Pregled bibliografske jedinice broj: 1215324
Novel reversed amidine benzothiazoles: design, synthesis, antitrypanosomal activity and ADME profiling
Novel reversed amidine benzothiazoles: design, synthesis, antitrypanosomal activity and ADME profiling // 27th EFMC International Symposium on Medicinal Chemistry 2022 (EFMC-ISMC)
Nica, Francuska, 2022. str. 334-334 (poster, podatak o recenziji nije dostupan, sažetak, znanstveni)
CROSBI ID: 1215324 Za ispravke kontaktirajte CROSBI podršku putem web obrasca
Naslov
Novel reversed amidine benzothiazoles: design,
synthesis, antitrypanosomal activity and ADME
profiling
Autori
Rep, Valentina ; Koštrun, Sanja ; Taylor, Martin C. ; Kelly, John M. ; Raić-Malić, Silvana
Vrsta, podvrsta i kategorija rada
Sažeci sa skupova, sažetak, znanstveni
Skup
27th EFMC International Symposium on Medicinal Chemistry 2022 (EFMC-ISMC)
Mjesto i datum
Nica, Francuska, 04.09.2022. - 08.09.2022
Vrsta sudjelovanja
Poster
Vrsta recenzije
Podatak o recenziji nije dostupan
Ključne riječi
arylimidamide ; benzothiazole ; antitrypanosomal activity ; ADME properties
Sažetak
Trypanosomatid protozoan parasites have a significant socioeconomic impact worldwide [1]. Amongst them are parasites of the Trypanosoma brucei species, which cause sleeping sickness, also known as human African trypanosomiasis (HAT). The current drugs used to treat HAT, pentamidine, suramin, melarsoprol and nifurtimoxeflornithine combination therapy (NECT), are toxic and not always effective due to the appearance of drug- resistance [1]. Although the design of arylimidamides (AIAs) was inspired by diamidine antiprotozoal agent pentamidine, AIAs possess physicochemical properties that are distinct from those of diamidines. In the AIAs, the imino group is bound to an aniline nitrogen atom, lowering the pKa of the amidine and increasing the lipophilicity of the molecule compared to a dicationic diamidine compound [2]. Previous studies by our group [3, 4] have shown that nitrogen heterocycles, such as benzimidazole and benzothiazole derivatives with cationic amidine moiety, have good antiprotozoal potency. Herein, we have designed and synthesized the arylimidamide-benzothiazoles with diversification in the substituted phenoxy moieties, as central part, and right-hand side of a molecule to modulate physicochemical and biological properties. Besides antitrypanosomal activity, physicochemical and ADME properties of prepared analogues will so be presented.
Izvorni jezik
Engleski
Znanstvena područja
Kemija
POVEZANOST RADA
Projekti:
HRZZ-IP-2018-01-4682 - Novi spojevi temeljeni na bioizosterima purina za ispitivanje njihovih antitumorskih i antipatogenih djelovanja (PurBioCaPa) (Raić-Malić, Silvana, HRZZ - 2018-01) ( CroRIS)