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Biomedical subjects

T N Bhalla

Publications and source records attributed to T N Bhalla.

At least 19 recordsLinked to original sources
PubMed1995

Synthesis and pharmacological evaluation of 1,2,4-triazine and its congeners.

3-[Mercapto]-n-propanoxy/methyl-ethanoxy branched chain in 5,6-Diphenyl- 1,2,4-triazine were condensed with O-phenylene diamine or O- aminophenol or o-aminothiophenol. The carboxylic groups of the synthesized compounds were cyclised to yield imidazoles, oxazoles and thiazoles. They were screened for their anti-inflammatory response in albino rats against carrageenin induced paw oedema. The active compounds were also evaluated for their ED50 value in albino rats and analgesic activity in albino mice. The compounds exhibited significant anti-inflammatory activity also showed marked protection against aconitine induced writhing response. The potent compounds showed high LD50 values.

Animals↗
PubMed1994

Synthesis of 1,3,4-thiadiazole-[3,2,-a]-s-triazine-5,7-dithione derivatives and their pharmacological evaluation.

2-Mercapto-6-phenyl-1,3,4-thiadiazole-(3,2-a)-s-triazine-5,7-dithione (1) was converted to 2-[3-carboxyl-2-methyl-1-mercapto]-6-phenyl-1,3,4-thiadiazole-(3,2-a)-s- triazine-5,6 dithione (2) and 2-thioethanoic acid-6-phenyl-1,3,4-thiadiazole-(3, 2-a)-s-triazine-5,7-dithione (4). This on reaction with o-phenylenediamine/ethylenediamine/o-aminophenol/o-aminothiophenol and polyphosphoric acid yielded compounds 3 (a-d) and 5 (a-d). The compounds 1,2,4,3 (a-d) and 5 (a-d) were evaluated for their anti-inflammatory activity against carrageenan induced paw oedema. The compounds found potent were further tested for their antiwrithmogenic activity in albino mice. Two compounds (2,3c) exhibited significant anti-inflammatory activity, also showed protection against aconitine induced writhing response, with high approximate LD50 values.

Animals↗
PubMed1993

Anti-inflammatory and analgesic activity of indolyl quinazolones and their congeners.

6,8-Disubstituted-2-methyl-3-[2-substituted-indol-3-yl-methyl(ene)imino] -quinazoline-4(3H)-ones (III), 6,8-disbustituted-2-methyl-3-[2-substituted-indol-3-yl methyl amino]-quinazoline-4(3H)-ones (IV), 6,8-disubstituted-2-methyl-2-[5-(2-substituted-indol-3-yl)-thiazolidine- 3- one]quinazoline-4(3H)-ones (V), propionic acid derivative of 6,8-disubstituted-2-methyl-3-[5-(2-substituted indol-3-yl)-thiazolidine-3-one]-quinazoline-4(3H)-ones (VI), 6,8-disubstituted-2-methyl-3-[5-(2-substituted-indol-3-yl)-2-substituted benzylidine-thiazolidine-3-one]-quinazoline 4(3H)-ones (VII), 6,8-disubstituted-2-methyl-3-[2-substituted-indol-3-yl-4- chloroazetidine-1-one]-quinazoline-4-(3H)-ones (VIII), and 6,8-disubstituted-2-methyl-3-[2-substituted-indol-3- yl-alpha-arylazo methylimino]-quinazoline-4(3H)-ones (IX) were synthesized and evaluated for their anti-inflammatory activity against carrageenin induced paw oedema. The compounds found potent were further tested for their anti-writhmogenic activity in albino mice. The compounds exhibiting significant anti-inflammatory activity also showed marked protection against aconitine induced writhing response. The low toxicity of the potent compounds was also reflected by their high approximate LD50 values.

Animals↗
PubMed1990

Anti-inflammatory activity of quinazolinoformazans.

Eight substituted quinazolonoformazans were synthesized and evaluated for anti-inflammatory activity. The degree of protection provided by seven of these compounds, at a dose of 100 mg/kg, po, against carrageenin-induced edema in rat paw ranged from 26 to 57%. The four active substituted quinazolonoformazans (1, 2, 6, 8), on further evaluation for antiwrithmogenic activity, provided 10-80% protection against the aconitine-induced writhing response in mice. The ulcerogenic liabilities of two of the most active compounds were also determined. The doses producing ulcers in 50% of the treated rats (UD50) were 155 and 260 mg/kg, ip, for 2 and 8, respectively. The low toxicities possessed by these substituted quinazolonoformazans were indicated by their LD50 values which ranged from 600 to 1300 mg/kg, ip, in mice.

Animals↗
PubMed1989

Anti-inflammatory and analgesic activities of 5-(4-[aryl(aryl azo)methyleneamino]phenyl)-1,3,4-oxadiazole-2(3H)-thiones.

Various new formazans of substituted oxadiazole 2(3H)-thiones were tested for their anti-inflammatory activity against carrageenin-induced paw oedema in albino rats. Among these, two most potent derivatives were evaluated in detail using cotton pellet implantation methods in albino rats of either sex. These two active analogues were also tested for their analgesic activity in albino mice and ulcerogenic liability in albino rats. The toxicity of the compounds was assessed by determination of their approximate LD50 value in albino mice. An attempt has also been made to establish the structure-activity relationship.

