Synthesis of Novel Substituted Tetrahydropyrimidine Derivatives and Evaluation of Their Pharmacological and Antimicrobial Activities

Abstract

Tetrahydropyrimidine derivative 1 was employed as intermediate compound, which in turn was allowed to react with different electrophilic and nucleophilic reagents to synthesize new polyfunctionalized series of substituted pyrimidine‐2‐thione derivatives. Structures of the newly synthesized compounds have been elucidated by spectroscopic data and elemental analyses. The pharmacological and antimicrobial activities of synthesized products have been evaluated as drug candidates.

3D‐pharmacophore study molecular docking and synthesis of pyrido[2,3‐d]pyrimidine‐4(1H) dione derivatives with in vitro potential anticancer and antioxidant activities

“…In continuation of our program aiming to synthesize polyfunctional substituted heterocyclic compounds of potential biological activity, [ 3,4,8,17,18,23–29 ] the synthesis of poly‐functionalized 7‐amino‐5‐(4‐methoxyphenyl)‐2,4‐dioxo‐1,2,3,4‐tetrahydropyrido[2,3‐ d ]pyrimidine‐6‐carbonitrile ( 1a ) and 2‐amino‐4‐(4‐methoxyphenyl)‐5‐oxo‐5 H ‐dipyrido[1,2‐a:3′,2′‐ e ]pyrimidine‐3‐carbonitrile ( 1b ) was achieved via one‐pot multicomponent reactions of the barbituric acid and/or 3 H ‐pyrido [1,2‐ a ]pyrimidine‐2,4‐dione, [ 26 ] anisaldehyde, ammonium acetate and malononitrile or three‐component reactions of barbituric acid and/or 3 H ‐pyrido[1,2‐ a ]pyrimidine‐2,4‐dione, arylidine of malononitrile and ammonium acetate, under fusion at 150°C (Scheme 1).…”

“…Heterocyclic‐compounds are of great‐significance in the synthesis of pharmacologically active compounds. [ 1–4 ] Pyridine‐moieties are familiar‐substructures in numerous‐natural products, pharmaceuticals and‐functional materials. [ 5,6 ] Polysubstituted‐pyridines possess remarkable biological and pharmacological activities and could also be used as‐agrochemicals such as herbicides and corrosion agent.…”

An overview on synthesis and biological activity of pyrimidines

“…Indolyl-pyrimidine derivatives (62-64) as potent antibacterial agents Some Novel Substituted Tetrahydro pyrimidine Derivatives (65-67) showed remarkable antimicrobial activity against S. aureus (G+ve) Pseudomonas aeruginosa (G-ve), C. albicans (yeast), and A. Niger (fungus) [28]. 68) and (69) were synthesized and evaluated for their antibacterial activity and showed high in vitro antibacterial activity against Escherichia coli, Pseudomonas aeruginosa and Staphylococcus aureus [29].…”

Pyrimidines as Anticancer and Antiviral: Synthesis & Reactions (A Review)

“…They form the core part of Deoxyribonucleic acids (DNA) and ribonucleic acid (RNA), so they have diverse biological activities [1][2][3] . Among these activities, are anti-inflammatory [4][5][6][7] , analgesic 8,9 , antioxidant [10][11][12] , antimalarial [13][14][15] , antimicrobial activity [16][17][18][19][20] , antitumor [21][22][23][24][25][26][27][28] and antiviral [29][30][31][32][33][34][35][36] . In this investigation we surveyed the synthesis and reaction of pyrimidines with antiviral and anticancer activity through the last five years.…”