Antimalarial Activity of Piperidine Alkaloids fromSenna spectabilisand Semisynthetic Derivatives

Mass spectrometry for characterization of homologous piperidine alkaloids and their activity as acetylcholinesterase inhibitors

“…Among these species, Senna spectabilis (syn. Cassia spectabilis ) is a source of rare piperidine alkaloids, which display various biological activities, including cytotoxic, antimicrobial, antimalarial, leishmanicidal, and anticholinesterase action.…”

“…To identify antimalarial prototypes, the piperidine alkaloids 1 and 2 isolated from S. spectabilis flowers and the semisynthetic derivatives 3 and 4 have been screened against a culture of Plasmodium falciparum ‐infected red blood cells. The natural compound 1 , with shorter side chain, proved to be more effective against the parasite . In fact, addition of one or more methylene groups to a bioactive molecule may change its physicochemical and stereoelectronic properties and hence affect its pharmacological profile …”

“…The natural compound 1, with shorter side chain, proved to be more effective against the parasite. 5 In fact, addition of one or more methylene groups to a bioactive molecule may change its physicochemical and stereoelectronic properties and hence affect its pharmacological profile. 11 Taking all these data into consideration, piperidine alkaloids constitute a rare class of natural products that exhibit a broad spectrum of biological activities.…”

Design, Synthesis, and Fungicidal Activity of Novel Thiosemicarbazide Derivatives Containing Piperidine Fragments

“…Heterocyclic compounds have received considerable attention in recent years owing to their broad bioactivities and have become of significant importance in industry and biology [ 19 ]. As a saturated heterocyclic, piperidine is a cyclic secondary amine that has been frequently reported for its multiple activities, such as anti-HIV [ 20 ], histamine H 3 R ligands ( Figure 2 A) [ 21 ], antimalarial [ 22 ], antimicrobial [ 23 ], antifungal ( Figure 2 B) [ 24 ], anticoagulant [ 25 ], and other biological properties [ 26 ]. For instance, oxathiapiprolin ( Figure 2 C), the first member of the piperidinyl thiazole isoxazoline fungicides developed globally as DuPont™ Zorvec™, can control plant diseases caused by oomycete pathogens in different stages of the pathogen’s life cycle at extremely low concentrations [ 27 ].…”

Paradigmas Do Ensino: Abordagem Na Farmacoterapia Da Septicemia Em Laboratório De Simulação Realística No 7º Semestre Do Curso De Medicina Através De Práticas Pedagógicas Ativas

“…Os alcaloides 1 e 10 exibiram forte atividade frente ao Plasmodium falciparum, enquanto que os seus derivados acetilados (-)-3-O-acetilcassina (2) e (-)-3-O-acetilespectalina (6) foram menos ativos comparados ao controle positivo cloroquina. Os resultados sugeriram que a acetilação da hidroxila na posição C-3 reduz a atividade antimalárica desses compostos (PIVATTO et al, 2014;VIEGAS JÚNIOR et al, 2004). Esta atividade também foi relatada para os alcaloides cassiarina A (34), isolado das folhas e galho de S. siamea, e cassiarina C (36), D (37), E (41), G (42), H (43), J (44), K (45) e F (46), isolados das flores desta espécie (DEGUCHI et al, 2011(DEGUCHI et al, , 2012OSHIMI et al, 2009).…”