An article Novel prenyloxy chalcones as potential leishmanicidal and trypanocidal agents: Design, synthesis and evaluation WOS:000461728400027 published article about DERIVATIVES; PREVENTION; DISEASE in [Espinoza-Hicks, Jose C.; Hernandez-Rivera, Jessica L.; Camacho-Davila, Alejandro] Univ Autonoma Chihuahua, Fac Ciencias Quim, Campus Univ,Apartado Postal 669, Chihuahua, Chih, Mexico; [Fabiola Chacon-Vargas, Karla; Enid Sanchez-Torres, Luvia] Inst Politecn Nacl, Escuela Nacl Ciencias Biol, Dept Inmunol, Prolongac Carpio & Plan de Ayala S-N, Mexico City 11340, DF, Mexico; [Fabiola Chacon-Vargas, Karla; Nogueda-Torres, Benjamin] Inst Politecn Nacl, Escuela Nacl Ciencias Biol, Dept Parasitol, Prolongac Carpio & Plan de Ayala S-N, Mexico City 11340, DF, Mexico; [Tamariz, Joaquin] Inst Politecn Nacl, Escuela Nacl Ciencias Biol, Dept Quim Organ, Prolongac Carpio & Plan de Ayala S-N, Mexico City 11340, DF, Mexico in 2019.0, Cited 43.0. Category: indole-building-block. The Name is 4′-Hydroxyacetophenone. Through research, I have a further understanding and discovery of 99-93-4
The available drugs for treating Leishmaniasis and American trypanosomiasis have high toxicity and multiple side effects, among other problems. More effective and less toxic treatments are urgently needed. A series of chalcones that contained a prenyloxy or geranyloxy substituent was synthesized and characterized. Each substituent was attached to the A ring in some compounds and to the B ring in others, with additional substituents placed on the chalcone moiety. The present aim was to evaluate the effect of the substitution pattern on leishmanicidal and trypanocidal activity. When tested at a single concentration, the compounds exerting a metabolic inhibition close to or exceeding 50% for Leishmania mexicana were 11, 17 and 12, and for Trypanosoma cruzi were 11, 17, 15 and 26. Upon determining the selectivity index (SI =IC50/CC50), the values were 80.9, 1.24 and 55.12 for 11, 17 and 12 (respectively) versus L mexicana, and 75.1, 1.43, 27.36 and 33.52 for 11, 17, 15 and 26 (respectively) versus T. cruzi. Structural isomers 11 and 17 showed activity for both the L mexicana and T. cruzi strains, though the greater cytotoxic activity of 17 led to a lower SI. Compounds 12, 15 and 26 were species specific. For I cruzi, the SI was higher for 11, 15 and 26 than for the reference drugs nifurtimox and benznidazole. The examination of promastigote morphology after exposing L mexicana and T. cruzi to 11 revealed a decrease in cell density. The current findings suggest that 11 could be a useful lead compound for further SAR studies. (C) 2019 Elsevier Masson SAS. All rights reserved.
Category: indole-building-block. Welcome to talk about 99-93-4, If you have any questions, you can contact Espinoza-Hicks, JC; Chacon-Vargas, KF; Hernandez-Rivera, JL; Nogueda-Torres, B; Tamariz, J; Sanchez-Torres, LE; Camacho-Davila, A or send Email.
Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles