Antiinflammatory activity of novel indole derivatives

Verma, Mahima; Tripathi, M.; Saxena, Abhishek; Shanker, K.

doi:10.1016/0223-5234(94)90193-7

Cited by 70 publications

(49 citation statements)

References 5 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The oral acute toxicity of synthesized steviolbioside 2 was evaluated using male mice (20 g each, Medical Research Institute, Alexandria University) according to Verma et al (1994). The animals were divided into groups of six mice each.…”

Section: Acute Toxicitymentioning

confidence: 99%

See 1 more Smart Citation

Physico-chemical and sensory characteristics of steviolbioside synthesized from stevioside and its application in fruit drinks and food

et al. 2017

View full text Add to dashboard Cite

Steviolbioside (Sb) was synthesized from stevioside and characterized by infrared, nuclear magnetic resonance ( 1 H NMR and 13 C NMR) spectroscopy. The purity melting point, solubility, acute toxicity, heat stability and sensory properties of Sb were evaluated. Physicochemical and sensory properties of low calorie fruit drinks and shortened cake prepared by replacing sugar with Sb were evaluated. Sb was stable in neutral or acidic aqueous solutions maintained at 100°C for 2 h. The sweetness intensity rate of Sb was found to be about 44 and 18.51 times sweeter than 0.5% and 10% sucrose solution, respectively. Sb solutions had sweet taste without bitterness compared to stevioside. No significant differences between the organoleptic properties of cakes prepared using sugar and those prepared replacing sugar with 50% Sb were observed. All drinks replacing sugar with Sb at 66% level had the highest overall acceptability scores comparable to those prepared using sugar alone.

show abstract

Section: Acute Toxicitymentioning

confidence: 99%

“…Steviolbioside 2 was further evaluated for its oral acute toxicity in male mice using a previously reported method (Verma et al 1994). The results indicated that the compound under investigation was nontoxic and well tolerated by experimental animals up to 300 mg/kg.…”

Section: Acute Toxicitymentioning

confidence: 99%

Physico-chemical and sensory characteristics of steviolbioside synthesized from stevioside and its application in fruit drinks and food

et al. 2017

View full text Add to dashboard Cite

show abstract

“…The compounds were given orally, suspended in 1% gum acacia, in doses of 1, 10, 100, 200, 250, 300 mg/kg. The mortality percentage in each group was recorded after 24 h 18 . Additionally the test compounds were investigated for their parenteral acute toxicity in groups of mice of six animals each.…”

Section: Acute Toxicitymentioning

confidence: 99%

“…Compounds 2a, 2g and 2h were further evaluated for their oral acute toxicity in male mice using a previously reported method 18,19 . The results indicated that the test compounds proved to be non-toxic and well tolerated by experimental animals up to 300 mg/kg.…”

Section: In Vivo Acute Toxicity Testmentioning

confidence: 99%

Synthesis and biological screening of some pyridine derivatives as anti-malarial agents

Bekhit

Hymete

Damtew

et al. 2011

Journal of Enzyme Inhibition and Medicinal Chemistry

View full text Add to dashboard Cite

“…Molecular operating environment (MOE) 18) docking studies of the inhibitors were performed using human MAO-A crystal structure (PDB ID: 2BXR).…”

Section: )mentioning

confidence: 99%

Synthesis of Some Pyridazinylacetic Acid Derivatives as a Novel Class of Monoamine Oxidase-A Inhibitors

Khattab

Bekhit

El‐Faham

et al. 2008

CHEMICAL & PHARMACEUTICAL BULLETIN

View full text Add to dashboard Cite

NotesMonoamic oxidase (MAO) (EC 1.4.3.4) is an integral flavin-containing enzyme of the outer mitochondrial membrane which is responsible for regulation and metabolism of major monoamine neurotransmitters such as serotonin (5-OH tryptamine), noradrenaline and dopamine. It is also involved in the biodegradation of exogenic amines such as benzylamine, tyramine, 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTT), 1-methyl-4-phenyl pyridium (MPP ϩ ), and a Parkinsonian-producing neurotoxin.2) It is found in two different isoforms designated as MAO-A and MAO-B which are encoded by two different genes 3) and distinguished by different substrate specificities and sensitivities to the selective inhibitors. 4)The new generation of MAO inhibitors is characterized by their relative specificities for the MAO subtypes and in some cases by the reversibility of their actions. In spite of considerable progress in our understanding of the interactions of the two enzyme forms with their preferred substrates and inhibitors, no general rules are yet available for the rational design of potent and selective inhibitors of MAO. This is partly due to the fact that the mechanism of interaction of several new drugs with MAOs has not been fully characterized. Therefore, the discovery of several selective MAO inhibitors has relied on serendipity. Preferential MAO-A inhibitors have been recognized as therapeutically useful antidepressants 5) , while MAO-B inhibitors have been found to be beneficial in the treatment of Parkinson's disease and Alzheimer's disease. 6,7)Recently, we have demonstrated a series of 3-benzyl-2-substituted quinoxalines as selective MAO-A inhibitors bearing substituted amino or hydrazino functionalities at position 2 (e.g. 2-morpholinoethylamino, 2-hydroxyethylamino, hydrazino, etc).8) The rational design of these compounds was based on a hybrid structure of known inhibitors. The aim of the present study was to design MAO-A inhibitors while taking into consideration various factors responsible for selectivity against the A isoform, 9) namely i) the presence of electron-rich aromatic moieties (e.g. Bazinaprine 10) ), ii) the presence of hydrazido functionality (e.g. Iproniazid 11) ), iii) the presence of an ethoxycarbonyl methylene group side chain of an aromatic system (e.g. Eugenol analog 12) ); exchanging the ester group with an amido group was also considered, and iv) the benzyl group was retained in the new model compounds in Fig. 1.The new substituted pyridazine-1-yl acetic acid derivatives (2, 3, 5) were designed as selective monoamine oxidase-A inhibitors. The synthesis and biological evaluation of these compounds were described. As a preliminary result of the biological investigation, compound 5d showed the highest MAO-A selectivity and could be the lead compound for designing more potent and selective MAO-A inhibitors.First, the 4-benzyl-2H-pyridazin-3-one derivatives 1 were prepared. The reaction of the 4-benzyl-2H-pyridazin-3-one derivatives 1 with bromo ethyl acetate in dimethyl formamide in the presence...

show abstract

Antiinflammatory activity of novel indole derivatives

Cited by 70 publications

References 5 publications

Physico-chemical and sensory characteristics of steviolbioside synthesized from stevioside and its application in fruit drinks and food

Physico-chemical and sensory characteristics of steviolbioside synthesized from stevioside and its application in fruit drinks and food

Synthesis and biological screening of some pyridine derivatives as anti-malarial agents

Synthesis of Some Pyridazinylacetic Acid Derivatives as a Novel Class of Monoamine Oxidase-A Inhibitors

Contact Info

Product

Resources

About