Aconitine↗
PubMed1988

Novel formazans as potent anti-inflammatory and analgesic agents.

Various new substituted formazans were synthesized and characterized by elemental analyses, IR and mass spectral data. The compounds were evaluated for their ability to protect against inflammation by carrageenin-induced paw edema in albino rats of either sex. The active derivatives of the present series were also tested for their analgesic activity against aconitine-induced writhing in albino mice and ulcerogenic activity in albino rats. The toxicity of the compounds was assessed by determination of their approximate LD50 on albino mice. An attempt has also been made to establish a structure-activity relationship.

Analgesics↗
PubMed1987

Tetrazoles as potent anti-inflammatory agents.

Various new tetrazoles were tested for their anti-inflammatory activity against carrageenin-induced paw oedema in albino rats. Among these, two most potent derivatives were evaluated in detail using cotton pellet implantation methods in albino rats of either sex. These two active analogues were also tested for their analgesic activity in albino mice and ulcerogenic liability in albino rats. All derivatives of the present series were evaluated for their antiproteolytic activity. The toxicity of the compounds was assessed by determination of their approximate LD50 in albino mice. An attempt has also been made to establish the structure activity relationship.

Animals↗
PubMed1985

Novel thiazolidinones as potent anti-inflammatory and analgesic agents.

Various new butyridenyl-2-hydroxybenzylidenyl-1,3-thiazolidinones were synthesized and characterized by elemental analyses, IR and PMR spectral data. The compounds were evaluated for their ability to afford protection against inflammation by carrageenin-induced oedema and cotton pellet implantation in albino rats of either sex. The active derivatives of the present series were also tested for their analgesic activity against aconitine-induced writhing in albino mice and ulcerogenic activity in albino rats. The toxicity of the compounds was reflected by determination of their approximate LD50 in albino mice. An attempt has also been made to correlate their structure-activity relationship.

Aconitine↗
PubMed1984

Anti-inflammatory activity of amino acyl benzoates.

Nineteen new piperazino or morpholino amino acyl benzoates were synthesized and screened against carrageenin induced oedema in albino rats. Several compounds of the series showed potent anti-inflammatory activity. Compound 10 was found to be the most potent. This compound was further evaluated in detail and compared with phenylbutazone for its relative anti-inflammatory potency and ulcerogenic liability. The compound, in addition, was compared with acetyl salicylic acid for its analgesic activity. This compound showed potent ant-inflammatory activity with minimal ulcerogenic liability.

Aminobenzoates↗
PubMed1984

Newer indolyl imidazolones as anti-inflammatory agents.

Sixteen new 1,2-disubstituted-4-(indol-3'-yl)methylene imidazol-5-ones were synthesized by the condensation of oxazolone with different aryl amines and evaluated as to their anti-inflammatory and antiproteolytic activities. These derivatives showed 2-38% protection against carrageenin-induced paw oedema in albino rats at a dose of 100 mg/kg p.o. All compounds showed antiproteolytic activity. The degree of inhibition against trypsin-induced hydrolysis of casein ranged from 10 to 75% at a concentration of 4 X 10(-4) mol/l. Furthermore, active compounds of the series were also screened for their analgesic activity against aconitine-induced writhing in albino mice. The toxicity of the compounds was reflected by their approximate LD50 values.

Animals↗
PubMed1984

Substituted triazoles as anti-inflammatory agents.

Newly synthesized triazoles were evaluated for their anti-inflammatory and antiproteolytic activities. These derivatives possessed potent anti-inflammatory and antiproteolytic activities. In addition, these compounds were relatively less toxic.

Animals↗
PubMed1983

Anti-inflammatory, analgesic and antiproteolytic activities of some novel thiadiazoles.

Eighteen novel acetyl salicyloyl/butyroyl mercapto 1,3,4-thiadiazoles have been synthesized and characterized by their elemental analyses, IR and PMR spectral studies. Their efficacy against carrageenin induced paw oedema was tested in albino rats of either sex at a dose of 100 mg/kg p.o. In vitro antiproteolytic activity of the compounds was assessed by determining their ability to inhibit trypsin induced hydrolysis of bovine serum albumin. Active anti-inflammatory compounds were tested for their analgesic activity against aconitine induced writhing in albino mice. Approximate LD50 values were also determined in albino mice.

Analgesics↗
PubMed1982

Antiinflammatory and antiproteolytic activities of newer indolyl isoquinolines.

Several indolyl isoquinoline derivatives were synthesized and evaluated for their antiinflammatory and antiproteolytic activities. These derivatives possessed 9.2-32.4% inhibition at a dose of 100 mg/kg i.p. against carrageenin-induced oedema. Four of these derivatives (IVb, IVd, IVe and IVk) exhibited high potency in inhibiting oedema. The degree of inhibition of trypsin-induced hydrolysis of bovine serum albumin, in vitro, by compounds IVb, IVd, IVe, IVi, IVj, IVk and IVl ranged from 10-42% at a final concentration of 1 mmol/l. In addition, these agents exhibited relatively non-toxic nature and their approx. LD50 was greater than 1000 mg/kg i.p.

Animals↗