novel linezolid like analogues: synthesis, characterization and biological evaluation
نویسندگان
چکیده
the synthesis of 4-(substituted benzylidene)-2-(pyrazin-2-yl) oxazol-5(4h)-one was achieved in two steps, in first step, pyrazine-2-carboxamide dissolved in etoh, 10% koh solution with clch2cooh produced compound 2-(pyrazine-2-carboxamido) acetic acid (ii) and in second step, compound (ii) in (ch3co)2o with aromatic aldehyde, and catalyst potassium acetate produced title compounds 4-(substituted benzylidene)-2-(pyrazin-2-yl) oxazol-5(4h)-one (pa1-pa14). all the newly synthesized compounds structure were elucidated using various spectral techniques viz. ft-ir, 1h-nmr, gc-ms spectroscopy, and chn elemental analysis data and screened for in vitro antimicrobial and antifungal activity. in vitro anti bacterial activity was carried out against organisms e.coli, k.pneumonia, s.aureus, and b. subtilis as well as antifungal activity were carried out against a.niger and s.cerevisiae activity byminimum inhibitory concentration method. the most promising broad spectrum compounds pa3, pa4, and pa5 were observed and study data reveals that additions of different functional groups had varying effects on activity. in addition, the greater biological activities were observed when the electron-withdrawing groups like fluorine, bromine and chlorine were incorporated at p-position of the phenyl ring.
منابع مشابه
Novel Linezolid like Analogues: Synthesis, Characterization and Biological Evaluation
The synthesis of 4-(substituted benzylidene)-2-(pyrazin-2-yl) oxazol-5(4H)-one was achieved in two steps, In first step, pyrazine-2-carboxamide dissolved in EtOH, 10% KOH solution with ClCH2COOH produced compound 2-(pyrazine-2-carboxamido) acetic acid (II) and in second step, compound (II) in (CH3CO)2O with aromatic aldehyde, and catalyst potassium ace...
متن کاملDesign, Synthesis and Biological Evaluation of Novel Peptide-Like Analogues as Selective COX-2 Inhibitors
A new series of peptide-like derivatives containing different aromatic amino acids andpossessing pharmacophores of COX-2 inhibitors as SO2Me or N3 attached to the para positionof an end phenyl ring was synthesized for evaluation as selective cyclooxygenase-2 (COX-2)inhibitors. The synthetic reactions were based on the solid phase peptide synthesis methodusing Wang resin. One of the analogues, i...
متن کاملDesign, Synthesis and Biological Evaluation of Novel Peptide-Like Analogues as Selective COX-2 Inhibitors
A new series of peptide-like derivatives containing different aromatic amino acids andpossessing pharmacophores of COX-2 inhibitors as SO2Me or N3 attached to the para positionof an end phenyl ring was synthesized for evaluation as selective cyclooxygenase-2 (COX-2)inhibitors. The synthetic reactions were based on the solid phase peptide synthesis methodusing Wang resin. One of the analogues, i...
متن کاملSynthesis and biological evaluation of novel PDMP analogues.
A new series of hybrid PDMP analogues, based both on PDMP and styryl analogues of natural ceramide, has been synthesized from D-serine. The synthetic route was developed such that future introduction of different aryl groups is straightforward. Biological evaluation, both in vitro on rat liver Golgi fractions as well as in HEK-293 and COS-7 cells, revealed two lead compounds with comparable inh...
متن کاملsynthesis and characterization of potentially biological active cyclometallated organoplatinum(ii) complexes
this work is presented in five parts. in the first part preparation of the starting complex [pt(c^n)cl(dmso)], 1, in which c^n = n(1),c(2?)-chelated, deprotonated 2-phenylpyridine, and dmso = dimethylsulfoxide, and its reaction with 1 equiv of the biphosphine ligands bis(diphenylphosphino)amine, dppa, or bis(diphenylphosphino)methane, dppm, to give the complex [pt(c^n)cl(dppa)], 2, or [pt(c^n)c...
15 صفحه اولTotal synthesis and biological evaluation of neodysiherbaine A and analogues.
Dysiherbaine (1) and its congener neodysiherbaine A (2) are naturally occurring excitatory amino acids with selective and potent agonistic activity for ionotropic glutamate receptors. We describe herein the total synthesis of 2 and its structural analogues 3-8. Advanced key intermediate 16 was employed as a branching point to assemble a series of these analogues 3-8 with respect to the C8 and C...
متن کاملمنابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
عنوان ژورنال:
iranian journal of pharmaceutical sciencesجلد ۱۰، شماره ۲، صفحات ۶۹-۷۸
میزبانی شده توسط پلتفرم ابری doprax.com
copyright © 2015-2023