Novel rationally-designed benzo[b]dihydrocarbazole antimicrobial drug candidates.

Research output: Contribution to conferencePoster

Abstract

Drug-resistant infections are an emergent threats to safety to many populations, specially in the III World countries. WHO is particularly concerned about bacterial resistance among Gram negative pathogens. Previous rigid benzo[a]dihydrocarbazole showed poor antibacterial activity against Gram positive and Gram negative bacteria. The aims of this research was to sinthesise new benzo[b]carbazole structures based on tetracycline pharmacophore scaffold to enhance antimicrobial activity and to reduce toxicity associated to tetracyclines.
In patent License AR20110103126 two potential benzo[b]carbazole lead candidates have been designed by in silico modeling techniques(or skills????). The antibacterial activity was assessed against Gram positive and Gram negative bacteria. Both compounds showed antibacterial activity against Gram positive and moderate activity against Gram negative and Candida albicans at µM level (1-8 µM). In silico and in vivo toxicological activity were performed and no alerts were observed. These results suggest us that flexible compounds may open new perspectives for future antimicrobial research.
LanguageEnglish
Publication statusAccepted/In press - 19 Sep 2018
Event2nd SCI / RSC Symposium on Antimicrobial Drug Discovery -
Duration: 12 Nov 201813 Nov 2019

Conference

Conference2nd SCI / RSC Symposium on Antimicrobial Drug Discovery
Period12/11/1813/11/19

Fingerprint

Gram-Negative Bacteria
Computer Simulation
Tetracyclines
Licensure
Tetracycline
Candida albicans
Research
Pharmaceutical Preparations
Toxicology
Safety
Infection
Population
carbazole

Cite this

Cobice, D. (Accepted/In press). Novel rationally-designed benzo[b]dihydrocarbazole antimicrobial drug candidates.. Poster session presented at 2nd SCI / RSC Symposium on Antimicrobial Drug Discovery , .
Cobice, Diego. / Novel rationally-designed benzo[b]dihydrocarbazole antimicrobial drug candidates. Poster session presented at 2nd SCI / RSC Symposium on Antimicrobial Drug Discovery , .
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title = "Novel rationally-designed benzo[b]dihydrocarbazole antimicrobial drug candidates.",
abstract = "Drug-resistant infections are an emergent threats to safety to many populations, specially in the III World countries. WHO is particularly concerned about bacterial resistance among Gram negative pathogens. Previous rigid benzo[a]dihydrocarbazole showed poor antibacterial activity against Gram positive and Gram negative bacteria. The aims of this research was to sinthesise new benzo[b]carbazole structures based on tetracycline pharmacophore scaffold to enhance antimicrobial activity and to reduce toxicity associated to tetracyclines.In patent License AR20110103126 two potential benzo[b]carbazole lead candidates have been designed by in silico modeling techniques(or skills????). The antibacterial activity was assessed against Gram positive and Gram negative bacteria. Both compounds showed antibacterial activity against Gram positive and moderate activity against Gram negative and Candida albicans at µM level (1-8 µM). In silico and in vivo toxicological activity were performed and no alerts were observed. These results suggest us that flexible compounds may open new perspectives for future antimicrobial research.",
author = "Diego Cobice",
year = "2018",
month = "9",
day = "19",
language = "English",
note = "2nd SCI / RSC Symposium on Antimicrobial Drug Discovery ; Conference date: 12-11-2018 Through 13-11-2019",

}

Cobice, D 2018, 'Novel rationally-designed benzo[b]dihydrocarbazole antimicrobial drug candidates.' 2nd SCI / RSC Symposium on Antimicrobial Drug Discovery , 12/11/18 - 13/11/19, .

Novel rationally-designed benzo[b]dihydrocarbazole antimicrobial drug candidates. / Cobice, Diego.

2018. Poster session presented at 2nd SCI / RSC Symposium on Antimicrobial Drug Discovery , .

Research output: Contribution to conferencePoster

TY - CONF

T1 - Novel rationally-designed benzo[b]dihydrocarbazole antimicrobial drug candidates.

AU - Cobice, Diego

PY - 2018/9/19

Y1 - 2018/9/19

N2 - Drug-resistant infections are an emergent threats to safety to many populations, specially in the III World countries. WHO is particularly concerned about bacterial resistance among Gram negative pathogens. Previous rigid benzo[a]dihydrocarbazole showed poor antibacterial activity against Gram positive and Gram negative bacteria. The aims of this research was to sinthesise new benzo[b]carbazole structures based on tetracycline pharmacophore scaffold to enhance antimicrobial activity and to reduce toxicity associated to tetracyclines.In patent License AR20110103126 two potential benzo[b]carbazole lead candidates have been designed by in silico modeling techniques(or skills????). The antibacterial activity was assessed against Gram positive and Gram negative bacteria. Both compounds showed antibacterial activity against Gram positive and moderate activity against Gram negative and Candida albicans at µM level (1-8 µM). In silico and in vivo toxicological activity were performed and no alerts were observed. These results suggest us that flexible compounds may open new perspectives for future antimicrobial research.

AB - Drug-resistant infections are an emergent threats to safety to many populations, specially in the III World countries. WHO is particularly concerned about bacterial resistance among Gram negative pathogens. Previous rigid benzo[a]dihydrocarbazole showed poor antibacterial activity against Gram positive and Gram negative bacteria. The aims of this research was to sinthesise new benzo[b]carbazole structures based on tetracycline pharmacophore scaffold to enhance antimicrobial activity and to reduce toxicity associated to tetracyclines.In patent License AR20110103126 two potential benzo[b]carbazole lead candidates have been designed by in silico modeling techniques(or skills????). The antibacterial activity was assessed against Gram positive and Gram negative bacteria. Both compounds showed antibacterial activity against Gram positive and moderate activity against Gram negative and Candida albicans at µM level (1-8 µM). In silico and in vivo toxicological activity were performed and no alerts were observed. These results suggest us that flexible compounds may open new perspectives for future antimicrobial research.

M3 - Poster

ER -

Cobice D. Novel rationally-designed benzo[b]dihydrocarbazole antimicrobial drug candidates.. 2018. Poster session presented at 2nd SCI / RSC Symposium on Antimicrobial Drug Discovery , .