmaceutical activities. Pyrazoles have been the recent target of numerous methodologies, mostly due to their prevalence as scaffolds in synthesis of bioactive compounds and reactions in different media. The ai...

The title compound, C(15)H(15)N(3)O(2)S·H(2)O, has been obtained in a search for new imidazo[1,2-b]pyrazole derivatives with better biological activity. The 1H-imidazo[1,2-b]pyrazole plane forms a dihedral angle of 16.90 (3)° with the benzene ring. π-π inter-actions are indicated by the short distance of 3.643 (2) Å between the centroids of the benzene and imidazole rings. The crystal structure...

Aiming for the synthesis of new heterocyclic compounds containing a sulfonamido moiety suitable for use as antibacterial agents, the precursor ethyl {[4-N-(4,6-dimethylpyrimidin-2-yl)sulfamoyl]phenylazo}cyanoacetate was reacted with a variety of active methylene compounds producing pyran, pyridine and pyridazine derivatives. Also, the reactivity of the precursor hydrazone towards hydrazine deri...

Several new pyrazole derivatives have demonstrated promising antiproliferative and cytotoxic effects, but their poor solubility raised concerns over possible biopharmaceutical limitations. In order to improve their pharmaceutical potential we performed the biopharmaceutical profiling for nine pyrazole compounds using in vitro and computational methods. The experimental solubility was determined...

Acetylene carboxylates and an acetylene phosphonate reacted with N-protected (S)-2-(diazoacetyl)pyrrolidines ((S)-diazoprolines) to give optically active bis-heterocyclic pyrazole derivatives in a regioselective [3+2] cycloaddition. The reactions occurred at 60 °C in THF solution in the absence of a catalyst. However, diethyl ethynylphosphonate reacted significantly slower than the carboxylates...

In this study, in order to find novel biologically active pyrazole oxime derivatives, twenty-eight new pyrazole oxime compounds containing a substituted isoxazole ring were synthesized and evaluated for their acaricidaland insecticidal activities. Bioassays exhibited that some target compounds indicated good acaricidal and insecticidal activities against Tetranychus cinnabarinus, Aphis medicagi...

A series of N-(substituted pyridinyl)-1-methyl(phenyl)-3-trifluoromethyl-1H-pyrazole-4-carboxamide derivatives were synthesized. All target compounds were characterized by spectral data (¹H-NMR, ¹³C-NMR, IR, MS) and elemental analysis and were bioassayed in vitro against three kinds of phytopathogenic fungi (Gibberella zeae, Fusarium oxysporum, Cytospora mandshurica). The results showed that so...

The present paper describes the synthesis of some symmetrical substituted 1-(2-chloroethyl) pyrazole-based dichalcogenides and monochalcogenides by reacting different 3,4,5-trisubstituted 1-(2-chloroethyl) pyrazole derivatives with in situ prepared Na2E2 (E = S, Se, Te) and sodium hydrogen selenide, respectively. All compounds were fully characterized by different spectroscopic techniques, name...