Synthesis, antimicrobial activity, pharmacophore analysis of some new 2-(substitutedphenyl/benzyl)-5-[(2-benzofuryl)carboxamido]benzoxazoles.
نویسندگان
چکیده
The synthesis and antimicrobial activity of a new series of 2-(substitutedphenyl/benzyl)-5-[(2-benzofuryl)carboxamido]benzoxazole derivatives 3-12 were described. The in vitro antimicrobial activity of the compounds was determined against some Gram-positive, Gram-negative bacteria and fungi and their drug-resistant isolates in comparison with standard drugs. Antimicrobial results indicated that the synthesized compounds possessed a broad spectrum of activity with MIC values 500-15.625 microg/ml. In the series, the most active compound against Candida krusei and Candida albicans isolate is 8 with MIC value 31.25 microg/ml. However, it is one dilution less potent than the compared fluconazole. Some of the screened compounds exhibit significant activity, having MIC value as 31.25 microg/ml in Pseudomonas aeruginosa having same activity as Rifampicin. Furthermore, considering the worth of developing new antibacterial agents against drug-resistant P. aeruginosa the present study explores the structure-activity relationship analysis of 2-(substitutedphenyl/benzyl)-5-[(2-benzofuryl)carboxamido]benzoxazoles using 3D-common features pharmacophore hypotheses approach.
منابع مشابه
Synthesis and antimicrobial activity of novel benzoxazoles.
A series of 2-(p-substituted-benzyl)-5-[[4-(p-chloro/fluoro-phenyl)piperazin-1-yl]acetamido]-benzoxazoles were synthesized in need of new compounds for the fight against microbial pathogens. Their structures were elucidated by spectral techniques. These new derivatives, along with previously synthesized 2-(p-substituted-benzyl)-5-substituted-benzoxazoles, were evaluated for their antibacterial ...
متن کاملSynthesis and antimicrobial activity of metal complexes from 2-(1’/2’-hydroxynaphthyl)benzoxazoles
Synthesis and antimicrobial activity of new metal [Mg(II), Fe(II), Co(II), Ni(II), Zn(II) and Cd(II)] complexes from 2-(1’/2’-hydroxynaphthyl)benzoxazoles have been described. Some of the metal complexes show significant antifungal activity (MIC <3.12 μg/ml). Further, 2-(1’/2’hydroxynaphthyl)benzoxazoles exhibit excited-state intramolecular proton transfer mechanism that has been studied using ...
متن کاملSynthesis and antimicrobial activity of some 2-[p-substituted-phenyl]benzoxazol-5-yl-arylcarboxyamides.
New 2-[p-substituted-phenyl ]benzoxazol-5-yl-arylcarboxyamides derivatives have been synthesized by reacting 5-amino-2-[p-substituted-phenyl ]benzoxazoles with substituted-arylcarboxylic acid chlorides. The structures of the synthesized compounds were confirmed by IR and (1)H NMR spectral data. Antimicrobial activities of the compounds were investigated using the two-fold serial dilution techni...
متن کاملSynthesis and Study of Antitumor Activity of Substituted Imidazolecarboxamides
In view of potential biological activities of small molecule polyamides, we synthesized some novel N-(2-aminoethyl)-1-benzyl-2- (alkylthio)-1H-imidazole-5-carboxamide (7a,b), and N-(2-(1-benzyl-2-(alkylthio) -1H-imidazole- 5-carboxamido) ethyl)-1-benzyl-2- (alkylthio)-1H-imidazole-5-carboxamides (8a,b) as antitumor agents. The antitumor activity of compounds 7a,b and 8a,b was studied at c...
متن کاملSynthesis and antimicrobial evaluation of 2-(p-substituted phenyl)-5-[(4-substituted piperazin-l-yl)acetamido]-benzoxazoles.
A series of 2-(p-substituted phenyl)-5-(2-{4-[(p-chloro-fluorophenyl)/phenyl] piperazin-1-yl}acetamido)-benzoxazoles were synthesized and tested for their antimicrobial activities. The structures of the new derivatives were elucidated by spectral techniques. The minimum inhibitory concentrations (MIC) of the new benzoxazoles, along with those of previously synthesized analogues, were determined...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
عنوان ژورنال:
- European journal of medicinal chemistry
دوره 43 11 شماره
صفحات -
تاریخ انتشار 2008