Synthesis of new functionalised derivatives of [1, 2, 4]triazolo[4, 3-a]pyrimidine and pyrimido[2, 1-b][1, 3, 5]thiadiazine as aromatase inhibitors. (9th July 2015)

• Record Type: Journal Article
• Authors: Gomha, Sobhi; Abdelrazek, Fathy; Abdulla, Mohamed
• Is Part Of: Journal of chemical research. Volume 39:Number 7(2015)
• Page Start: 425
• Page End: 429
• Publication Date: 2015-07-09
• Subjects: Chemistry -- Research -- Periodicals; Chemistry -- Periodicals; 540.5
• DOI: 10.3184/174751915X14360216187281
• Languages: English
• ISSNs: 1747-5198

Abstract

New functionalised 3, 4-dihydropyrimido[2, 1-b][1, 3, 5]thiadiazine-6, 8-(2H, 7H)-dione and [1, 2, 4]triazolo[4, 3-a]pyrimidine-5, 7-(1H, 6H)- dione derivatives were synthesised through the reaction of thiobarbituric acid with aromatic amines and formaldehyde and from thiobarbituric acid and hydrazonoyl halides, respectively. The structures of the target compounds were confirmed by 1H NMR, IR and MS spectra. Moreover, the newly synthesised products were tested for their aromatase inhibition activities and the results obtained were promising compared with the drug letrozole, a non-steroidal aromatase inhibitor.