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Beta lactam derivatives exhibit a range of bioactivities, including
anti-angiogenic, anti-tumour, anti-malarial, anti-inflammatory and
analgesic, anti-tubercular, anti-glaucoma, anti-HIV, cytotoxic and
antimicrobial properties. The synthesis of metal complexes of
lactam derivatives had received much attention due to the fact that
they are among the first effective chemotherapeutic agents to be
employed for the prevention and cure of bacterial infection in
humans. The pharmacological activity of these types of molecules is
often enhanced by complexation with metal ions.Certain theories had
been advanced advocating that a major portion of drug action
occurred through complexation. The importance of metal ions in
biological systems is well known. One of the most interesting
features of metal coordinated systems is the concerted spatial
arrangement of the ligands around the metal atom.
During the era of 1935-1945 the sulfonamide provided exceptional
advances in the control of infectious diseases, particularly for
these three major diseases hemolytic streptococcal infections,
gonorrhea and other like pneumococcal pneumonia and meningitis etc.
They also proved effective in urinary tract infections. As a
therapeutic agent sulfonamides were succeeded as an antibiotic.
After this it showed broad control of such infection like
tuberculosis, staphylococcal sepsis, rickettsia disease, and
infections due to other gram negative bacteria.
This book describes the synthesis and characterization using
proton-NMR, IR, CHNS analyzer, single crystal X-ray diffractometer
and quantum chemical studies of novel derivatives of
5-aminotetrazole. The reactions involving acid chlorides were
performed in inert atmosphere. The reactions with sulfonyl
chlorides gave products with cleaved tetrazole ring structure. In
1H NMR spectrums, aromatic protons were observed at 7.4-7.9 ppm in
all derivatives. The density functional theory has been used to
investigate the geometric and electronic properties of all the
compounds. The B3LYP/6-311G** level of theory was found better than
the B3LYP/6-31G** level of theory to reproduce the experimental
data. The HOMOs and LUMOs of all the compounds under study were
also calculated.
The use of antibiotics in the treatment of various infections of
humans caused by microbes has been a great success. Over the past
years there has been an increase in the resistance of
microorganisms against a large number of drugs. Keeping in view the
biological activity and medicinal importance of sulfonamides, new
sulfonamides are being synthesized. This book describes the
synthesis of N-benzyl-4-methylbenzenesulfonamide, its N-alkylated
derivatives and evaluation of their anti-microbial activity.
N-benzyl-4- methylbenzene sulfonamide was synthesized by the
condensation of benzyl amine with p-toluene
benzenesulfonylchloride. The solvent used for this reaction was
water.N-alkylated derivatives were prepared by reacting
N-benzyl-4-methylbenzenesulfonamide with different alkylating
agents and sodium hydride using DMF as solvent. The synthesized
compounds were characterized by different techniques like X-ray
crystallography, FT-IR, Elemental analyzer and melting point.
Evaluation of anti-microbial activity was carried out by employing
deep well method against different bacterial strains.The
synthesized compounds exhibited appreciable anti-microbial
activity.
This Book describes the synthesis, crystal structure determination,
antibacterial, antifungal, Brine-Shrimp Cytotoxocity assay and DPPH
antioxidants studies of a range of new N- & O-Sulphonated
derivatives of tyrosine. The targeted compounds were prepared by
the reaction of Tyrosine with different sulfonyl chlorides via
different synthesis schemes from moderate to excellent yields. The
final products were extensively screened to investigate their
antibacterial and antifungal potentials. All the derivatives were
found to be active against Staphylococcus aureus, Micrococcus
luteus, Escherichia coli, Bacillus broncistepica, Salmonella
typhimurium and Enterobacter aerogenes. These Derivative did not
show any bioactivity against fungal strains such as Mucor species,
Aspergillus niger, Aspergillus flavus, Aspergillus fumigatus and
Fusarium solani. The targeted compounds were also subjected to
Brine-Shrimp cytotoxic studies. Only one compound showed good
cytotoxic activity while other derivatives exhibit no activity at
all.Antioxidant potential of these derivatives was investigated by
DPPH Assay. All compounds showed excellent antioxidant activities.
The chemistry of antioxidants has developed rapidly. Natural and
synthetic antioxidants found their various applications in
petrochemical industry, cosmetics, food industry, and rubber
industry and in medicines. This book will be of immense value to
students, practicing professionals and others to learn something
about the importance of antioxidants. This book is unique in this
sense that it elucidates the role of spectrophotometry in
evaluating the antioxidant potential of natural and synthetic
compounds. In addition, it will give you an idea to identify the
class of natural products by simple phytochemical screening tests.
The present study aimed to investigate the antioxidant potential of
Monotheca buxifolia by employing some in-vitro contemporary
methods. The results obtained and Phytochemical screening deduce
that Monotheca buxifolia possesses effective natural antioxidants
and radical scavenging activity but it can not be associated with
the total phenolic and total Flavanoid contents of the plant
A stability indicating RP-HPLC method was developed and validated
for the determination of Gemifloxacin in tablet formulation. The
drug was subjected to forced degradation study in terms of acidic,
thermal, oxidative, photo and basic stresses. Degradation products
produced as a result of stress testing were successfully separated
through C18 column (250 x 4.6 mm, 5 m) using ammonium acetate
buffer (pH 2.7; 0.05 M) and acetonitrile (70:30, v/v) as a mobile
phase at a flow rate of 0.7 mL/min. The diode array detection was
performed at 272 nm. The method was linear over the concentration
range of 0.256-128 g/mL with correlation coefficient equal to
0.9990. The LOD and LOQ were 10 ng/mL and 30 ng/mL respectively.
The proposed method was validated according to ICH guidelines. The
method showed adequate separation of Gemifloxacin from its stress
induced degradation products and excipients with resolution greater
than 1.5 within 11 minutes. The method is therefore considered as
stability indicating, rapid and suitable for the chromatographic
purity and assay determination of Gemifloxacin not only in routine
quality control analysis but also for stability studies.
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