91915-33-2

Upstream product

• 90-02-8 salicylaldehyde 
• 20939-15-5 3-methyl-4-amino-5-mercapto-1,2,4-triazole 
• 20939-15-5 4-amino-5-methyl-2,4-dihydro-[1,2,4]triazole-3-thione 

Relevant academic research and scientific papers

4-Salicylideneamino-3-methyl-1,2,4-triazole-5-thione as a sensor for aniline recognition

Tridentate triazole based Schiff base 4-salicylideneamino-3-methyl-1,2,4- triazole-5-thione has been found to selectively detect toxic aromatic amines such as aniline and benzene-1,4-diamine by simple titration techniques like UV-visible, fluorescence spe

Design, synthesis and biological evaluation of pleuromutilin-Schiff base hybrids as potent anti-MRSA agents in vitro and in vivo

A series of pleuromutilin derivatives with 1,2,4-triazole-3-substituted Schiff base structure were designed and synthesized under mild conditions. The in vitro antibacterial activities of the synthesized derivatives against 4 strains of Staphylococcus aureus (MRSA ATCC 43300, S.aureus ATCC 29213, S.aureus 144 and S.aureus AD3) and 1 strain of E. coli (ATCC 25922) were evaluated by the broth dilution method. Among these derivatives, compound 60 exhibited superior in vitro antibacterial effect against MRSA (MIC = 0.25 μg/mL) than tiamulin (MIC = 0.5 μg/mL), and compound 60 (?2.28 log10 CFU/mL) also displayed superior in vivo antibacterial efficacy than tiamulin (?1.40 log10 CFU/mL) in reducing MRSA load in the mouse thigh infection model. The time-kill study and the post-antibiotic effect study indicated that compound 60 showed a faster bactericidal kinetic and longer PAE time (exposure to 2 × MIC and 4 × MIC for 2 h, the PAE was 4.06 and 4.27 h) against MRSA compared with tiamulin (exposure to 2 × MIC and 4 × MIC for 2 h, the PAE was 1.72 and 2.14 h). Meanwhile, most of these compounds had no significant inhibitory effect on RAW 264.7 cells and HepG2 cells at the concentration of 4 μg/mL. Additionally, the development of resistance study showed that MRSA did not easily develop resistance against compound 60 compared with tiamulin after induction for 8 passages.

Pleuromutilin derivative with 1,2,4-triazole Schiff base as well as preparation and application of pleuromutilin derivative

The invention belongs to the field of medicinal chemistry, and particularly relates to a pleuromutilin derivative with 1,2,4-triazole Schiff base as well as preparation and application of the pleuromutilin derivative. The pleuromutilin derivative with 1,2,4-triazole Schiff base is a compound represented by a formula 2 or a pharmaceutically acceptable salt thereof, and a solvate, an enantiomer, a diastereoisomer, a tautomer or a mixture of the solvate, the enantiomer, the diastereoisomer and the tautomer of the compound of formula 2 or the pharmaceutically acceptable salt thereof, the compoundnot only has good in-vitro antibacterial activity, but also has the advantage of low preparation cost compared with valnemulin and retapamulin, so that the compound is particularly suitable for beingused as a novel antibacterial drug for preventing and treating human or animal bacterial infectious diseases, particularly infectious diseases caused by drug-resistant staphylococcus aureus.

Tautomerism aspect of thione-thiol combined with spectral investigation of some 4-amino-5-methyl-1,2,4-triazole-3-thione Schiff's bases

Reaction of 4-amino-3-methyl-1,2,4-triazole-5-thione with some substituted benzaldehydes in presence of catalytic amount of hydrochloric acid afforded the respective Schiff's bases 3a-e. Computational studies using DFT incorporating the B3LYP/6-311G(d,p)

Synthesis and biological evaluation of novel hydroxybenzaldehyde-based kojic acid analogues as inhibitors of mushroom tyrosinase

Two series of novel kojic acid analogues (4a–j) and (5a–d) were designed and synthesized, and their mushroom tyrosinase inhibitory activities was evaluated. The result indicated that all the synthesized derivatives exhibited excellent tyrosinase inhibitor

5 - Substituted - 3 - [5 - hydroxy - 4 - pyrone - 2 - yl - methylthio] - 4 - hydroxybenzoic amino - 1, 2, 4 - triazole compound and use thereof

The invention provides novel 5-substituted-3-[5-hydroxyl-4-pyrone-2-yl-methylthio]-4- hydroxybenzyl-methylamino-1,2,4-triazole compounds represented in a formula (I). In the formula (I), a substituent R1 is H, -CH3, -CH2CH3, C6H5-, 2-CH3C6H4-, 3-CH3C6H4-,

Copper complexes with N-aminotriazolethione azomethines: Structures and magnetochemical properties

Azomethine derivatives of 4-amino-1,2,4-triazole-3-thiones (H2L) and their metal complexes were obtained. The stabilities of the ligand conformers were calculated using quantum-chemical techniques. Ab initio (B3LYP/LANL2DZ) calculations of the complexes in the lower singlet and triplet states were performed with full geometry optimization. The structures and magnetochemical properties of the chelate complexes obtained were examined over a wide temperature range.

Synthesis of New Schiff Bases Derived from 4-Amino-5-mercapto-3-methyl-1,2,4-triazole and Salicylaldehyde or Substituted Salicylaldehydes and Their Copper(II) Complexes

Six new schiff bases, derived from 4-amino-5-mercapto-3-methyl-1,2,4-triazole and salicylaldehyde, 5-chlorosalicylaldehyde, 5-bromosalicylaldehyde, 5-nitrosalicylaldehyde, 3-ethoxysalicylaldehyde or 2-hydroxy-1-naphthaldehyde, and their copper(II) complexes have been synthesized and characterized on the basis of elemental analyses, IR and electronic spectra and magnetic susceptibility measurements.The schiff basis act as dibasic, tridentate ONS donors and form copper(II) complexes with 1:1 (metal:ligand) ratio.The complexes exhibit subnormal magnetic moments in the range 1.15-1.34 B.M. due to the presence of antiferromagnetic exchange.The exchange coupling constant (J) values of the complexes are in the range -296 to -389 cm -1 and are indicative of S=0 ground state with antiferromagnetic spin-spin coupling.The complexes show a ligand field band around 15500 cm -1 and a charge-transfer band around 24000 cm -1.An oxygen bridged dimetallic structure has been deduced.