Dual-protected amino acid derivatives as new antitubercular agents.
Pedro Pôssa de CastroDébora L CamposFernando R PavanGiovanni Wilson AmarantePublished in: Chemical biology & drug design (2018)
Tuberculosis is an infectious disease with high incidence and growing drug-resistant rates. In an attempt to develop new antitubercular agents, 35 compounds were synthesized, most of them bearing a carbamate and enantiopure amino acid moiety. These compounds had their activity evaluated toward a Mycobacterium tuberculosis strain (ATCC 27294) and cytotoxicity against fibroblast MRC-5 cells (ATCC CCL-171). Three of the prepared derivatives presented a good antimicrobial inhibition and two of them a moderate cytotoxicity. The lipophilicity seems to play a vital role in the cell growth activity, with best results for the derivatives with a higher logP.
Keyphrases
- drug resistant
- amino acid
- mycobacterium tuberculosis
- infectious diseases
- multidrug resistant
- acinetobacter baumannii
- induced apoptosis
- pulmonary tuberculosis
- staphylococcus aureus
- cell cycle arrest
- risk factors
- structure activity relationship
- signaling pathway
- cell death
- liver fibrosis
- cystic fibrosis
- pseudomonas aeruginosa
- hepatitis c virus