Current Advances in Antitubercular Drug Discovery: Potent Prototypes and New Targets

Author(s)

dos Santos Fernandes, Guilherme Felipe ^[1] ; Jornada, Daniela Hartmann ^[1] ; de Souza, Paula Carolina ^[1] ; Chin, Chung Man ^[1] ; Pavan, Fernando Rogerio ^[1] ; dos Santos, Jean Leandro ^[1]

Affiliation

^[1] Univ Estadual Paulista, UNESP, Fac Ciencias Farmaceut, Araraquara - Brazil

• Document type: Journal article
• Source: Current Medicinal Chemistry; v. 22, n. 27, p. 3133-3161, 2015.
• Web of Science Citations: 7

Abstract

Tuberculosis (TB) is an infectious disease caused by bacterium of the Mycobacterium genus, mainly by Mycobacterium tuberculosis (MTB). The World Health Organization aims to substantially reduce the number of cases in the coming years; however, the increased number of multidrug-resistant (MDR) and extremely drug-resistant (XDR) forms of the bacterium and the lack of treatment for latent tuberculosis are challenges to be overcome. In this review, we have identified the most potent compounds described in the literature during recent years with MIC values <7 mu M, low toxicity and a high selective index. In addition, emerging targets in MTB are presented to provide new perspectives for the discovery of new antitubercular drugs. This review aims to summarize the current advances in and promote insights into antitubercular drug discovery. (AU)

• FAPESP's process: 14/24811-0 - Design and synthesis of new 1,4-di-N-oxide quinoxaline as antitubercular compounds to treat multi drug-resistant (MDR) and latent tuberculosis
• Grantee: Guilherme Felipe dos Santos Fernandes
• Support Opportunities: Scholarships abroad - Research Internship - Master's degree
• FAPESP's process: 14/02240-1 - Design, Synthesis and anti Mycobacterium tuberculosis activity of new N-oxides derivatives
• Grantee: Guilherme Felipe dos Santos Fernandes
• Support Opportunities: Scholarships in Brazil - Master
• FAPESP's process: 13/14957-5 - Research potential against tuberculosis of a new class of furoxan compounds and nanostructured compounds of the ruthenium(II) and copper (II)
• Grantee: Fernando Rogério Pavan
• Support Opportunities: Research Grants - Young Investigators Grants