Title |
The 4-aminopiperidine series has limited anti-tubercular and anti-staphylococcus aureus activity
|
---|---|
Published in |
Journal of Negative Results in BioMedicine, February 2015
|
DOI | 10.1186/s12952-015-0024-x |
Pubmed ID | |
Authors |
N Susantha Chandrasekera, Torey Alling, Mai Bailey, Aaron Korkegian, James Ahn, Yulia Ovechkina, Joshua Odingo, Tanya Parish |
Abstract |
Tuberculosis (TB) caused by Mycobacterium tuberculosis is the leading cause of death from a bacterial infection. The 4-aminopiperidine (PIP) series has been reported as having anti-bacterial activity against M. tuberculosis. We explored this series for its potential to inhibit aerobic growth of M. tuberculosis. We examined substitution at the N-1 position and C-4 position of the piperidine and modifications of the piperidine moiety systematically to delineate structure-activity relationships influencing potency. Compounds were tested for growth-inhibitory activity against virulent M. tuberculosis. A selected set of compounds were also tested for its activity against Staphylococcus aureus. The compound with a norbornenylmethyl substituent at the N-1 position and N-benzyl-N-phenethylamine at the C-4 position of the piperidine (1) was the only active compound with a minimum inhibitory concentration (MIC) of 10 μM against M. tuberculosis. Compounds were not active against S. aureus. We were unable to derive any other analogs with MIC < 20 μM against M. tuberculosis. Therefore we conclude that the lack of activity is a liability in this series precluding it from further development. |
X Demographics
Geographical breakdown
Country | Count | As % |
---|---|---|
United States | 1 | 50% |
Unknown | 1 | 50% |
Demographic breakdown
Type | Count | As % |
---|---|---|
Members of the public | 2 | 100% |
Mendeley readers
Geographical breakdown
Country | Count | As % |
---|---|---|
Unknown | 24 | 100% |
Demographic breakdown
Readers by professional status | Count | As % |
---|---|---|
Student > Bachelor | 4 | 17% |
Researcher | 4 | 17% |
Student > Postgraduate | 3 | 13% |
Student > Master | 3 | 13% |
Student > Doctoral Student | 1 | 4% |
Other | 3 | 13% |
Unknown | 6 | 25% |
Readers by discipline | Count | As % |
---|---|---|
Medicine and Dentistry | 7 | 29% |
Immunology and Microbiology | 4 | 17% |
Biochemistry, Genetics and Molecular Biology | 2 | 8% |
Arts and Humanities | 1 | 4% |
Environmental Science | 1 | 4% |
Other | 1 | 4% |
Unknown | 8 | 33% |