Synthesis, anti-inflammatory and analgesic activity evaluation of some 2-(9-acridinylamino )pyridines and 2-(9-acridinylamino/imino)thiazolines

620-62

Bioactivity of marine organisms: Part X - Screening of some marine fauna from the Indian coasts

754-756Methanolic and chloroform-methanol extracts of 25 identified species of marine fauna have been screened for a wide range of biological activities. Of these, 2 extracts exhibited diuretic activity, while antibacterial, antiviral, oxytocic and spasmolytic activities, were observed in 1 extract each

Synthesis, anti-inflammatory and analgesic activity evaluation of some pyrimidine derivatives

273-281A number of pyrimidine derivatives 1-3, 5-19 have been synthesized by condensation of bis(2-(vinyloxy))ethylamine, cyclopropylamine, N-(2-amino-4-ethoxyphenyl)acetamide, 2-(aminomethyl thiophene), 2-thiophen ethylamine, 2-hydrazinopyridine, 1-aminonaphthalen-2-ol hydrochloride, furfuryl amine, 2-(4-imidazolyl)ethylamine, 2-picolylamine and 4-methoxyl-2-nitroaniline with various isothiocyanatoketones. These compounds have been screened for anti-inflammatory and analgesic activities. Compounds 10 and 14 have exhibited 40% and 39% anti-inflammatory and compound 11 has showed 75% analgesic activity at 100 mg/kg p.o. respectively

Synthesis of condensed pyrimidines and their evaluation for anti-inflammatory and analgesic activities

136-143Condensation of 4-isothiocyanato-4-methylpentane-2-one with 1,2-diaminocyclohexane, 3-amino-2-naphthol, 1-amino-2-naphthol hydrochloride, 3-amino-2-naphthoic acid, 1,3-diamino-2-hydroxypropane and 1,3-diaminoguanidine hydrochloride give condensation products 1 and 3-8 respectively whereas condensation of 3-isothiocyanato butanal with 1,2-diaminocyclohexane and 1,3-diaminoguanidine hydrochloride give compounds 2 and 9. All these compounds have been characterized by FT-IR, ¹H NMR, MS and elemental analysis. Compounds 1, 2, 4 and 6-9 have been screened for anti-inflammatory and analgesic activity. Compounds 1 and 8 exhibit good analgesic activity whereas all other compounds exhibit moderate anti-inflammatory and analgesic activity

Synthesis of sulpha drug acridine derivatives and their evaluation for anti-inflammatory, analgesic and anticancer activity

2659-2666Various sulpha drugs i.e. sulphaacetamide, sulphathiazole, sulphadiazine and sulphamerazine are coupled with 9-chloro-2,4(un)substituted acridines and 9- isothiocyanato-2, 4(un) substituted acridines to give corresponding coupled products 3a-f and 4a-h respectively. The structures of all synthesized compounds have been confirmed by spectroscopic methods. Anti-inflammatory activity evaluation of 3a,b,c and 4a-h was carried out and compounds 4a, 4d, 4g and 4h showed 8,13,22 and 3% activity respectively at 100mg/ kg p.o. Analgesic activity evaluation of 3a,b,c and 4a-h indicated that these compounds possess 25,75,50,25, 50,50, 0.75, 50, 50 and 50% analgesic activity at 100mg/kg p.o. Anticancer activity evaluation of 3a-f and 4a-h against a small panel of seven cancer cell lines consisting of lung (NCIH 460);colon (HT 29): melanoma (LOX); breast (MCF 7 and MCF 7 / ADR); prostate (DU 145) and CNS (U251) tumors was carried out. Best GI50 (concentration which inhibits the cell growth by 50%) values are shown by 4b, 0.4 μM (lung carcinoma, cell line NCIH 460): 4b, 0.3 μM (colon tumor, cell line HT29); 3e, 7.2μm (melanoma tumor, cell line LOX): 4b, 0.7μM (breast tumor, cell line MCF7); 4c, 1.9μM (breast tumor, cell line MCF7/ADR); 4b, 0.8μM (prostate tumor, cell line DU 145) and 4b, 1.4μ M (CNS tumor, cell line U251) respectively. Out of all the compounds reported here GI50 value shown by 4c i.e. 1.9μM against breast tumor (MCF7/ADR) is quite close to the GI50 value i.e.1.2μM of the sta ndard drug doxorubicin. Also it is worthwhile to mention here that compound 4b, has shown good anticancer activity against four tumor cell lines i.e. GI50 value M.</i

