دورية أكاديمية
Identification of pyrrolo-pyridine derivatives as novel class of antibacterials.
| العنوان: | Identification of pyrrolo-pyridine derivatives as novel class of antibacterials. |
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| المؤلفون: | Veselov MS; Institute of Biochemistry and Genetics Russian Academy of Science (IBG RAS) Ufa Scientific Centre, Oktyabrya Prospekt 71, Ufa, Russian Federation, 450054. mark.veselov@phystech.edu.; Moscow Institute of Physics and Technology (State University), 9 Institutskiy Lane, Dolgoprudny City, Moscow Region, Russian Federation, 141700. mark.veselov@phystech.edu.; Skolkovo Institute of Science and Technology, Skolkovo, Russian Federation. mark.veselov@phystech.edu., Ivanenkov YA; Institute of Biochemistry and Genetics Russian Academy of Science (IBG RAS) Ufa Scientific Centre, Oktyabrya Prospekt 71, Ufa, Russian Federation, 450054.; Moscow Institute of Physics and Technology (State University), 9 Institutskiy Lane, Dolgoprudny City, Moscow Region, Russian Federation, 141700.; Chemistry Department, Lomonosov Moscow State University, Leninskie Gory, Building 1/3 GSP-1, Moscow, Russian Federation, 119991.; Skolkovo Institute of Science and Technology, Skolkovo, Russian Federation.; ChemDiv, 6605 Nancy Ridge Drive, San Diego, CA, 92121, USA., Yamidanov RS; Institute of Biochemistry and Genetics Russian Academy of Science (IBG RAS) Ufa Scientific Centre, Oktyabrya Prospekt 71, Ufa, Russian Federation, 450054., Osterman IA; Chemistry Department, Lomonosov Moscow State University, Leninskie Gory, Building 1/3 GSP-1, Moscow, Russian Federation, 119991.; Skolkovo Institute of Science and Technology, Skolkovo, Russian Federation., Sergiev PV; Department of Chemistry and A.N. Belozersky Institute of Physico-Chemical Biology, Lomonosov Moscow State University, Moscow, Russian Federation.; Skolkovo Institute of Science and Technology, Skolkovo, Russian Federation., Aladinskiy VA; Moscow Institute of Physics and Technology (State University), 9 Institutskiy Lane, Dolgoprudny City, Moscow Region, Russian Federation, 141700.; Skolkovo Institute of Science and Technology, Skolkovo, Russian Federation., Aladinskaya AV; Moscow Institute of Physics and Technology (State University), 9 Institutskiy Lane, Dolgoprudny City, Moscow Region, Russian Federation, 141700.; Skolkovo Institute of Science and Technology, Skolkovo, Russian Federation., Terentiev VA; Institute of Biochemistry and Genetics Russian Academy of Science (IBG RAS) Ufa Scientific Centre, Oktyabrya Prospekt 71, Ufa, Russian Federation, 450054.; Moscow Institute of Physics and Technology (State University), 9 Institutskiy Lane, Dolgoprudny City, Moscow Region, Russian Federation, 141700.; Skolkovo Institute of Science and Technology, Skolkovo, Russian Federation., Ayginin AA; Institute of Biochemistry and Genetics Russian Academy of Science (IBG RAS) Ufa Scientific Centre, Oktyabrya Prospekt 71, Ufa, Russian Federation, 450054.; Moscow Institute of Physics and Technology (State University), 9 Institutskiy Lane, Dolgoprudny City, Moscow Region, Russian Federation, 141700., Skvortsov DA; Department of Chemistry and A.N. Belozersky Institute of Physico-Chemical Biology, Lomonosov Moscow State University, Moscow, Russian Federation., Komarova KS; Department of Chemistry and A.N. Belozersky Institute of Physico-Chemical Biology, Lomonosov Moscow State University, Moscow, Russian Federation.; Skolkovo Institute of Science and Technology, Skolkovo, Russian Federation., Chemeris AV; Institute of Biochemistry and Genetics Russian Academy of Science (IBG RAS) Ufa Scientific Centre, Oktyabrya Prospekt 71, Ufa, Russian Federation, 450054., Baimiev AK; Institute of Biochemistry and Genetics Russian Academy of Science (IBG RAS) Ufa Scientific Centre, Oktyabrya Prospekt 71, Ufa, Russian Federation, 450054., Sofronova AA; Faculty of Bioengineering and Bioinformatics, Lomonosov Moscow State University, Moscow, Russian Federation., Machulkin AE; Chemistry Department, Lomonosov Moscow State University, Leninskie Gory, Building 1/3 GSP-1, Moscow, Russian Federation, 119991., Petrov RA; Chemistry Department, Lomonosov Moscow State University, Leninskie Gory, Building 1/3 GSP-1, Moscow, Russian Federation, 