Solvatomorphism of Moxidectin

The solvatomorphism of the anthelmintic drug moxidectin is investigated, and a new solvatomorph with nitromethane is reported. Moreover, the hitherto unknown crystal structures of the solvatomorphs with ethanol and 2-propanol are reported and discussed. The thermal characterization of these solvatomorphs through variable-temperature powder X-ray diffraction analysis (VT-PXRD) is also described, providing new insights into the crystallochemistry of this active pharmaceutical ingredient

First synthesis of orthogonally 1,7-diprotected cyclens

The first examples of 1,7-orthogonally diprotected cyclen (1,4,7,10-tetraazacyclododecane) derivatives have been prepared through a straightforward and convenient synthetic strategy. These compounds represent useful starting materials for the preparation of several functionalised macrocyclic chelating agents

11 Positron Emission Tomography (PET) Driven Theranostics

\u201cTheranostics\u201d or \u201ctheragnostics\u201d is a concept combining therapy and diagnostics, particularly in vivo to maximize efficient delivery of targeted therapeutic agents to the tumors. It enables \u201cpersonalized medicine\u201d, meaning that the therapy is tailored to the needs of a given patient. Diagnostic imaging has also a great role in the monitoring of therapy, because continuation or change of treatment plan can be decided based on the information about the tracer accumulation in the tumors. In this chapter we briefly describe positron emission tomography-based theranostics in cancer treatment and diagnosis, with a focus on metal-based agents. The chapter will cover the thermodynamics, formation and dissociation kinetics of metal ion-based radiopharmaceuticals for the selection of optimal chelates for the complexation of radiometals and the development of novel and more effective cancer specific theranostic agents

An In Vitro Study on the Application of Silver-Doped Platelet-Rich Plasma in the Prevention of Post-Implant-Associated Infections

: Implant therapy is a common treatment option in dentistry and orthopedics, but its application is often associated with an increased risk of microbial contamination of the implant surfaces that cause bone tissue impairment. This study aims to develop two silver-enriched platelet-rich plasma (PRP) multifunctional scaffolds active at the same time in preventing implant-associated infections and stimulating bone regeneration. Commercial silver lactate (L) and newly synthesized silver deoxycholate:β-Cyclodextrin (B), were studied in vitro. Initially, the antimicrobial activity of the two silver soluble forms and the PRP enriched with the two silver forms has been studied on microbial planktonic cells. At the same time, the biocompatibility of silver-enriched PRPs has been assessed by an MTT test on human primary osteoblasts (hOBs). Afterwards, an investigation was conducted to evaluate the activity of selected concentrations and forms of silver-enriched PRPs in inhibiting microbial biofilm formation and stimulating hOB differentiation. PRP-L (0.3 μg/mm2) and PRP-B (0.2 μg/mm2) counteract Staphylococcus aureus, Staphylococcus epidermidis and Candida albicans planktonic cell growth and biofilm formation, preserving hOB viability without interfering with their differentiation capability. Overall, the results obtained suggest that L- and B-enriched PRPs represent a promising preventive strategy against biofilm-related implant infections and demonstrate a new silver formulation that, together with increasing fibrin binding protecting silver in truncated cone-shaped cyclic oligosaccharides, achieved comparable inhibitory results on prokaryotic cells at a lower concentration

Solvatomorphism of Moxidectin

The solvatomorphism of the anthelmintic drug moxidectin is investigated, and a new solvatomorph with nitromethane is reported. Moreover, the hitherto unknown crystal structures of the solvatomorphs with ethanol and 2-propanol are reported and discussed. The thermal characterization of these solvatomorphs through variable-temperature powder X-ray diffraction analysis (VT-PXRD) is also described, providing new insights into the crystallochemistry of this active pharmaceutical ingredient

Quinone-related hexacyclic by-products in the production process of exemestane

Exemestane, a 3(rd)-generation aromatase inhibitor, is clinically used in the treatment of breast cancer in postmenopausal women. The key step of the industrial synthetic process, i.e., a dehydrogenation to introduce the \u394(1)-unsaturation, is normally performed with quinones such as p-chloranil or DDQ. We observed the formation of two different hexacyclic by-products, depending on the quinone used in the oxidation step. These compounds arise from an initial [4+2] cycloaddition between the precursor 6-methylenandrost-4-ene-3,17-dione and the quinone reagent, followed by a twofold dehydrohalogenation (with p-chloranil) or dehydrogenation (with DDQ). The structures of these unprecedented hexacyclic adducts were determined by a combination of mass spectrometry, NMR techniques and crystallographic analysis