79513-35-2Relevant articles and documents
Discovery of Amphamide, a Drug Candidate for the Second Generation of Polyene Antibiotics
Bychkova, Elena N.,Bykov, Evgeny E.,Efimova, Svetlana S.,Grammatikova, Natalia E.,Isakova, Elena B.,Mirchink, Elena P.,Ostroumova, Olga S.,Pereverzeva, Eleonora R.,Shchekotikhin, Andrey E.,Solovieva, Svetlana E.,Tevyashova, Anna N.,Treshchalin, Ivan D.,Zatonsky, George V.
, p. 2029 - 2044 (2020/09/21)
Amphotericin B (AmB, 1) is the drug of choice for treating the most serious systemic fungal or protozoan infections. Nevertheless, its application is limited by low solubility in aqueous media and serious side effects such as infusion-related reactions, hemolytic toxicity, and nephrotoxicity. Owing to these limitations, it is essential to search for the polyene derivatives with better chemotherapeutic properties. With the objective of obtaining AmB derivatives with lower self-aggregation and improved solubility, we synthesized a series of amides of AmB bearing an additional basic group in the introduced residue. The screening of antifungal activity in vitro revealed that N-(2-aminoethyl)amide of AmB (amphamide, 6) had superior antifungal activity compared to that of the paternal AmB. Preclinical studies in mice confirmed that compound 6 had a much lower acute toxicity and higher antifungal efficacy in the model of mice candidosis sepsis compared with that of AmB (1). Thus, the discovered amphamide is a promising drug candidate for the second generation of polyene antibiotics and is also prospective for in-depth preclinical and clinical evaluation.
Tmob Side Chain-Protected S-Cysteine- and Homo-S-cysteinesulfonamides, their Nα-Protected and Nω-Aminoethylated Derivatives
Videnov, Georgi,Aleksiev, Boris,Stoev, Mincho,Paipanova, Tamara,Jung, Guenther
, p. 941 - 946 (2007/10/02)
The 2,4,6-trimethoxybenzyl (Tmob) group is very suitable for temporary protection of the aminosulfonyl group of S-cysteine- and homo-S-cysteinesulfonamides.Both the introduction and removal of the Tmob-protecting group can be achieved in high yields. 2-Am