Privileged scaffolds as MAO inhibitors: Retrospect and prospects.

The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.

Triazole compounds that modulate HSP90 activity

In the five membered nitrogen containing heterocyclic family, pyrazoline could be recognized as a promising scaffold for the inhibition of Monoamine oxidase. Substitution at 1, 3 and 5-position of the pyrazoline nucleus displayed a significant activity towards MAO in the past 15 years. Our study identified the detailed structure activity relationship, the structural requirement for enzyme interaction and the effect of chirality on the pyrazoline nucleus towards MAO-A and MAO-B. We propose that the selectivity of pyrazoline nucleus towards MAO isoenzyme depends up on the bulkiness of the ring in the 1 and 3 position of the scaffold. The current review revealed that the derivatives of pyrazolines have proven to be versatile pharmacophores for the inhibition of MAO on the basis of existing literatures between (1998-2013).

Pyrazoline: a promising scaffold for the inhibition of monoamine oxidase.

In this study, we have amalgamated computational methodologies, viz. Petra, Osiris and Molinspiration (POM) to identify pharmacophores and antipharmacophores for antibacterial/antiviral activities of some 2-pyrazolines derivatives. Lipophilicity and the presence of tautomerism process are the major factors that govern the orientation to antibacterial and/or antiviral activity. On other hand, it was observed that these compounds have two different active sites and can inhibit both antiviral and antibacterial strains. Further, we have carried out receptor-based electrostatic analysis to confirm the electronic, steric and hydrophobic requirements for future modifications. The analyses provide substantial idea about the structural features responsible for their combined antibacterial/antiviral activity and provide guidelines for further modifications, with the aim of improving the activity and selectivity of designed drugs targeting HIV and tuberculosis microorganisms. The speculative assertions presented in many papers published in many reputed journals are meaningless. Most of the authors discuss of the antiviral activity compared to the antibacterial activity. There authors seem to consider that there is only one tautomeric form taking one mechanism of action for both antiviral and antibacterial activities. This is false; here, we clarify things on the basis of POM analyses.

Tautomeric origin of dual effects of N1-nicotinoyl-3-(4′-hydroxy-3′-methyl phenyl)-5-[(sub)phenyl]-2-pyrazolines on bacterial and viral strains: POM analyses as new efficient bioinformatics’ platform to predict and optimize bioactivity of drugs

The present work deals with the synthesis of acetoxysulfonamide pyrazole derivatives, substituted 4,5-dihydropyrazole-1-carbothioamide and 4,5-dihydropyrazole-1-isonicotinoyl derivatives starting from substituted vanillin chalcones. Acetoxysulfonamide pyrazole derivatives were prepared from the reaction of chalcones with p-sulfamylphenylhydrazine followed by treatment with acetic anhydride. At the same time 4,5-dihydropyrazole-1-carbothioamide and 4,5-dihydropyrazole-1-isonicotinoyl derivatives were prepared from the reaction of chalcones with either thiosemicarbazide or isonicotinic acid hydrazide, respectively. The synthesized compounds were structurally characterized on the basis of IR, 1H-NMR, 13C-NMR spectral data and microanalyses. All of the newly isolated compounds were tested for their antimicrobial activities. The antimicrobial screening using the agar well-diffusion method revealed that the chloro derivatives are the most active ones. Moreover, the antioxidant and anti-inflammatory activity of these chloro derivatives are also studied using the DPPH radical scavenging and NO radical scavenging methods, respectively.

/pdf/synthesis-characterization-antimicrobial-screening-and-free-35aytdmnda.pdf

Synthesis, Characterization, Antimicrobial Screening and Free-Radical Scavenging Activity of Some Novel Substituted Pyrazoles.

Substituted 1,5-diaryl-3(4-chlorophenyl)-delta 2-pyrazolines were synthesized and evaluated for anticonvulsant activity. Most pyrazolines (100 mg/kg) provided 20-80% protection against pentylenetetrazol-induced convulsions in mice. All compounds inhibited rat brain mitochondrial monoamine oxidase (MAO) and succinic dehydrogenase (SDH) and exhibited low toxicity as reflected by approximate LD50 values (500 to greater than 1000 mg/kg) in mice.

Inhibition of rat brain monoamine oxidase and succinic dehydrogenase by anticonvulsant pyrazolines.

Analgesic activity and monoamine oxidase inhibitory property of substituted mercapto 1,2,4-triazoles

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Inhibition of rat brain monoamine oxidase and succinic dehydrogenase by anticonvulsant pyrazolines.

Analgesic activity and monoamine oxidase inhibitory property of substituted mercapto 1,2,4-triazoles