dc.description.abstract |
Present work consists of study of β-Lactamase (BLase) inhibitory potential of
phytochemicals from Apocynaceae & Compositae families and Ketophosph(on)ates.
For this study; an easy, efficient & economical method was developed, used
successfully and published.
In this study, thirty two compounds were prepared and characterized by EIMS
&
1
H-NMR. These compounds comprise of: Diethyl (2-oxo-2-phenylethyl)
phosphonate(1), Diethyl [(E)-1-benzoyl-2-phenylvinyl] phosphonate(2), Diethyl[(E)-
1-benzoyl-2-(2-hydroxyphenyl) vinyl] phosphonate(3), Diethyl [(1E,3E)-1-benzoyl-4-
phenylbuta-1,3-dien-1-yl] phosphonate(4), Diethyl [(1E)-1-benzoyl-2-phenylprop-1-
en-1-yl]phosphonate(5),
Diethyl
[(E)-1-benzoyl-2-(4-hydroxy-3-methoxyphenyl)
vinyl] phosphonate(6), Diethyl benzyl phosphonate(7), Diethyl [2-(2-hydroxyphenyl)-
2-oxo-1-phenylethyl] phosphonate(8), Diethyl [(3E)-2-oxo-1,4-diphenylbut-3-en-1-
yl] phosphonate(9), Diethyl(2-oxo-1,2-diphenylethyl) phosphonate(10), Diethyl (2,4-
dioxo-1-phenylpentyl)
phosphonate(11),
Diethyl
(2,4-dioxo-1,4-diphenylbutyl)
phosphonate(12), Ethyl (diethoxyphosphoryl) acetate(13),
Diethyl (oxiran-2-
ylmethyl) phosphonate(14), Diethyl[2-(2-hydroxyphenyl)-1-oxiran-2-yl-2-oxoethyl]
phosphonate(15),
phosphonate(16),
6-Diethyl
Diethyl
[(3E)-1-oxiran-2-yl-2-oxo-4-phenylbut-3-en-1-yl]
(1-oxiran-2-yl-2-oxo-2-phenylethyl)
phosphonate(17),
Diethyl (1-oxiran-2-yl-2,4-dioxopentyl) phosphonate(18), Diethyl (1-oxiran-2-yl-2,4-
dioxo-4-phenylbutyl) phosphonate(19), Diethyl (2-nitrobenzyl) phosphonate(20), six
derivatives (21-26) containing the Tetraethyl ethane-1,2-diylbis (phosphonate) motif,
Diethyl
methylphosphonate(27),
phosphonate(28),
Diethyl
Diethyl
Diethyl
[2-(2-hydroxyphenyl)-2-oxoethyl]
[(3E)-2-oxo-4-phenylbut-3-en-1-yl]
(2-oxo-2-phenylethyl)
phosphonate(30),
phosphonate(29),
Diethyl(2,4-dioxopentyl)
phosphonate(31) and Diethyl (2,4-dioxo-4-phenylbutyl) phosphonate (32). Seventeen
compounds showed BLase inhibition activity. The compounds 1, 12, 29 & 32 were
found more active than Clavulanic acid (used as standard).
Extraction and bioassay guided isolation of Cichorium intybus resulted in the
purification and identification of ten compounds: [Lupeol (33), β-Sitosterol(34), p-
hydroxy phenyl acetic acid(35),
Isovanillic acid(36), Syringic acid(37), Vanillic
acid(38), Esculetin(39), Scopoletin(40), Umbelliferone(41) and Kaempferol(42)].
Stigmasterol(43) was the only compound isolated from Ageratum conyzoides but six
compounds:
[Conessine(44),
Kurchinin(45),
Conimine(46),
Kurchamine(47),
Holaromine(48) & Kurchessine(49)] were extracted from Holarrhena antidysenterica.
viiiHowever two compounds: [Lupeol(32) & Campesterol(50)], were extracted from
Carissa opaca while Quercetin(51) & Kaempferol(42) were isolated from Alstonia
scholaris. β-Sitosterol(34), α-Amyrin(52) & Ursolic acid(53) came out of Calotropis
procera. All the phytochemicals were subject to BLase inhibition study. In general
these
phytochemicals
showed
poor
activity
however
Kurchamine(47),
Holaromine(48) and Quercetine(51) were relatively more active in this respect. |
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