119991., Maklakova SY; Chemistry Department, Lomonosov Moscow State University, Leninskie Gory, Building 1/3 GSP-1, Moscow, Russian Federation, 119991., Bezrukov DS; Skolkovo Institute of Science and Technology, Skolkovo, Russian Federation., Filkov GI; Moscow Institute of Physics and Technology (State University), 9 Institutskiy Lane, Dolgoprudny City, Moscow Region, Russian Federation, 141700., Zainullina LF; Institute of Biochemistry and Genetics Russian Academy of Science (IBG RAS) Ufa Scientific Centre, Oktyabrya Prospekt 71, Ufa, Russian Federation, 450054., Maximova MA; Institute of Biochemistry and Genetics Russian Academy of Science (IBG RAS) Ufa Scientific Centre, Oktyabrya Prospekt 71, Ufa, Russian Federation, 450054., Zileeva ZR; Institute of Biochemistry and Genetics Russian Academy of Science (IBG RAS) Ufa Scientific Centre, Oktyabrya Prospekt 71, Ufa, Russian Federation, 450054., Kartsev VG; InterBioScreen Ltd, Chernogolovka, Moscow Region, Russian Federation., Vakhitova YV; Institute of Biochemistry and Genetics Russian Academy of Science (IBG RAS) Ufa Scientific Centre, Oktyabrya Prospekt 71, Ufa, Russian Federation, 450054., Dontsova OA; Chemistry Department, Lomonosov Moscow State University, Leninskie Gory, Building 1/3 GSP-1, Moscow, Russian Federation, 119991.; Department of Chemistry and A.N. Belozersky Institute of Physico-Chemical Biology, Lomonosov Moscow State University, Moscow, Russian Federation.; Skolkovo Institute of Science and Technology, Skolkovo, Russian Federation. |
| المصدر: | Molecular diversity [Mol Divers] 2020 Feb; Vol. 24 (1), pp. 233-239. Date of Electronic Publication: 2019 Apr 04. |
| نوع المنشور: | Journal Article |
| اللغة: | English |
| بيانات الدورية: | Publisher: ESCOM Science Publishers Country of Publication: Netherlands NLM ID: 9516534 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1573-501X (Electronic) Linking ISSN: 13811991 NLM ISO Abbreviation: Mol Divers Subsets: MEDLINE |
| أسماء مطبوعة: | Original Publication: Leiden, The Netherlands : ESCOM Science Publishers, c1995- |
| مواضيع طبية MeSH: | Anti-Bacterial Agents/*chemistry , Anti-Bacterial Agents/*pharmacology , Indolizines/*chemistry , Pyridines/*chemistry, Cell Survival ; Drug Evaluation, Preclinical ; High-Throughput Screening Assays ; Microbial Sensitivity Tests ; Structure-Activity Relationship |
| مستخلص: | A series of 5-oxo-4H-pyrrolo[3,2-b]pyridine derivatives was identified as novel class of highly potent antibacterial agents during an extensive large-scale high-throughput screening (HTS) program utilizing a unique double-reporter system-pDualrep2. The construction of the reporter system allows us to perform visual inspection of the underlying mechanism of action due to two genes-Katushka2S and RFP-which encode the proteins with different imaging signatures. Antibacterial activity of the compounds was evaluated during the initial HTS round and subsequent rescreen procedure. The most active molecule demonstrated a MIC value of 3.35 µg/mL against E. coli with some signs of translation blockage (low Katushka2S signal) and no SOS response. The compound did not demonstrate cytotoxicity in standard cell viability assay. Subsequent structural morphing and follow-up synthesis may result in novel compounds with a meaningful antibacterial potency which can be reasonably regarded as an attractive starting point for further in vivo investigation and optimization. |
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| معلومات مُعتمدة: | 20.9907.2017/VU Ministry of Education and Science of the Russian Federation; №17-74-30012 Russian Science Foundation |
| فهرسة مساهمة: | Keywords: Antibacterial compounds; Antibiotics; HTS; MIC; Ribosome; SOS response; Translation inhibition |
| المشرفين على المادة: | 0 (Anti-Bacterial Agents) 0 (Indolizines) 0 (Pyridines) 274-40-8 (indolizine) |
| تواريخ الأحداث: | Date Created: 20190406 Date Completed: 20201013 Latest Revision: 20201013 |
| رمز التحديث: | 20240628 |
| DOI: | 10.1007/s11030-019-09946-3 |
| PMID: | 30949901 |
| قاعدة البيانات: | MEDLINE |
Find this article in full text from Springer Verlag. 
Full Text Finder | تدمد: | 1573-501X |
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| DOI: | 10.1007/s11030-019-09946-3 |