Synthesis and Pharmacological Evaluation of Some New Pyrimidine Derivatives Containing 1,2,4-Triazole
Purpose: An efficient method has been described for synthesis of 6-(substituted aryl)-4-(3,5-diphenyl-1H-1,2,4-triazol-1-yl)-1, 6-dihydropyrimidine-2-thiol, as a beneficial antimicrobial, anticonvulsant and anticancer agents. Methods: The clalcones of title compounds were synthesized in three steps...
| Main Authors: | , , , |
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| Format: | Article |
| Language: | English |
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Tabriz University of Medical Sciences
2012-08-01
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| Series: | Advanced Pharmaceutical Bulletin |
| Subjects: | |
| Online Access: | http://journals.tbzmed.ac.ir/PDF/APB/Manuscript/APB-2-213.pdf |
| _version_ | 1819115745896824832 |
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| author | Shantaram Gajanan Khanage S. Appala Raju Popat Baban Mohite Ramdas Bhanudas Pandhare |
| author_facet | Shantaram Gajanan Khanage S. Appala Raju Popat Baban Mohite Ramdas Bhanudas Pandhare |
| author_sort | Shantaram Gajanan Khanage |
| collection | DOAJ |
| description | Purpose: An efficient method has been described for synthesis of 6-(substituted aryl)-4-(3,5-diphenyl-1H-1,2,4-triazol-1-yl)-1, 6-dihydropyrimidine-2-thiol, as a beneficial antimicrobial, anticonvulsant and anticancer agents. Methods: The clalcones of title compounds were synthesized in three steps and subsequently these chalcones were further reacted with thiourea in the presence of KOH in ethanol, which led to the formation of dihydropyrimidine derivatives (4a-j). Compounds 4a-j were screened for their in vitro antimicrobial activity by agar well method and their anticonvulsant activity by the MES model. Anticancer activity of two newly synthesized heterocycles were evaluated at National Cancer Institute (NCI) Maryland, USA against 60 cell lines of different human tumor at a single dose of 10-5M. Results: Compound 4b, 4c, 4d, 4i and 4j were exhibited significant antimicrobial potential against tested strains at 50μg/ml and 100μg/ml concentrations. Out of the ten compounds studied 4a, 4b, 4c, 4h and 4j showed comparable MES activity to Phenytoin and Carbamazepine after 0.5h. Tested compounds did not showed to be more potent than standard drugs after 4h. Compound 4a and 4d were found active on Non-Small Cell Lung Cancer (HOP-92). Conclusion: Ten noveldihydropyrimidine analogues has been synthesized, characterized and found to bepromising antibacterial, anticonvulsant and antitumor agents. |
| first_indexed | 2024-12-22T05:06:05Z |
| format | Article |
| id | doaj.art-e819b435434a47adbd5fc98e896681cd |
| institution | Directory Open Access Journal |
| issn | 2228-5881 2251-7308 |
| language | English |
| last_indexed | 2024-12-22T05:06:05Z |
| publishDate | 2012-08-01 |
| publisher | Tabriz University of Medical Sciences |
| record_format | Article |
| series | Advanced Pharmaceutical Bulletin |
| spelling | doaj.art-e819b435434a47adbd5fc98e896681cd2022-12-21T18:38:07ZengTabriz University of Medical SciencesAdvanced Pharmaceutical Bulletin2228-58812251-73082012-08-0122213222Synthesis and Pharmacological Evaluation of Some New Pyrimidine Derivatives Containing 1,2,4-TriazoleShantaram Gajanan KhanageS. Appala RajuPopat Baban MohiteRamdas Bhanudas PandharePurpose: An efficient method has been described for synthesis of 6-(substituted aryl)-4-(3,5-diphenyl-1H-1,2,4-triazol-1-yl)-1, 6-dihydropyrimidine-2-thiol, as a beneficial antimicrobial, anticonvulsant and anticancer agents. Methods: The clalcones of title compounds were synthesized in three steps and subsequently these chalcones were further reacted with thiourea in the presence of KOH in ethanol, which led to the formation of dihydropyrimidine derivatives (4a-j). Compounds 4a-j were screened for their in vitro antimicrobial activity by agar well method and their anticonvulsant activity by the MES model. Anticancer activity of two newly synthesized heterocycles were evaluated at National Cancer Institute (NCI) Maryland, USA against 60 cell lines of different human tumor at a single dose of 10-5M. Results: Compound 4b, 4c, 4d, 4i and 4j were exhibited significant antimicrobial potential against tested strains at 50μg/ml and 100μg/ml concentrations. Out of the ten compounds studied 4a, 4b, 4c, 4h and 4j showed comparable MES activity to Phenytoin and Carbamazepine after 0.5h. Tested compounds did not showed to be more potent than standard drugs after 4h. Compound 4a and 4d were found active on Non-Small Cell Lung Cancer (HOP-92). Conclusion: Ten noveldihydropyrimidine analogues has been synthesized, characterized and found to bepromising antibacterial, anticonvulsant and antitumor agents.http://journals.tbzmed.ac.ir/PDF/APB/Manuscript/APB-2-213.pdfChalconesCondensationDihydropyrimidineAntimicrobial activityMES activityAntitumor agent |
| spellingShingle | Shantaram Gajanan Khanage S. Appala Raju Popat Baban Mohite Ramdas Bhanudas Pandhare Synthesis and Pharmacological Evaluation of Some New Pyrimidine Derivatives Containing 1,2,4-Triazole Advanced Pharmaceutical Bulletin Chalcones Condensation Dihydropyrimidine Antimicrobial activity MES activity Antitumor agent |
| title | Synthesis and Pharmacological Evaluation of Some New Pyrimidine Derivatives Containing 1,2,4-Triazole |
| title_full | Synthesis and Pharmacological Evaluation of Some New Pyrimidine Derivatives Containing 1,2,4-Triazole |
| title_fullStr | Synthesis and Pharmacological Evaluation of Some New Pyrimidine Derivatives Containing 1,2,4-Triazole |
| title_full_unstemmed | Synthesis and Pharmacological Evaluation of Some New Pyrimidine Derivatives Containing 1,2,4-Triazole |
| title_short | Synthesis and Pharmacological Evaluation of Some New Pyrimidine Derivatives Containing 1,2,4-Triazole |
| title_sort | synthesis and pharmacological evaluation of some new pyrimidine derivatives containing 1 2 4 triazole |
| topic | Chalcones Condensation Dihydropyrimidine Antimicrobial activity MES activity Antitumor agent |
| url | http://journals.tbzmed.ac.ir/PDF/APB/Manuscript/APB-2-213.pdf |
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