Synthesis and in vitro anti Mycobacterium tuberculosis activity of a series of phthalimide derivatives

Author(s)

Santos, Jean L. ^[1] ; Yamasaki, Paulo R. ^[1] ; Chin, Chung Man ^[1] ; Takashi, Celio H. ^[2] ; Pavan, Fernando R. ^[2] ; Leite, Clarice Q. F. ^[2]

Affiliation

^[1] Univ Estadual Paulista, Lapdesf Lab Pesquisa & Desenvolvimento Farmacos, Fac Ciencias Farmaceut, BR-14801902 Araraquara, SP - Brazil

^[2] Univ Estadual Paulista, Dept Ciencias Biol, Fac Ciencias Farmaceut, BR-14801902 Araraquara, SP - Brazil

• Document type: Journal article
• Source: Bioorganic & Medicinal Chemistry; v. 17, n. 11, p. 3795-3799, JUN 1 2009.
• Web of Science Citations: 52

Abstract

New phthalimide derivatives were easily prepared through condensation of phthalic anhydride and selected amines with variable yields (70-90%). All compounds (3a-l) were evaluated against Mycobacterium tuberculosis H(37)Rv using Alamar Blue susceptibility. The compounds 3c, 3i, and 3l have the minimum inhibitory concentrations (MICs) of 3.9, 7.8, and 5.0 mu/mL, respectively, and could be considered new lead compounds in the treatment of tuberculosis and multi-drug resistant tuberculosis. Crown Copyright (C) 2009 Published by Elsevier Ltd. All rights reserved. (AU)

• FAPESP's process: 07/56115-0 - Optimization, synthesis and pharmacological evaluation of dual hybrid compounds useful to treat the symptoms of sickle cell disease
• Grantee: Jean Leandro dos Santos
• Support Opportunities: Scholarships in Brazil - Doctorate
• FAPESP's process: 08/10390-2 - Determination of pre-clinical profile in vitro and in vivo anti-tuberculosis activity of ruthenium(II)phosphine / picolinate complexes
• Grantee: Fernando Rogério Pavan
• Support Opportunities: Scholarships in Brazil - Doctorate