Tuberculosis (TB) represents a never-ending challenge toward which research efforts are needed. Drug resistance is the key problem that scientists in the field need to fight. The development of new drugs endowed with novel modes of action against different biological targets is of extreme importance; these new agents should also exhibit lower toxicity compared with the anti-TB drugs currently available. Furthermore, new drugs should be inexpensive since most of the TB-infected population lives in developing nations. In the last few years, numerous researchers have focused their attention on TB, leading to the discovery of some interesting compounds. Among these, the pyrrole-derived compounds we developed can be considered very promising antimycobacterial agents. Aided by molecular modeling studies, we synthesized numerous compounds characterized by the same 1,5-diarylpyrrole scaffold and elucidated very interesting antitubercular/antimycobacterial properties. Some compounds identified are extremely promising and represent a step towards the design of novel lead structures in the fight against TB. Our efforts to this end are reviewed here.

Biava, M., PORRETTA G., C., Poce, G., Battilocchio, C., Alfonso, S., DE LOGU, A., et al. (2011). Developing Pyrrole-Derived Antimycobacterial Agents: a Rational Lead Optimization Approach. CHEMMEDCHEM, 6(4), 593-599 [10.1002/cmdc.201000526].

Developing Pyrrole-Derived Antimycobacterial Agents: a Rational Lead Optimization Approach

MANETTI, FABRIZIO;BOTTA, MAURIZIO
2011

Abstract

Tuberculosis (TB) represents a never-ending challenge toward which research efforts are needed. Drug resistance is the key problem that scientists in the field need to fight. The development of new drugs endowed with novel modes of action against different biological targets is of extreme importance; these new agents should also exhibit lower toxicity compared with the anti-TB drugs currently available. Furthermore, new drugs should be inexpensive since most of the TB-infected population lives in developing nations. In the last few years, numerous researchers have focused their attention on TB, leading to the discovery of some interesting compounds. Among these, the pyrrole-derived compounds we developed can be considered very promising antimycobacterial agents. Aided by molecular modeling studies, we synthesized numerous compounds characterized by the same 1,5-diarylpyrrole scaffold and elucidated very interesting antitubercular/antimycobacterial properties. Some compounds identified are extremely promising and represent a step towards the design of novel lead structures in the fight against TB. Our efforts to this end are reviewed here.
Biava, M., PORRETTA G., C., Poce, G., Battilocchio, C., Alfonso, S., DE LOGU, A., et al. (2011). Developing Pyrrole-Derived Antimycobacterial Agents: a Rational Lead Optimization Approach. CHEMMEDCHEM, 6(4), 593-599 [10.1002/cmdc.201000526].
File in questo prodotto:
File Dimensione Formato  
2011ChemMedChem_Review_AntiTB.pdf

non disponibili

Tipologia: Post-print
Licenza: NON PUBBLICO - Accesso privato/ristretto
Dimensione 262.17 kB
Formato Adobe PDF
262.17 kB Adobe PDF   Visualizza/Apri   Richiedi una copia

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11365/22447
 Attenzione

Attenzione! I dati visualizzati non sono stati sottoposti a validazione da parte dell'ateneo