2689-39-6Relevant articles and documents
One-pot synthesis and biological evaluation of novel 4-[3-fluoro-4-(morpholin-4-yl)]phenyl-1H-1,2,3-triazole derivatives as potent antibacterial and anticancer agents
Narsimha, Sirassu,Nukala, Sathesh Kumar,Ravinder, M.,Savitha Jyostna, T.,Srinivasa Rao, M.,Vasudeva Reddy, N.
, (2020)
In search of better antibacterial and anticancer agents, a series of novel 4-[3-fluoro-4-(morpholin-4-yl)]phenyl-1H-1,2,3-triazole derivatives were synthesized (6a-l and 8a-j) by using 3-fluoro-4-morpholinoaniline, alkyne, and triflyl azide via an in situ
Novel Linezolid analogues with antiparasitic activity against Hymenolepis nana
Alcántar-Zavala, Eleazar,Hernández-Guevara, Esteban,Ochoa-Terán, Adrián,Montes-ávila, Julio,Estrada-Zavala, Edgar A.,Salazar-Medina, Alex J.,Alday, Efraín,Cabrera, Alberto,Aguirre, Gerardo,Miranda-Soto, Valentín,Velazquez, Carlos,Díaz-Camacho, Sylvia P.,Medina-Franco, José L.
, (2020)
The stereoselective synthesis and anti- Hymenolepis nana activity of six Linezolid-type compounds, obtained by chemical modification of L-Alanine, are reported in this work. The synthetic strategy was to prepare diasteromeric N,N-dibenzylamino oxazolidino
Biofilm inhibition of linezolid-like Schiff bases: Synthesis, biological activity, molecular docking and in silico ADME prediction
Sangshetti, Jaiprakash N.,Khan, Firoz A. Kalam,Patil, Rajendra H.,Marathe, Sayali D.,Gade, Wasudev N.,Shinde, Devanand B.
, p. 874 - 880 (2015)
Herein, we report the synthesis and screening of linezolid-like Schiff bases as inhibitors of biofilm formation. The result of biofilm inhibition of Pseudomonas aeruginosa suggested that compounds 5h (IC50 value = 12.97 ± 0.33 μM) and 5i (IC50 value = 15.63 ± 0.20 μM) had more inhibitory activity when compared with standard linezolid (IC50 = 15.93 ± 0.18 μM) without affecting the growth of cells (and thus behave as anti-quorum sensing agents). The compounds 5h (MIC range = 2.5-10 μg/mL) and 5i (MIC range = 3.5-10 μg/mL) with 2-chloroquinolinyl and 2-chloro-8-methylquinolinyl motif, respectively, showed antibacterial activity in comparable range of linezolid (MIC range = 2-3 μg/mL) and were more potent when compared with ciprofloxacin (MIC range = 25-50 μg/mL). Thus, the active derivatives were not only potent inhibitors of P. aeruginosa biofilm growth but also efficient antibacterial agents. The docking study of most active compounds 5h and 5i against PqsD enzyme of P. aeruginosa exhibited good binding properties. In silico ADME properties of synthesized compounds were also analyzed and showed potential to develop as good oral drug candidates.
Benzofuroxan Derivatives as Potent Agents against Multidrug-Resistant Mycobacterium tuberculosis
Fernandes, Guilherme F. S.,Campos, Débora L.,Da Silva, Isabel C.,Prates, Jo?o L. B.,Pavan, Aline R.,Pavan, Fernando R.,Dos Santos, Jean L.
supporting information, p. 1268 - 1282 (2021/02/16)
Tuberculosis (TB) is currently the leading cause of death related to infectious diseases worldwide, as reported by the World Health Organization. Moreover, the increasing number of multidrug-resistant tuberculosis (MDR-TB) cases has alarmed health agencies, warranting extensive efforts to discover novel drugs that are effective and also safe. In this study, 23 new compounds were synthesized and evaluated in vitro against the drug-resistant strains of M. tuberculosis. The compound 6-((3-fluoro-4-thiomorpholinophenyl)carbamoyl)benzo[c][1,2,5]oxadiazole 1-N-oxide (5 b) was particularly remarkable in this regard as it demonstrated MIC90 values below 0.28 μM against all the MDR strains evaluated, thus suggesting that this compound might have a different mechanism of action. Benzofuroxans are an attractive new class of anti-TB agents, exemplified by compound 5 b, with excellent potency against the replicating and drug-resistant strains of M. tuberculosis.
