Synthesis and anti-inflammatory activity of imidazo[1,2-a]pyrimidine derivatives

Thioxopyrimidine in Heterocyclic Synthesis I: Synthesis of Some Novel 6‐(Heteroatom‐substituted)‐(thio)pyrimidine Derivatives

“…Also, the interesting torsion angles which entirely de�ne the molecule conformation are selected and listed in Table 5. Moreover, the C(9)-C(10) [1.401(2) Å] and N(1)-C(7) [1.341(2) Å] bonds are longer than the N(2)-C(10) [1.334 (19) Å]. e C(1)-C(2) phenyl ring has a dihedral angle with N(2)-C(10) pyrimidine ring of 171.1 ∘ , while the carbonylmethylthio's dihedral angle with this pyrimidine is 101.0 ∘ .…”

“…Microanalyses for C, H, and N were performed on a Perkin-Elmer 240 elemental Analyzer. Enaminone derivatives 14a-f, 5-amino-4-phenylazo-3-methyl-1H-pyrazole 26, and 3-amino-4-methyl-6-phenylpyrazolo- [3,4- C (17) C (18) C (19) C (20) C (16) C (15) C (14) C ( 2.1. 5-Cyano-1,6-dihydro-4-methyl-2-phenyl-6-thioxopyrimidine (1).…”

“…Pyrimidine derivatives and related fused heterocycles are important classes of heterocyclic compounds that exhibit a broad spectrum of biological activities such as anticancer [1][2][3][4][5], antiviral [6], antibacterial [7,8], antioxidant [9,10], anxiolytic [11], and antidepressant activities [12]. Furthermore, they possess anti-in�ammatory [13][14][15][16][17][18][19] and analgesic activities that are well documented in the literature [20][21][22]. e incorporation of two moieties increases biological activity of both and thus it was of value to synthesize some new heterocyclic derivatives having two moieties in the same molecules.…”

“…[1.353(5) Å], C(18)-C(19) [1.383(5) Å], C(19)-C(20) [1.385(4) Å], and C(16)-C(17) [1.374(3) Å] bond lengths compared to the standard C ar -C ar distance of 1.397(1) Å [30]. In addition, the C(16)-C(17) phenyl and carbonyl group are in a staggered conformation with respect to the O atom giving rise to angular distortion at C(15) and C(14) [C(16)-C(15)-C(14)C(20)-C(15)-C(14)]…”

Therapeutic potential of heterocyclic pyrimidine scaffolds

“…10 ) has selective COX-2 inhibition (IC 50 = 13 µmol/l) which is 13 times more potent than its inhibitory activity to COX-1 (IC 50 = 170 µmol/l) and swollen inhibition 63.8%. The results indicated that imidazo[1,2- a ] pyrimidine compounds keep moderate anti-inflammatory activity as compared to ibuprofen (standard drug) [ 49 ].…”