Synthesis and antiprotozoal activity of some 2-(trifluoromethyl)-1H-benzimidazole bioisosteres (Record no. 42047)

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fixed length control field 01925nam a2200289Ia 4500
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control field MX-MdCICY
005 - DATE AND TIME OF LATEST TRANSACTION
control field 20250625124706.0
040 ## - CATALOGING SOURCE
Transcribing agency CICY
090 ## - LOCALLY ASSIGNED LC-TYPE CALL NUMBER (OCLC); LOCAL CALL NUMBER (RLIN)
Classification number (OCLC) (R) ; Classification number, CALL (RLIN) (NR) B-7724
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245 10 - TITLE STATEMENT
Title Synthesis and antiprotozoal activity of some 2-(trifluoromethyl)-1H-benzimidazole bioisosteres
490 0# - SERIES STATEMENT
Volume/sequential designation European Journal of Medicinal Chemistry, 41(1), p.135-141, 2006
520 3# - SUMMARY, ETC.
Summary, etc. A series of 2-(trifluoromethyl)-1H-benzimidazole derivatives with various 5- and 6-position bioisosteric substituents (-Cl, -F, -CF3, -CN), namely 1-7, were prepared using a short synthetic route. Each analogue was tested in vitro against the protozoa Giardia intestinalis and Trichomonas vaginalis in comparison with albendazole and metronidazole. Several analogues had IC50 values < 1 ìM against both species, which make them significantly more potent than either standard. Compound 4 [2,5(6)-bis(trifluoromethyl)-1H-benzimidazole], was 14 times more active than albendazole against T. vaginalis. This compound (4)also showed moderate antimalarial activity against W2 and D6 strains of Plasmodium falciparum (5.98 and 6.12 ìM, respectively). Studying further structure activity relationships through the use of bioisosteric substitution in these benzimidazolic derivatives should provide new leads against protozoal and possibly malarial diseases.
650 14 - SUBJECT ADDED ENTRY--TOPICAL TERM
Topical term or geographic name entry element BENZIMIDAZOLES
650 14 - SUBJECT ADDED ENTRY--TOPICAL TERM
Topical term or geographic name entry element TRICHOMONAS VAGINALIS
650 14 - SUBJECT ADDED ENTRY--TOPICAL TERM
Topical term or geographic name entry element BIOISOSTERIC REPLACEMENT
700 12 - ADDED ENTRY--PERSONAL NAME
Personal name Navarrete-Vázquez, G.
700 12 - ADDED ENTRY--PERSONAL NAME
Personal name Rojano-Vilchis, M.M.
700 12 - ADDED ENTRY--PERSONAL NAME
Personal name Yépez-Mulia, L.
700 12 - ADDED ENTRY--PERSONAL NAME
Personal name Meléndez,V.
700 12 - ADDED ENTRY--PERSONAL NAME
Personal name Gerena,L.
700 12 - ADDED ENTRY--PERSONAL NAME
Personal name Hernández-Campos,A.
700 12 - ADDED ENTRY--PERSONAL NAME
Personal name Castillo, R.
700 12 - ADDED ENTRY--PERSONAL NAME
Personal name Castillo, R.
856 40 - ELECTRONIC LOCATION AND ACCESS
Uniform Resource Identifier <a href="https://drive.google.com/file/d/1ALfkjkGFfYhAQloPPAbY-KeXMueOQlRM/view?usp=drivesdk">https://drive.google.com/file/d/1ALfkjkGFfYhAQloPPAbY-KeXMueOQlRM/view?usp=drivesdk</a>
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Source of classification or shelving scheme Clasificación local
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  Clasificación local     Ref1 CICY CICY Documento préstamo interbibliotecario 25.06.2025   B-7724 25.06.2025 25.06.2025 Documentos solicitados