Synthesis of 11-(Piperazin-1-yl)-5H-dibenzo[b,e] [1,4]diazepine on Kilo Scale

Abstract: A synthesis of 11-(piperazin-1yl)-5H-dibenzo [b,e][1,4]diazepine on kilo scale without any chromatographic purification step is reported. Key steps involved are Ullmann condensation, catalytic hydrogenation, and catalyzed cyclization

Nano-carrier based drug delivery systems for sustained antimicrobial agent release from orthopaedic cementous material

Total joint replacement (TJR), such as hip and knee replacement, is a popular procedure worldwide. Prosthetic joint infections (PJI) after this procedure have been widely reported, where treatment of such infections is complex with high cost and prolonged hospital stay. In cemented arthroplasties, the use of antibiotic loaded bone cement (ALBC) is a standard practice for the prophylaxis and treatment of PJI. Recently, the development of bacterial resistance by pathogenic microorganisms against most commonly used antibiotics increased the interest in alternative approaches for antimicrobial delivery systems such as nanotechnology. This review summarizes the efforts made to improve the antimicrobial properties of PMMA bone cements using nanotechnology based antibiotic and non-antibiotic delivery systems to overcome drawbacks of ALBC in the prophylaxis and treatment of PJIs after hip and knee replacement

Phosphine-Free Tetradentate Salicylaldimine Ligand Complexed with Palladium: First Application in Heck Reactions

<div><p></p><p>Heck reactions were carried out using phosphine-free tetradentate salicylaldimine ligand complexed with PdCl₂ under mild reaction conditions, short reaction time, and low palladium loading. All aryl iodides underwent coupling reactions with olefins, giving corresponding <i>trans</i>-products, with good to excellent yields, whereas aryl bromides gave very poor yields and aryl chlorides failed to react.</p> </div

Evaluation of Oleic Acid and Polyethylene Glycol Monomethyl Ether Conjugate (PEGylated Oleic Acid) as a Solubility Enhancer of Furosemide

Poor aqueous solubility limits the therapeutic efficacy of many marketed and investigational drugs. Synthesis of new drugs with improved solubility is challenging due to time constraint and expenses involved. Therefore, finding the solubility enhancers for existing drugs is an attractive and profitable strategy. In this study, PEGylated oleic acid (OA-mPEG5000), a conjugate of oleic acid and mPEG5000 was synthesized and evaluated as a solubilizer for furosemide. OA-mPEG5000 was evaluated as a nanocarrier for furosemide by formulating polymersomes. Solubility of furosemide in milli-Q water and aqueous OA-mPEG5000 solution was determined using shake flask method. At 37 &deg;C, the solubility of furosemide in OA-mPEG5000 (1% w/w) and milli-Q water was 3404.7 &plusmn; 254.6 &micro;g/mL and 1020.2 &plusmn; 40.9 &micro;g/mL, respectively. Results showed there was a 3.34-fold increase in solubility of furosemide in OA-mPEG5000 compared to water at 37 &deg;C. At 25 &deg;C, there was a 3.31-fold increase in solubilization of furosemide in OA-mPEG5000 (1% w/w) (90.0 &plusmn; 1.45 &micro;g/mL) compared to milli-Q water (27.2 &plusmn; 1.43 &micro;g/mL). Size, polydispersity index and zeta potential of polymersomes ranged from 85&ndash;145.5 nm, 0.187&ndash;0.511 and &minus;4.0&ndash;12.77 mV, respectively. In-vitro release study revealed a burst release (71%) within 1 h. Significant enhancement in solubility and formation of polymersomes suggested that OA-mPEG5000 could be a good solubilizer and nanocarrier for furosemide