title: Novel pyridopyrimidine derivatives as inhibitors of stable toxin a (STa) induced cGMP synthesis.
abstract: A series of pyridopyrimidine derivatives were synthesized and evaluated for their ability to inhibit cyclic nucleotide synthesis in the presence of stable toxin a of Escherichia coli. The structure activity relationships around the basic core structure were examined and examples with better activity and potentially better pharmacological properties are presented.
authors.affiliation: Department of Pharmacology and Toxicology, The University of Texas Medical Branch, Galveston, TX 77555-0650, USA.
authors.forename: Eric A
authors.initials: EA
authors.lastname: Tanifum
authors.forename: Alexander Y
authors.initials: AY
authors.lastname: Kots
authors.forename: Byung-Kwon
authors.initials: BK
authors.lastname: Choi
authors.forename: Ferid
authors.initials: F
authors.lastname: Murad
authors.forename: Scott R
authors.initials: SR
authors.lastname: Gilbertson
mesh_terms: D001427:Bacterial Toxins / Q000378:metabolism*; D045744:Cell Line, Tumor; D006152:Cyclic GMP / Q000096:biosynthesis*; D004768:Enterotoxins / Q000378:metabolism*; D004926:Escherichia coli / Q000378:metabolism; D029968:Escherichia coli Proteins; D006162:Guanylate Cyclase / Q000037:antagonists & inhibitors / Q000378:metabolism; D006801:Humans; D011743:Pyrimidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D000074261:Receptors, Enterotoxin; D050705:Receptors, Guanylate Cyclase-Coupled; D018000:Receptors, Peptide / Q000037:antagonists & inhibitors / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D001427:Bacterial Toxins; D004768:Enterotoxins; D029968:Escherichia coli Proteins; D011743:Pyrimidines; D018000:Receptors, Peptide; C034151:heat stable toxin (E coli); D006162:Guanylate Cyclase; D000074261:Receptors, Enterotoxin; D050705:Receptors, Guanylate Cyclase-Coupled; D006152:Cyclic GMP