Synthesis, hydrolysis over silica column, anticancer, anti-inflammatory and analgesic activity evaluation of some pyridine and pyrazine derivatives

387-399Various 3,4-diaryl-2-iminothiazolines 1a-s have been condensed with 4-cyanopyridine and 2-cyanopyrazine by refluxing in methanol for about 16 hr to give corresponding 3,4-diaryl-2-imino-N-(4'-pyridyliminomethyl)-4-thiazoline (2a-k, n-p) and 3, 4-diaryl-2-imino-N-(2'-pyrazinyliminomethyl)-4-thiazoline (3a-m, q-s) derivatives. In some cases when these pyridyl and pyrazinyl derivatives are purified by column chromatography over silica gel these compounds get hydrolysed to give corresponding 3,4-diaryl-2-imino-N-(4'-carbonylpyridyl)-4-thiazoline (2o,p) and 3,4-diaryl-2-imino-N-(2'-carbonylpyrazinyl)-4-thiazoline (3q-s) derivatives. The structures of all synthesized compounds have been confirmed by spectroscopic methods. Compounds 2a-c,e-h,k,n,p, 3a-i and 3l,m,q are screened for anticancer activity against a small panel of six human cancer cell lines consisting of prostate (DU 145) colon (HT 29) breast (MCF 7) breast (MCF 7/ADR), CNS (U 251) and lung large (NCIH 460) tumors. Best GI50 values are shown by 3f, 11.5 M (prostate tumor, cell line DU 145), 3f, 1.0 M (colon tumor, cell line HT 29), 2n, 6.2M (breast tumor, cell line MCF 7), 2p, 4.8M (breast tumor, cell line MCF 7/ADR), 2p, 6.3M (CNS tumor, cell line U 251) and 3f, 0.9 M (lung large carcinoma, cell line NCIH 460) respectively. Compound 3f has shown good anticancer activity against three cancer cell lines, whereas compounds 2n and 2p against one and two cancer cell lines respectively. Antiinflammatory activity evaluation of 2a-k,n,o,p, 3a-m and 3q,r,s has been carried out and compounds 2a-h, 2j, 2o,p, 3a,b,c,g,m and 3r showed 13, 32.5, 48.8, 6.5, 13.9, 7.0, 4.3, 16.6, 20.0, 17.3, 27.7, 16.2, 18.4, 34.7, 15.6, 24.0 and 4.7% activity, respectively, at 100mg/kg p.o. Analgesic activity, evaluation of 2a-k,n,o,p, 3a-m and 3q,r,s indicates that these compounds possess 50, 25,75, 25, 50, 75, 50, 50, 25, 0.0, 50, 50, 0.0, 75, 50, 25, 25, 25, 75, 0.0, 25, 25, 25, 50, 50, 75, 25, 50, 75 and 50% analgesic activity at 100mg/kg p.o

Immunomodulation by opioid peptidomimetic compound

Objective: As a follow-up to our earlier studies on immunomodulation with opioid peptides, we synthesized and evaluated immunomodulatory activity of four peptidomimetic compounds, i.e. Tyr-NH-C(Me)2-CH2-O-Phe-NH2(1), Tyr-NH-C6H5-(o)-CH2-CH2-O-Phe-NH2 (2), Tyr-NH-CH2-CH2-O-Phe-NH2 (3) and Tyr-NH-CH(D-Et)-CH2-O-Phe-NH2 (4). Methods: These compounds were synthesized in solution phase and evaluated for their immunomodulatory properties in vitro by mixed lymphocyte reaction (MLR), proliferation of opioid receptor-expressing cells, production of tumor necrosis factor-&#945; (TNF-&#945; ) and nitric oxide. Results: This study shows the immunosuppressive potential of synthetic peptidomimetic compound 3. This compound inhibited two-way MLR and suppressed the proliferation of the &#956; -opioid receptor expressing human embryonic kidney cells HEK 293 in vitro. Inhibition of MLR by compound 3 was reversed by naloxone (opioid receptor antagonist) and &#946; -funaltrexamine hydrochloride (&#956; -opioid receptor antagonist). The immunosuppressive effect of compound 3 was further demonstrated by inhibition of TNF-&#945; and nitric oxide production in lipopolysaccharide-stimulated human PBMCs and mouse macrophage cells RAW 264.7, respectively. Conclusion: These observations suggest that compound 3 inhibits MLR through &#956; -opioid receptor present on cells