0000000000972786
AUTHOR
Raimondi Maria Valeria
THE ROLE OF THE CLINICAL PHARMACIST IN THE MANAGEMENT OF ANTIRETROVIRAL THERAPY
Over the last few years, the Hospital Pharmacy has developed in an excellent way in Europe, proposing in many countries the clinical pharmacist as a new professional figure, and adapting its responsibilities to national health systems. The purpose of this study is to evaluate and promote the prescriptive appropriateness through the close collaboration between the pharmacist and the medical team. The aspect of the dispensation of antiretroviral therapy was deepened by providing useful information to the patient on the possible undesired effects and interactions due to the polypharmacy, on the correct way of storing the drugs, and on the importance of the regularity of the polypharmacy intake…
Synthesis, biological evaluation, and molecular docking studies of aldotetronic acid-based LpxC inhibitors
: In order to develop novel inhibitors of the bacterial deacetylase LpxC bearing a substituent to target the UDP binding site of the enzyme, a series of aldotetronic acid-based hydroxamic acids was accessed in chiral pool syntheses starting from 4,6-O-benzylidene-d-glucose and l-arabinitol. The synthesized hydroxamic acids were tested for LpxC inhibitory activity in vitro, revealing benzyl ether 17a ((2S,3S)-4-(benzyloxy)-N,3-dihydroxy-2-[(4-{[4-(morpholinomethyl)phenyl]ethynyl}benzyl)oxy]butanamide) as the most potent LpxC inhibitor. This compound was additionally tested for antibacterial activity against a panel of clinically relevant Gram-negative bacteria, bacterial uptake, and suscepti…
Development of [1,2]oxazoloisoindoles tubulin polymerization inhibitors: Further chemical modifications and potential therapeutic effects against lymphomas
Lymphomas are among the ten most common cancers, and, although progress has been achieved in increasing survival, there is still an unmet need for more effective therapeutic approaches, including better options for patients with refractory tumors that initially respond but then relapse. The lack of effective alternative treatment options highlights the need to develop new therapeutic strategies capable of improving survival prospects for lymphoma patients. Herein, we describe the identification and exploration of the SAR of a series of [1,2]oxazolo[5,4-e]isoindoles as potent small molecules that bind to the colchicine site of tubulin and that have promise for the treatment of refractory lym…