- Synthesis, anti-inflammatory and analgesic activities evaluation of some mono, bi and tricyclic pyrimidine derivatives
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3-Aminobenzonitrile and 2-amino-4-phenyl thiazole on condensation with 4-isothiocyanato-4-methyl pentane-2-one gave condensed monocyclic pyrimidine derivatives 1 and 2, 3, respectively. Condensation of 3-aminopropyl imidazole with 3-isothiocyantobutanal g
- Sondhi, Sham M.,Singh, Nirupma,Johar, Monika,Kumar, Ashok
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- Synthesis, Anti-Inflammatory, Analgaesic and Anti-Amoebic Activity Evaluation of Some Pyrimidobenzimidazole and Pyrimidopyridoimidazole Derivatives
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o-Phenylenediamine, 4-nitro-1,2-phenylenediamine, 3,4-diaminobenzophenone, 3,4-diaminotoluene, 4,5-dimethylphenylenediamine and 3,4-diaminobenzoic acid (la-f) react with 4-isothiocyanatobutan-2-one to give the pyrimidobenzimidazole derivatives (2a-f) respectively. Condensation of 4-nitro-1,2-phenylenediamine with 4-isothiocyanatobutan-2-one at room temperature gave the thiourea derivative (3). o-Nitroaniline, on condensation with 4-isothiocyanatobutan-2-one at pH ca. 5 and under reflux conditions, gave the thiourea derivative (4). 2,3-Diaminopyridine, on condensation with 4-isothiocyanatobutan-2-one, gave product (5). Condensation of 2,3-diaminopyridine with 4-isothiocyanato-4-methylpentan-2-one using acetic acid as solvent gave compounds (6)-(8), whereas compounds (7) and (9) were isolated from the same reagents in dimethylformamide (DMF). 4-Isothiocyanato-4-methylpentan-2-one, on refluxing in acetic acid, gave compound (6). Anti-inflammatory activity evaluation was carried out at 100 mg/kg p.o. (paw oedema) for compounds (2a-f), (7) and (8). Compounds (2b), (2d) and (7) showed good anti-inflammatory and analgesic activities. Anti-amoebic activity evaluation of (2a-f) and (7) against Entamoeba histolytica (strain HM-1: IMSS) was carried out, and compound (2b) exhibited anti-amoebic activity similar to metronidazole in vitro.
- Sondhi, Sham M.,Johar, Monika,Shukla, Rakesh,Raghubir, Ram,Bharti, Neelam,Azam, Amir
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- SYNTHESIS, STRUCTURE, AND REACTIVITY OF 1,2,3,6-TETRAHYDROPYRIMIDINE-2-THIONES
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Dehydration of 4-hydroxyhexahydropyrimidine-2-thiones formed 1,2,3,6-tetrahydropyrimidine-2-thiones containing no substituent at the C(4) carbon atom.It is shown that the synthesized compounds, in contrast to their 4-alkyl-substituted analogs, react easily with various nucleophilic reactants (alcohols,butylmercaptan, benzenesulfinic acid, hydrazoic acid, p-toluidine) to from the corresponding 4-functionally substituted hexahydropyrimidine-2-thiones.
- Shutalev, A. D.,Komarova, E. N.,Pagaev, M. T.,Ignatova, L. A.
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p. 1077 - 1086
(2007/10/02)
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- Synthesis of Heterocycles via Enamines: Part XI - Reactions of 1,4-Dihydropyrimidine-2(3H)-thiones/-ones with 1,2- and 1,3-Binucleophiles
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The addition, cleavage and ring transformation reactions of derivatives of 4,4,6-trimethyl-1,4-dihydro-pyrimidine-2(3H)-thione/one with hydroxylamine, hydrazine and thiourea are reported.
- Singh, Harjit,Kumar, Subodh
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p. 688 - 691
(2007/10/02)
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- REACTION OF 2,3-O-ISOPROPYLIDENERIBOFURANOSYLAMINE TOSYLATE WITH 4-METHYL-4-ISOTHIOCYANATO-2-PENTANONE
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The condensation of 2,3-O-isopropylideneribofuranosylamine tosylate with 4-methyl-4-isothiocyanato-2-pentanone in the presence of bases was studied.In pyridine the reaction gives a mixture of 3-(2',3'-O-isopropylidene-β-D-ribofuranosyl)-4,6,6-trimethyl-1,2,3,6-tetrahydropyrimidine-2-thione and 3-(2',3'-O-isopropylidene-β-D-ribofuranosyl)-4-methylene-6,6-dimethylhexahydropyrimidine-2-thione.
- Shutalev, A. D.,Ignatova, L. A.,Unkovskii, B. V.
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p. 201 - 203
(2007/10/02)
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