182170-94-1Relevant academic research and scientific papers
Efficient Synthesis of 5-Carboxanilide-Dihydropyrimidinones Using Cobalt(II) Nitrate Hexahydrate
Kangan, Mehrnoush,Hazeri, Nourallah,Yazdani-Elah-Abadi, Afshin,Maghsoodlou, Malek-Taher
, p. 481 - 485 (2017)
5-Carboxanilide-dihydropyrimidinone derivatives were synthesized in good yield in a three-component and efficient process by the condensation reaction of acetoacetanilide, aldehyde and urea/thiourea in the presence of cobalt(II) nitrate hexahydrate as cat
Synthesis of novel calcium channel blockers with ACE2 inhibition and dual antihypertensive/anti-inflammatory effects: A possible therapeutic tool for COVID-19
Mahgoub, Shahenda,Kotb El-Sayed, Mohamed-I,El-Shehry, Mohamed F.,Mohamed Awad, Samir,Mansour, Yara E.,Fatahala, Samar S.
, (2021/09/04)
Hypertension has been recognized as one of the most frequent comorbidities and risk factors for the seriousness and adverse consequences in COVID-19 patients. 3,4-dihydropyrimidin-2(1H) ones have attracted researchers to be synthesized via Beginilli reaction and evaluate their antihypertensive activities as bioisosteres of nifedipine a well-known calcium channel blocker. In this study, we report synthesis of some bioisosteres of pyrimidines as novel CCBs with potential ACE2 inhibitory effect as antihypertensive agents with protective effect against COVID-19 infection by suppression of ACE2 binding to SARS-CoV-2 Spike RBD. All compounds were evaluated for their antihypertensive and calcium channel blocking activities using nifedipine as a reference standard. Furthermore, they were screened for their ACE2 inhibition potential in addition to their anti‐inflammatory effects on LPS-stimulated THP‐1 cells. Most of the tested compounds exhibited significant antihypertensive activity, where compounds 7a, 8a and 9a exhibited the highest activity compared to nifedipine. Moreover, compounds 4a,b, 5a,b, 7a,b, 8a,c and 9a showed promising ACE2:SARS-CoV-2 Spike RBD inhibitory effect. Finally, compounds 5a, 7b and 9a exerted a promising anti-inflammatory effect by inhibition of CRP and IL-6 production. Ultimately, compound 9a may be a promising antihypertensive candidate with anti-inflammatory and potential efficacy against COVID-19 via ACE2 receptor inhibition.
A Convenient Synthesis of Thiazolopyrimidine, Thiazolodipyrimidines and Heterocyclothiazolopyrimidines
Sharaf, M. A. F.,Aal, F. A. Abdel,Fattah, A. M. Abdel,Khalik, A. M. R. Abdel
, p. 1956 - 1969 (2007/10/03)
4-Aryl-6-methyl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxanilides I reacted with chloracetic acid/acetic anhydride and aromatic aldehyde to yield thiazolopyrimidine derivative IV.Compounds I reacted with bromomalononitrile to give 3-amino-5-aryl-2-cyano-7-methyl-5H-thiazolopyrimidine-6-carboxanilides VI.The latter compounds VI reacted with formic acid, ethyl cyanoacetate and with hydroxylamine hydrochloride to give annulated pyrimido-, pyridino-, and pyrazolo- derivatives VII, VIII, IX respectively (Scheme 1).
