Synthesis of 3-tetrazolylmethyl-4H-chromen-4-ones via Ugi-azide and biological evaluation against Entamoeba histolytica, Giardia lamblia and Trichomona vaginalis.
The synthesis of novel 3-tetrazolylmethyl-4H-chromen-4-ones via an Ugi-azide multicomponent reaction and their biological evaluation against Entamoeba histolytica, Giardia lamblia and Trichomona vaginalis are described. Reported yields are moderate to good and biological results show that these compounds could be considered as candidates to anti-parasitic drugs, especially against G. lamblia.
Departamento de Química, DCNE, Universidad de Guanajuato, Noria Alta S/N, Guanajuato C.P. 36050, Guanajuato, Mexico.
Pedro A
PA
Cano
Departamento de Química, DCNE, Universidad de Guanajuato, Noria Alta S/N, Guanajuato C.P. 36050, Guanajuato, Mexico.
Alejandro
A
Islas-Jácome
Unidad Profesional Interdisciplinaria de Ingeniería, Instituto Politécnico Nacional, Av. Mineral de Valenciana 200, Col. Fracc. Industrial Puerto Interior, Silao de la Victoria C.P. 36275, Guanajuato, Mexico.
Joaquín
J
González-Marrero
Unidad de Investigación Médica en Enfermedades Infecciosas y Parasitarias, UMAE, Hospital de Pediatría, Centro Médico Nacional Siglo XXI, IMSS, Av. Cuauhtémoc No. 330, Col. Doctores, C.P. 06725 México DF, Mexico.
Lilian
L
Yépez-Mulia
Unidad de Investigación Médica en Farmacología, UMAE, Hospital de Especialidades, 2do Piso, CORSE, Centro Médico Nacional Siglo XXI, IMSS, Av. Cuauhtémoc No. 330, Col. Doctores, C.P. 06725 México DF, Mexico.
Fernando
F
Calzada
Departamento de Química, DCNE, Universidad de Guanajuato, Noria Alta S/N, Guanajuato C.P. 36050, Guanajuato, Mexico. Electronic address: rociogm@ugto.mx.
Rocío
R
Gámez-Montaño
D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000981:Antiprotozoal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001386:Azides / Q000737:chemistry*; D001578:Benzopyrans / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D018360:Crystallography, X-Ray; D004748:Entamoeba histolytica / Q000187:drug effects*; D016829:Giardia lamblia / Q000187:drug effects*; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D008968:Molecular Conformation; D013329:Structure-Activity Relationship; D014246:Trichomonas vaginalis / Q000187:drug effects*
D000890:Anti-Infective Agents; D000981:Antiprotozoal Agents; D001386:Azides; D001578:Benzopyrans
1,5-Disubstituted-1H-tetrazoles; 3-Substituted-chromen-4-ones; Anti-parasitic drug; Half maximal inhibitory concentration; Ugi-azide