Polymorphism: an evaluation of the potential risk to the quality of drug products from the Farmácia Popular Rede Própria

Polymorphism in solids is a common phenomenon in drugs, which can lead to compromised quality due to changes in their physicochemical properties, particularly solubility, and, therefore, reduce bioavailability. Herein, a bibliographic survey was performed based on key issues and studies related to polymorphism in active pharmaceutical ingredient (APIs) present in medications from the Farmácia Popular Rede Própria. Polymorphism must be controlled to prevent possible ineffective therapy and/or improper dosage. Few mandatory tests for the identification and control of polymorphism in medications are currently available, which can result in serious public health concerns

Synthesis of isoxazoles and quinoxalines as potential anticancer agents

421-4242-Acetylbenzimidazole on condensation with various aldehydes yield chalcones 1 which on cyclisation with hydroxylaminehydrochloride in sodium acetate furnish 3-(benzimidazol-2'-yl)-5-arylisoxazoles 2a-1. Dibromo derivative of chalcones 1 on reaction with 2-phenylene diamine in sulphuric acid furnish 2-(benzimidazol-2'-yl-methyl)-3-arylquinoxalines 3a-1. The structure of the compounds 3a-1 have been confirmed from elemental analyses, IR, 1H NMR and mass spectral data. The purity of the synthesised compounds have been checked by thin layer chromatography and screened for their antimicrobial and anticancer activity. All the products have been evaluated for their in vitro growth inhibitory activity against different microbes

Synthesis and Biological Screening of Pyrano[3,2‑<i>c</i>]quinoline Analogues as Anti-inflammatory and Anticancer Agents

A series of pyrano­[3,2-<i>c</i>]­quinoline based structural analogues was synthesized using one-pot multicomponent condensation between 2,4-dihydroxy-1-methylquinoline, malononitrile, and diverse un­(substituted) aromatic aldehydes. The synthesized compounds were evaluated for their anti-inflammatory and cytotoxicity activity. Initially, all the compounds were evaluated for the percent inhibition of cytokine release, and cytotoxicity activity and 50% inhibitory concentrations (IC₅₀) were also determined. Based on the primary results, it was further studied for their ability to inhibit TNF-α production in the human peripheral blood mononuclear cells (hPBMC) assay. The screening results revealed that compound <b>4c</b>, <b>4f</b>, <b>4i</b>, and <b>4j</b> were found most active candidates of the series against both anti-inflammatory and anticancer activity. The structure–activity relationship is discussed and suggested that 3-substitution on the aryl ring at C4 position of the pyrano­[3,2-<i>c</i>]­quinolone structural motif seems to be an important position for both TNF-α and IL-6 inhibition and anticancer activity as well. However, structural diversity with electron withdrawing, electron donating, sterically hindered, and heteroaryl substitution sincerely affected both the inflammation and anticancer activities