| Title |
Rational design and synthesis of novel diphenyl ether derivatives as antitubercular agents
|
|---|---|
| Published in |
Drug Design, Development and Therapy, July 2016
|
| DOI | 10.2147/dddt.s104037 |
| Pubmed ID | |
| Authors |
Sidhartha S Kar, Varadaraj Bhat G, Praveen PN Rao, Vishnu P Shenoy, Indira Bairy, G Gautham Shenoy |
| Abstract |
A series of triclosan mimic diphenyl ether derivatives have been synthesized and evaluated for their in vitro antitubercular activity against Mycobacterium tuberculosis H37Rv. The binding mode of the compounds at the active site of enoyl-acyl carrier protein reductase of M. tuberculosis has been explored. Among them, compound 10b was found to possess antitubercular activity (minimum inhibitory concentration =12.5 µg/mL) comparable to triclosan. All the synthesized compounds exhibited low levels of cytotoxicity against Vero and HepG2 cell lines, and three compounds 10a, 10b, and 10c had a selectivity index more than 10. Compound 10b was also evaluated for log P, pKa, human liver microsomal stability, and % protein binding, in order to probe its druglikeness. Based on the antitubercular activity and druglikeness profile, it may be concluded that compound 10b could be a lead for future development of antitubercular drugs. |
X Demographics
The data shown below were collected from the profile of 1 X user who shared this research output. Click here to find out more about how the information was compiled.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| United Kingdom | 1 | 100% |
Demographic breakdown
| Type | Count | As % |
|---|---|---|
| Members of the public | 1 | 100% |
Mendeley readers
The data shown below were compiled from readership statistics for 33 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 33 | 100% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Student > Ph. D. Student | 6 | 18% |
| Other | 4 | 12% |
| Student > Bachelor | 4 | 12% |
| Researcher | 2 | 6% |
| Unspecified | 2 | 6% |
| Other | 4 | 12% |
| Unknown | 11 | 33% |
| Readers by discipline | Count | As % |
|---|---|---|
| Chemistry | 8 | 24% |
| Biochemistry, Genetics and Molecular Biology | 3 | 9% |
| Unspecified | 2 | 6% |
| Pharmacology, Toxicology and Pharmaceutical Science | 2 | 6% |
| Medicine and Dentistry | 2 | 6% |
| Other | 2 | 6% |
| Unknown | 14 | 42% |
Attention Score in Context
This research output has an Altmetric Attention Score of 1. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 04 August 2016.
All research outputs
#23,065,269
of 25,707,225 outputs
Outputs from Drug Design, Development and Therapy
#1,763
of 2,278 outputs
Outputs of similar age
#325,062
of 368,447 outputs
Outputs of similar age from Drug Design, Development and Therapy
#45
of 73 outputs
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So far Altmetric has tracked 2,278 research outputs from this source. They typically receive a little more attention than average, with a mean Attention Score of 7.3. This one is in the 1st percentile – i.e., 1% of its peers scored the same or lower than it.
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We're also able to compare this research output to 73 others from the same source and published within six weeks on either side of this one. This one is in the 1st percentile – i.e., 1% of its contemporaries scored the same or lower than it.