New (−)−Cytisine Derivatives with Nootropic Activity

Study of the Analgesic Activity Of(s)-1-Methyl-3-(1-(5-Phenyl Isoxazole-3-Carbonyl) Piperidine-2-Il) Pyridine-1-Ium Iodide

“…Ажыратымдылығы жоғары масс-спектрлер DFS ThermoScientific масс-спектрометрінде зерттелді (буландырғыш температурасы 200-250°С, электронды әсер ету ионизациясы, 70 эВ). Mettler Toledo FP 900 терможүйесінде балқу температурасы анықталды [6].…”

Semisynthesis of novel N‐acyl/sulfonyl derivatives of 5(3,5)‐(di)halogenocytisines/cytisine and their pesticidal activities against Mythimna separata Walker, Tetranychus cinnabarinus Boisduval, and Sitobion avenae Fabricius

“…), isolated from plants of the family Leguminosae, is a prevalent quinolizidine alkaloid. Cytisine and its derivatives exhibit a variety of biological properties such as antineoplastic, anti‐inflammatory and nootropic activity, they are agonists of α4β2 nicotinic acetylcholine receptors, inhibitors of hydroxysteroid 17‐β‐dehydrogenase‐4, inhibitors of the menin–mixed lineage leukemia (MLL) interaction, and show insecticidal activity . However, we previously investigated halogenation of the E‐ring of podophyllotoxins and prepared a series of 4α‐acyloxy‐2′(2′,6′)‐(di)halogenopodophyllotoxins ( I , Fig.…”

“…Cytisine and its derivatives exhibit a variety of biological properties such as antineoplastic, anti-inflammatory and nootropic activity, they are agonists of 4 2 nicotinic acetylcholine receptors, inhibitors of hydroxysteroid 17--dehydrogenase-4, inhibitors of the menin-mixed lineage leukemia (MLL) interaction, and show insecticidal activity. [17][18][19][20][21][22][23][24][25] However, we previously investigated halogenation of the E-ring of podophyllotoxins and prepared a series of 4 -acyloxy-2 ′ (2 ′ ,6 ′ )-(di)halogenopodophyllotoxins (I, Fig. 1), 26 2 -chloro-4 -acyloxy-2 ′ (2 ′ ,6 ′ )-(di)halogenopicropodophyllotoxins (II, Fig.…”

Synthesis of N-Arylcytisine Derivatives Using the Copper-Catalyzed Chan-Lam Coupling

“…This has often been achieved with more or less complex substituted alkyl groups, including benzyl substituents, by nucleophilic substitution using alkyl or benzyl halides 29 to relevant biological activities. 30 Cytisine (sometimes substituted on the pyridone ring) has been used as the amine component in Mannich reactions of phenolic natural products and for the obtention of N 3 -benzimidazole and -benzothiazole derivatives. 31 N 3 -Acylcytisines are another small group, including sulfonyl-, carbamyl-, and thiocarbamyl derivatives, and N 3 -acyl amino-acid derivatives have been reported reacting cytisine with methyl esters of amino-acid isocyanates.…”

“…Aside from the well-known pyridone ring-halogenated and nitrated derivatives, further modifications of these, including N -substitution, an unusual aza-Michael reaction, and an aliphatic bridge arylation, , most described cytisine derivatives are substituted on the amine nitrogen N 3 . This has often been achieved with more or less complex substituted alkyl groups, including benzyl substituents, by nucleophilic substitution using alkyl or benzyl halides in some cases leading to relevant biological activities . Cytisine (sometimes substituted on the pyridone ring) has been used as the amine component in Mannich reactions of phenolic natural products and for the obtention of N 3 -benzimidazole and -benzothiazole derivatives …”