In the recent years, the role of LOX enzymes in the cause of neoplastic diseases such as colorectal, skin, pancreatic and renal cancers has been confirmed. A new series of 1,3,4-thiadiazole derivatives bearing 2-pyridyl moiety was synthesized and their cytotoxicity was assessed using MTT protocol. Enzyme inhibitory activity of prepared compounds was also tested against 15-lipoxygenase-1 as nove...

The effect of monochloro and dichloro substitution into the ethyl portion on the pyrolysis of ethyl vinyl ether has been studied. This involved four possible monosubstituted derivatives and six disubstituted derivatives. For the monochloro derivatives, B- chloro substitution enhanced the rate constant while a- chloro substitution depressed it noticeably. For the dichloro derivatives, substi...

An efficient approach for the synthesis of norbuprenorphin derivatives through coupling of enkephalins and norbuprenorphine intermediate is described. Norbuprenorphine derivative was synthesized from thebaine and then, its reaction with succinic acid and phthalic acid was also studied. Meanwhile, the synthesis of enkephalins was done using solid phase peptide synthesis approach. Furthermore, af...

Oxazine derivatives are significant class of heterocycle compounds, which has involved much synthetic attention due to their extensive variety of pharmacological activities. Oxazine is a heterocyclic compound can be formally derived from benzene, and its reduction products, by suitable substitution of carbon (and hydrogen) atoms by nitrogen and oxygen. In the last few years oxazine derivatives ...

although several methods for the preparation of 4o propargyl indole derivatives have been published, this synthetic transformation is complicated by the tendency of 3o propargyl alcohols to form allenium intermediates in acidic media.  it is therefore a challenge to find an efficient method for the c-3 propargylation of indoles with 3° propargylic alcohols.  in this paper we wish to report on t...

a very efficient one-pot three-component synthesis of pyran derivatives has been improved by condensation of aldehydes and malononitrile with dimedone under 80 °c using sucrose as natural and biodegradable catalyst in water. this method offers some advantages including inexpensive, high to quantitative yields, short reaction time, and easy work-up. therefore, this methodology is entirely green ...

An efficient approach for the synthesis of norbuprenorphin derivatives through coupling of enkephalins and norbuprenorphine intermediate is described. Norbuprenorphine derivative was synthesized from thebaine and then, its reaction with succinic acid and phthalic acid was also studied. Meanwhile, the synthesis of enkephalins was done using solid phase peptide synthesis approach. Furthermore, af...

Quercetin, a ubiquitous flavonol, represents a promising leading drug for development of new chemotherapeutic agents. However, its limited cytotoxicity to cancer cells hampers its clinical use. In order to obtain novel quercetin derivatives with superior cytotoxicity, seven alkylated quercetin derivatives were synthesized. Solubility of these derivatives was determined by turbidimetry. Cytotoxi...

Various antibacterial fluoroquinolone compounds were prepared by the direct amination of 7-halo-6- fluoroquinolone-3-carboxylic acids with variety of piperazine derivatives and (4aR,7aR)-octahydro-1H-pyrrolo[3,4-b] pyridine using Zirconia Sulfuric Acid (ZrSA) nanoparticle, as a catalyst in refluxing water. The results showed that ZrSA exhibited high catalytic activity towards the synthesis of f...