Synthesis of Some New Folic Acid-Based Heterocycles of Anticipated Biological Activity

• Published in: Molecules (Basel, Switzerland) Switzerland), 2021-01, Vol.26 (2), p.368
• Main Authors: Abu Ali, Ola A, Saad, Hosam A, Al Malki, Bodor M A
• Format: Article
• Language: English
• Subjects: biological activity; folic acid; glutamic acid; imidazo[2,1-b]pteridine; tetrahydroimidazo[2,1-b]pteridine
• ISSN: 1420-3049; 1420-3049
• DOI: 10.3390/molecules26020368

To date, no fused heterocycles have been formed on folic acid molecules; for this reason, and others, our target is to synthesize new derivatives of folic acid as isolated or fused systems. Folic acid reacted with ethyl pyruvate, triethyl orthoformate, ethyl chloroformate, thioformic acid hydrazide, and aldehydes to give new derivatives of folic acid - , . Moreover, It reacted with benzylidene malononitrile, acetylacetone, ninhydrin, ethyl acetoacetate, ethyl cyanoacetate, and ethyl chloroacetate to give the pteridine fused systems - , respectively. Ethoxycarbonylamino derivate reacted with some nucleophiles containing the NH group, such as aminoguanidinium hydrocarbonate, hydrazine hydrate, glycine, thioformic acid hydrazide, and sulfa drugs in different conditions to give the urea derivatives - , . Compound reacted with the same nucleophiles to give the methylidene amino derivatives - , . The fused compound reacted with thioglycolic acid carbon disulfide, malononitrile, and formamide to give the four cyclic fused systems - , respectively. The biological activity of some synthesized showed moderate effect against bacteria, but no effect shown towards fungi.