Design, synthesis, and antihypertensive activity of new pyrimidine derivatives endowing new pharmacophores

Synthesis of novel calcium channel blockers with ACE2 inhibition and dual antihypertensive/anti-inflammatory effects: A possible therapeutic tool for COVID-19

“…Among structure modifications of DHPs, the bioisosters aza-analogs of DHPs, which gave rise to the dihydropyrimidines (DHPMs) [21] . DHPMs are privileged heterocyclic scaffolds due to their biological and pharmaceutical activities as anti-inflammatory, anti-oxidant, anti-hypertensive, anti-filarial and anti-SARS [22] , [23] , [24] , Fig. 1 .…”

“…Furthermore, their anti‐inflammatory effects on LPS-stimulated THP‐1 cells were evaluated. Here, we developed a program for the synthesis and evaluation of such nifedipine dihydropyridine bioisosteres, namely dihydropyrimidines (DHPMs) [22] , [23] , as revealed in Fig. 2 .…”

Multisubstituted pyrimidines effectively inhibit bacterial growth and biofilm formation of Staphylococcus aureus

“…Pyrimidines are heterocyclic aromatic compounds that are present in many natural and synthetic products and constitute essential building blocks for DNA and RNA biosynthesis 13 . Pyrimidine derivatives have shown a wide spectrum of biological activities including both non-chemotherapeutic, such as cardiovascular 14 and anti-inflammatory 15 , as well as chemotherapeutic, such as anticancer 16 , antiviral 17 , and antibacterial 18 , 19 . In our previous work, we prepared a set of multisubstituted pyrimidines designed to target the C1 domain of protein kinase C 20 .…”

Design, Synthesis and Biological Evaluation of Novel 4-(4-Methoxynaphthalen-1-yl)-5-arylpyrimidin-2-amines as Tubulin Polymerization Inhibitors

“…Pyrimidine, a 6-membered heterocyclic ring, containing two nitrogen atoms at 1, 3-positions, which is a versatile pharmacophore for designing and development of potent bioactive agents 10) . Small molecules with pyrimidine ring have been observed to possess various pharmacological activities, such as anti-inflammatory 11) , anti-HIV 12) , antimicrobial 13) , neuroprotective 14) , antiviral 15) , antimalarial 16) , antihypertensive 17) and anticancer activity [18][19][20] . Over the last few years, numbers of pyrimidine-containing drugs have been approved for clinical use, such as Imatinib (anticancer), Macitentan (antihypertensive), and Ceritinib (anticancer) (Figure 1) 21,22) .…”