Synthesis, investigation of the new derivatives of dihydropyrimidines and determination of their biological activity

Synthesis, crystal structure and antibacterial studies of 2,4,6-trimetoxybenzaldehyde based dihydropyrimidine derivatives

“…First of all, the synthesis was started by performing Biginelli reaction on the basis of 2,4,6trimethoxybenzaldehyde, urea and acetylacetone in the presence of acetic acid [16] leading to the obtaining of new dihydropyrimidine 4 with 58% yield. The positive side of this protocol was simple work-up procedure -during cooling of the reaction mixture, the formed precipitate was washed just with distilled water.…”

“…[Hmim]HSO4-NaNO3 [62], TMSCl/CAN [63], GaI3 [64], CAN [65], Sm(ClO4)3 [66], La(OTf)3 [67], RuCl3 [68], HBF4-SiO2 [69], H3PMo12O40 [70], Sc(OTf)3 [71], MgCl2×6H2O [72], In(OTf)3 [73] and NH4Cl [16] did not lead to the desired effect. Only improving the [74] procedure by performing the reaction in the presence of Cu(OTf)2 in microwave conditions allowed us to obtain targeted dihydropyrimidine with 80% yield.…”

“…The reason of such reputation is caused by the broad spectrum of biological activities of dihydropyrimidines [4][5][6]. According to the umpteen investigations, these compounds demonstrate anti-leishmanial [7], antitumor [8][9][10][11][12][13], antiviral [14,15], antifungal [16], antiproliferative [17,18], antibacterial [19][20][21], anti-inflammatory [22][23][24], anti-hypertensive [25][26][27], antiepileptic [28], anti-HIV [29], antidiabetic [30,31], anti-malarial [32], mPGES-1 inhibitors [33], antitubercular [34], miscellaneous [35][36][37] activities, as well as calcium [38] and potassium channels [39][40][41] and α1aadrenergic antagonists [42]. However, the mentioned broad spectrum of activities is not an application limit of dihydropyrimidines in medicine.…”

Synthesis, crystal structure and antibacterial properties of 6-methyl-2-oxo-4-(quinolin-2-yl)-1,2,3,4-tetrahydropyrimidine-5-carboxylate

“…A combination of aldehyde, urea derivative and methylene active compound leads to the obtaining of dihydropyrimidine -a class of organic compounds which are widely used in medicine due to their broad spectrum of biological activities [4]. The reason of their popularity in medicine is caused by the multicomponent nature of this reaction allowing introducing various pharmacophoric groups in the structure of dihydropyrimidines [5][6][7][8]. Various investigations using molecular manipulations allow determining that this class of compounds demonstrate such activities as antiviral, antifungal [6,7], anti-leishmanial, antiproliferative [9], antitumor [10][11][12][13][14][15], antibacterial [16][17][18][19], anti-inflammatory [20][21][22], anti-hypertensive [23][24][25][26][27], anti-HIV [28], antiepileptic [29], antidiabetic, anti-malarial [30], mPGES-1 inhibitors [31], antitubercular [32], miscellaneous [33][34][35], potassium [36][37][38] and calcium channels [39] and α1aadrenergic antagonists [40].…”

Antibacterial Studies of Dihydropyrimidinones and Pyrimidinethiones

“…These are large group of structurally diverse compounds which are known to possess some characteristic properties like manifestations of novel structures, thermal stability, relevant biological properties, high synthesis flexibility and medicinal utility. [1][2][3][4][5][6][7][8][9][10][11][12] Further, some of dihydropyrimidines are reported to overcome multidrug resistance efficiently. 13 Thus, in the present paper, some new dihydropyrimidinone and pyrimidinethione compounds (shown in Figure 1) have been synthesized and their antibacterial activities have been studied in dimethyl formamide and dimethyl sulphoxide against some Gram positive and Gram negative bacteria.…”