Literature DB >> 27025339

Synthesis and molecular modeling of antimicrobial active fluoroquinolone-pyrazine conjugates with amino acid linkers.

Siva S Panda1, Oleksandr S Detistov2, Adel S Girgis3, Prabhu P Mohapatra4, Ahmed Samir5, Alan R Katritzky2.   

Abstract

Novel fluoroquinolone-pyrazine conjugates 7a-h with amino acid linkers were synthesized in good yields utilizing benzotriazole chemistry. Antimicrobial bioassay showed that the synthesized bis-conjugates have antimicrobial properties comparable to the parent drugs. Compound 7h showed superior antibacterial activity against Staphylococcus aureus and Streptococcus pyogenes (MIC=74.6 μM and 149.3 μM, respectively). This matched well with the estimated values obtained from 3D-pharmacophore and 2D-QSAR studies (MIC=67 μM and 92.9 μM, respectively).
Copyright © 2016 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Antibiotics; Benzotriazole chemistry; Computational studies; Conjugates

Mesh：

Substances：

Year:  2016        PMID： 27025339     DOI： 10.1016/j.bmcl.2016.03.062

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  8 in total

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Authors:  Adel S Girgis; Altaf H Basta; Houssni El-Saied; Mohamed A Mohamed; Ahmad H Bedair; Ahmad S Salim
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5.  Synthesis, Antibacterial Evaluation, and Computational Studies of a Diverse Set of Linezolid Conjugates.

Authors:  Riham M Bokhtia; Adel S Girgis; Tarek S Ibrahim; Fatma Rasslan; Eman S Nossier; Reham F Barghash; Rajeev Sakhuja; Eatedal H Abdel-Aal; Siva S Panda; Amany M M Al-Mahmoudy
Journal:  Pharmaceuticals (Basel)       Date:  2022-02-03

6.  Synthesis, computational studies, antimycobacterial and antibacterial properties of pyrazinoic acid-isoniazid hybrid conjugates.

Authors:  Siva S Panda; Adel S Girgis; Bibhuti B Mishra; Mohamed Elagawany; Venkatasai Devarapalli; William F Littlefield; Ahmed Samir; Walid Fayad; Nehmedo G Fawzy; Aladdin M Srour; Riham M Bokhtia
Journal:  RSC Adv       Date:  2019-07-01       Impact factor: 4.036

7.  Facile synthetic approach towards vasorelaxant active 4-hydroxyquinazoline-4-carboxamides.

Authors:  Marian N Aziz; Siva S Panda; ElSayed M Shalaby; Nehmedo G Fawzy; Adel S Girgis
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8.  Cephem-Pyrazinoic Acid Conjugates: Circumventing Resistance in Mycobacterium tuberculosis.

Authors:  Malcolm S Cole; Michael D Howe; Joseph A Buonomo; Sachin Sharma; Elise A Lamont; Scott I Brody; Neeraj K Mishra; Yusuke Minato; Joshua M Thiede; Anthony D Baughn; Courtney C Aldrich
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  8 in total

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