Testing enabling techniques for olefin metathesis reactions of lipophilic substrates in water as a diluent.

Olefin metathesis reactions of diverse polyfunctional substrates were conducted in water emulsions using two hydrophobic ruthenium catalysts in the presence of air. Instead of using surfactants to increase the efficiency of the metathesis reaction in water, ultrasound and microwave techniques were tested on a small-scale reaction, whereas conventional heating and mechanical stirring were effective enough to provide high conversion and selectivity on a larger scale. The developed conditions extend known protocols for the aqueous metathesis methodology, utilizing relatively low catalyst loadings and allowing for simple product isolation and purification.

Synthesis and biological screening of novel 2-morpholinoquinoline nucleus clubbed with 1,2,4-oxadiazole motifs.

Novel series of 2-morpholinoquinoline scaffolds (6a-n), containing the 1,2,4-oxadiazole and moiety, was designed and synthesized in good yield (76-86%). The synthesized compounds were screened for their preliminary in vitro antimicrobial activity against a panel of pathogenic strains of bacteria and fungi. Molecular docking and pharmacokinetic study were carried out for the prepared compounds.

Novel morpholinoquinoline nucleus clubbed with pyrazoline scaffolds: Synthesis, antibacterial, antitubercular and antimalarial activities.

A series of novel morpholinoquinoline based conjugates with pyrazoline moiety were synthesized under microwave irradiation. The newly synthesized compounds were screened for their preliminary in vitro antibacterial activity against a panel of pathogenic strains of bacteria and fungi, antituberculosis activity against Mycobacterium tuberculosis H37Rv and antimalarial activity against Plasmodium falciparum. Most of them exhibited significant antibacterial activity as compared to the first line drugs.

Design, synthesis and characterization of fluoro substituted novel pyrazolylpyrazolines scaffold and their pharmacological screening.

A novel series of fluoro substituted pyrazolylpyrazolines 7a-l was synthesized in good to excellent yield (77-88%) from pyrazole chalcones 5a-d and substituted phenyl hydrazine hydrochlorides 6a-c under microwave irradiation. The newly synthesized compounds were screened for their preliminary in vitro antibacterial activity against a panel of pathogenic stains of bacteria and fungi, antituberculosis activity against Mycobacterium tuberculosis H37Rv and antimalarial activity against Plasmodium falciparum. Compounds 7a, 7b, 7g, 7h, 7j and 7k displayed excellent activity against P.

Congenital cheek teratoma with temporo-mandibular joint ankylosis managed with ultra-thin silicone sheet interpositional arthroplasty.

Primary cheek teratomas are rare with < 5 reported cases. None had associated temporo mandibular joint ankylosis (TMJA). The fundamental aim in the treatment of TMJA is the successful surgical resection of ankylotic bone, prevention of recurrence, and aesthetic improvement by ensuring functional occlusion.

Continuous opioid agonist treatment dose-dependently regulates mu-opioid receptors and dynamin-2 in mouse spinal cord.

Continuous opioid agonist treatment produces tolerance and in some cases mu opioid receptor (muOR) down-regulation. Previous studies indicate that down-regulation of muOR is more likely with high-efficacy opioid agonists (e.g.

Opioid agonist and antagonist treatment differentially regulates immunoreactive mu-opioid receptors and dynamin-2 in vivo.

Opioid agonists and antagonists can regulate the density of mu-opioid receptors in whole animal and in cell culture. High intrinsic efficacy agonists (e.g.

Chronic opioid antagonist treatment dose-dependently regulates mu-opioid receptors and trafficking proteins in vivo.

Chronic opioid antagonist treatment increases the density of mu-opioid receptors (muOR) in many model systems. In previous studies, naltrexone treatment produced an increase in muOR density accompanied by decreases in GRK-2 and DYN-2 protein abundance. To examine the relationship between changes in receptor density and proteins involved in receptor trafficking, the dose-dependent effect of chronic naloxone infusion was determined.

Chronic opioid antagonist treatment selectively regulates trafficking and signaling proteins in mouse spinal cord.

Chronic opioid antagonist treatment produces functional supersensitivity and mu-opioid receptor (muOR) upregulation. Studies suggest a role for G-protein receptor kinases (GRKs) and dynamin (DYN), but not signaling proteins (e.g.