Current Issue : July - September Volume : 2013 Issue Number : 3 Articles : 7 Articles
Keeping in view the importance of Oxadiazole and Azetidinone compound, it is planned to synthesize a hybrid molecule comprising Oxadiazole and Azetidinone and were evaluated for Anticonvulsant activity. The Structures of all the synthesized compounds were elucidated on the basis of physical characterization (Melting point, TLC) and different Spectroscopy techniques (IR, 1H NMR and Mass spectroscopy). In the present study, anticonvulsant activities of Oxadiazole derivatives were evaluated by maximal electroshock method (MES) at 30, 100 and 200 mg/kg dose levels. Neurotoxicity of the compounds was also assessed at the same dose levels. Synthesized Compounds (SK0101- SK0109) gives anticonvulsant activity at different dose when compare with standard drug Phenytoin among that SK0101, SK0103, SK0105 gives better activity then others. Compounds SK0104, SK0106, SK0107, SK0109 show neurotoxicity at 100 mg and 200mg dose....
Etodolac has been conjugated with different antioxidants having antiulcerogenic activity with the objective of obtaintingEtodolac ââ?¬â??antioxidant mutual prodrugs as safer NSAIDs devoid of ulcerogenic side effects.SynthesizedPurified prodrugswere characterized by m.p., TLC, elemental analysis, FTIR, NMR and MS. The synthesized derivatives are screened for their anti-inflammatory ,analgesic and antiulcer activity. The biological evaluation of mutual prodrugsshowed retention of anti-inflammatory activity withreduced ulcerogenic side effects. The masking of parent drug in mutual prodrug of etodolac resulted in less exposure to gastric mucosa. The results indicated that Etodolac ââ?¬â??antioxidant mutual prodrugs have the potential to be developed as safer gastrosparing NSAIDs....
The structural and therapeutic diversity coupled with commercial viability of small heterocyclic molecules has fascinated organic and medicinal chemist. So, a great deal of research was carried out in the field of heterocyclic containing sulphur and nitrogen, because of their immense biological importance. In the present research work, the main motto was to develop new chemical entities of Edaravone. The chemical name of Edaravone is 3-methyl-1-phenyl-1H-pyrazol-5(4H)-one (2, 4-dinitro). The thiadiazole derivatives posses’ different pharmacological and biological activity. The starting material 3-methyl-1-substituted-1H-pyrazol-5(4H)-ones (1) were synthesized in high yields according to reported method using by the treatment of ethyl acetoacetate with appropriate 1-phenylhydrazine. Ethyl 2-(4, 5-dihydro-3-methyl-5-oxo-1-phenyl-1H-pyrazol-4-yl) acetate (2) was synthesized by reaction of ethyl chloroacetate with (1). 1-(2-(4, 5-dihydro-3-methyl-5-oxo-1-phenyl-1H-pyrazol-4-yl) acetyl) thiosemicarbazide (3) prepared by reaction of thiosemicarbazide with (2) in presence of solvent methanol. 4-((5-amino-1, 3, 4-thiadiazol-2-yl) methyl)-3-methyl-1-phenyl-1H-pyrazol-5(4H)-one (4) synthesized by reaction of (3) with con. H2SO4 and ammonia kept overnight. 4-((5-(4-substituted benzylideneamino)-1, 3, 4-thiadiazol-2-yl) methyl)-3-methyl-1-phenyl-1H-pyrazol-5(4H)-one (MG1-MG4) synthesized by using compound 4 and substituted aromatic aldehydes in presence of methanol as solvent. The structures of newly synthesized compounds were characterized by TLC and FT-IR. The newly synthesized compounds were screened for antibacterial, antifungal activity....
A novel series of substituted-2, 5-diphenyl-1, 3, 4-oxadiazole derivatives (3a-i) have been synthesized with the aim to get better anti-inflammatory and selective cox-2 inhibitor activity. Compound (2a-i) was reacted with several aryl acid hydrazides in phosphorousoxychloride to obtain the title compounds. Structures of the synthesized compounds were supported by means of IR, 1H NMR and mass spectroscopy. All synthesized derivatives were determined by the carrageenan induced rat paw oedema model for anti-inflammatory activity. The entire compound gives good response for anti-inflammatory activity for this activity indomethacine was used as standard drug and compared to new synthesized drugs. Some new synthesized drugs have to shown better activities for anti-inflammatory. Title compounds were evaluated for their anti-inflammatory and selective cox-2 activities. These compounds also exhibited significant anti-inflammatory activity, which is comparable to that of celecoxib in the carrageenan-induced rat paw edema method. The selected compounds were evaluated for their preliminary in-vitro cyclooxygenase inhibitory activity against COX-2 and COX-1 enzymes. The compounds tested showed selective inhibitory activity toward COX-2 (72-5%) over COX-1 (3.5%), amongst them compounds 3c and 3i showed appreciable COX-2 selective inhibitory activity....
A series of novel 5-(2-Amino-phenyl)-3H-[1, 3, 4] oxadiazole-2-thione was prepared by reacting Methyl anthranilate and hydrazine hydrate to give 2-Amino-benzoic acid hydrazide which reacts with CS2 / KOH to give 5-(2-Amino-phenyl)-3H-[1, 3, 4] oxadiazole-2-thione Compounds were synthesized by conventional synthesis method The purity of all synthesized compounds was determined by thin layer chromatography .All synthesized compounds by IR spectroscopy confirmed the functional groups .NMR indicated that all the chemical shift values were found in range. Mass confirms molecular weight of synthesized compound Oxadiazole nucleus is continuously drawing interest for development of newer drug moiety. Due to its wide range of activities viz. anticancer, antibacterial, antifungal, antimalarial, anticonvulsant anti-inflammatory etc. the steady research is going on in oxadiazole nucleus. Oxadiazole type of heterocyclic compounds contains oxygen and two nitrogen atoms...
In 1893, the synthesis of functionalized 3,4-dihydropyrimidin-2(1H)-ones (DHPMS) via three-component condensation reaction of an aromatic aldehyde, urea and ethyl acetoacetate was reported for the first time by P. Biginelli. In the past decades, such Biginelli-type dihydropyrimidones have received a considerable amount of attention due to the interesting pharmacological properties associated with this heterocyclic scaffold. In this review oxazolo [3,2-a] and pyrimido [2,1-b][1,3]oxazine have been prepared from 3,4-dihydropyrimidin-2(1H)-ones.Then I was focused my work to make new derivatives of oxazolopyrimidine, and pyrimidooxazine, having sulfonyl linkage and to check their Antibacterial and Antifungal activity . Purity of each compounds were checked by TLC using silica gel plate. All newly synthesized compounds were characterized by IR....
A series of 2-[(substitutedbenzylidene)amino]-N-(furan-2-ylmethyl)-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxamide (IV a-j) were synthesized from 2-amino-N-(furan-2-ylmethyl)-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxamide (III). The starting material 2-amino-N-(furan-2-ylmethyl)-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxamide (III) was synthesized as per Gewald’s method which was reacted with ten different substituted benzaldehydes to give respective Schiff bases (IV a-j). The newly synthesized compounds were characterized by Melting point, TLC, IR, NMR and Mass spectra. The synthesized compounds were subjected to antibacterial and anti fungal screening involving Gram positive, Gram negative bacterial and fungal species using Streptomycin and Fluconazole as standard at the same concentration. In conclusion, the compound IV (g) 2-[(4-hydroxy-3-methoxybenzylidene) amino]-N-(furan-2-ylmethyl)-tetrahydrobenzo[b]thiophene-3-carboxamide was found....
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