Novel N-aryl- and N-heteryl phenazine-1-carboxamides as potential agents for the treatment of infections sustained by drug-resistant and multidrug-resistant Mycobacterium tuberculosis

Logu, Alessandro De; Palchykovska, L. G.; Kostina, Valentina H.; Sanna, Angela; Meleddu, Rita; Chisu, L; Alexeeva, I. V.; Shved, A. D.

doi:10.1016/j.ijantimicag.2008.09.016

Cited by 23 publications

(16 citation statements)

References 21 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…Whereas in a series of phenazine carboxamides, compounds 85a and 85b showed excellent activity against Mtb H37Rv with a MIC of 0.19 μg/L and also against DR strains of Mtb. Most interestingly, this series was found to be nontoxic [103], validating them as future anti-TB drugs. While a macrolactone (86) derived from benzo[a]phenazine exhibited best potency against Mtb H37Rv with a MIC 0.62 μg/mL, which is better than that of RIF [104].…”

Section: Quinoline and Quinoxaline Derivativesmentioning

confidence: 57%

Recent Efforts for the Development of Antitubercular Drug Containing Diazine Ring

Asif¹

2012

Med chem

View full text Add to dashboard Cite

There has been considerable interest in the development of new molecule with antibacterial activities particularly against tuberclosis because mycobacterium species have developed resistant against currently used drugs, their toxic effect and long duration of therapy. The diazine (pyridazine, pyrimidine and piperazine) derivatives possess an important class of compound for new drugs research and development. Therefore, many researchers have synthesized these compounds as target structures and evaluated their antitubercular activity. These observations have been guiding for the development of new molecules that possess potent antitubercular activity with minimum side effects or effective against MDR, XDR mycobacterium strains, and also in patient co-infected with HIV/AIDS.

show abstract

Section: Quinoline and Quinoxaline Derivativesmentioning

confidence: 57%

Recent Efforts for the Development of Antitubercular Drug Containing Diazine Ring

Asif¹

2012

Med chem

View full text Add to dashboard Cite

show abstract

“…Phenazine derivatives are useful compounds for new anti--TB drug development, particularly Tubermicyn B and Clofazimine (phenazine analouges). Similarly, a series of 20 Quinoxaline derivatives have shown broad spectrum of biological activities. Quinoxaline--N--oxide derivatives are known as M. tuberculosis bioreductor agents.…”

Section: Non--fluoroquinolonesmentioning

confidence: 99%

“…The purine N--9 is important for activity, in the case of purine C--8, an atom can be exchanged without losing activity and a change in purine N--7 results in a loss of activity, although there are 7--deazapurines derivatives (19) that could be compared with RIF. 28 As pyrimidines have potential therapeutic applications as anti--TB agents, design of pyrimidine derivatives is a possible option (20). The nature of substituent at 2 nd position can modulate cytotoxic activity.…”

Section: Nitrogen Heterocyclic Derivativesmentioning

confidence: 99%

Antitubercular drugs: advances in nitrogen containing heterocyclic compounds and some other derivatives

Asif

2014

J PHARM CHEM

View full text Add to dashboard Cite

Tuberculosis (TB) caused by Mycobacterium tuberculosis is an infectious disease. Control of TB is complicated by difficulties in the long--course chemotherapy treatment, the inability to eliminate latent microbes, and the increasing emergence of Multidrug Resistant (MDR) strains of M. tuberculosis. New anti--TB drugs are urgently needed, including developments of short--term treatments to minimize the emergence of drug resistance and new drugs to treat multidrug resistant tuberculosis and to eliminate the latent microbes. Many new structural anti--TB agents exhibited promising activities against susceptible and resistant strains of M. tuberculosis. The diarylquinoline with superior anti--tuberculotic activity and encouraging results of nitroimidazopyrans and oxazolidinones have generated considerable excitement.

show abstract

“…The capability of 1,2,4-triazine derivatives to play the role of «universal base», capable of forming strong complexes with canonic Thy, Ade, Cyt, Gua, prompted us to perform triazine-based synthesis of the hybrid compounds with phenazine-1-carboxylic acid (PCA-1; 2) -non-nucleoside inhibitors [14]. At the same time, taking into account pharmacophoric properties of carboxamide group, we developed convenient methods of obtaining the series of N-substituted amides of triazinyl-6-propanecarboxylic acid (PCA; 3) [15,16] and N-arylamides of PCA-1 (4) [17].…”

mentioning

confidence: 99%

Synthesis and study on biological activity of nitrogen-containing heterocyclic compounds – regulators of enzymes of nucleic acid biosynthesis

Alexeeva

Shved

2013

Biopolym. Cell

View full text Add to dashboard Cite

Results of investigations on the development of new regulators of functional activity of nucleic acid biosynthesis enzymes based on polycyclic nitrogen-containing heterosystems are summarized. Computer design and molecular docking in the catalytic site of target enzyme (T7pol) allowed to perform the directed optimization of basic structures. Several series of compounds were obtained and efficient inhibitors of herpes family (simple herpes virus type 2, Epstein-Barr virus), influenza A and hepatitis C viruses were identified, as well as compounds with potent antitumor, antibacterial and antifungal activity. It was established that the use of model test systems based on enzymes participating in nucleic acids synthesis is a promising approach to the primary screening of potential inhibitors in vitro

show abstract

Novel N-aryl- and N-heteryl phenazine-1-carboxamides as potential agents for the treatment of infections sustained by drug-resistant and multidrug-resistant Mycobacterium tuberculosis

Cited by 23 publications

References 21 publications

Recent Efforts for the Development of Antitubercular Drug Containing Diazine Ring

Recent Efforts for the Development of Antitubercular Drug Containing Diazine Ring

Antitubercular drugs: advances in nitrogen containing heterocyclic compounds and some other derivatives

Synthesis and study on biological activity of nitrogen-containing heterocyclic compounds – regulators of enzymes of nucleic acid biosynthesis

Contact Info

Product

Resources

About