X-Ray Structure, Conformational Analysis, Enantioseparation, and Determination of Absolute Configuration of the Mitotic Kinesin Eg5 Inhibitor Monastrol

New environmentally benign protocol for the synthesis of 3,4-dihydropyrimidin-2(1H)-ones: Practical access to mitotic kinesin EG5 inhibitor Monastrol

“…8 By using traditional conditions ethanol/HCl turned out to be not compatible with the thiourea obtained 4i in much lower yield (17%). 13 Thus, variations in all three components have been accommodated very comfortably. However, under the present reaction conditions β-ketoaldehydes do not produce the corresponding…”

A convenient synthesis of some new fused pyridine and pyrimidine derivatives of antimicrobial profiles

“…The minimum inhibitory concentrations (MIC) were recorded for compounds that showed promising growth inhibition using the two-fold serial dilution method [21]. The MIC (lg/mL) values against the tested bacterial and fungal isolates were recorded in (Table 2).…”

“…In addition to the previously mentioned properties, thiazolo [3,2-a]pyridines, also containing two fused heterocyclic moieties in one molecule, are found in a broad range of biologically active compounds and have many important bioactivities such as inhibitors of beta-amyloid production [8], CDK2-cyclin-A [9], and a-glucosidase [10], potential uterus stimulants [11,12], and antibacterial and antifungal activities [13], and are found to exhibit a broad spectrum of potent anticancer activity and are useful for chemotherapy of various cancers, such as leukemia, lung cancer, and melanoma [14]. On the other hand, certain pyrimidine derivatives are also known to exhibit diverse pharmacological properties such as effective bactericides and fungicides [15], as antimalarial [16], antioxidant [17,18], and antihypertensive agents, as adrenergic and neuropeptide antagonists [19] and having anti-HIV activities [20,21]. Along with the varied biological activities of pyrimidine, other heterocycles fused with pyrimidines play an essential role in several biological processes and have a considerable chemical and pharmacological importance [22,23].…”

Nickel Nanoparticles: An Ecofriendly and Reusable Catalyst for the Synthesis of 3,4-Dihydropyrimidine-2(1H)-ones via Biginelli Reaction

“…3 The compounds bearing dihydropyrimidinones moiety are common in variety of biologically important natural products and potent drugs including anti-viral, 4 anti-inflammatory, 5 analgesic, 6 anti-mitotic, 7 anti-cancer, 8 and anti-hypertensive agents.…”