In the pharmaceutical industry, co-crystals are becoming increasingly valuable as crystalline solids that can offer altered/improved physical properties of an active pharmaceutical ingredient (API) without changing its chemical identity or biological activity. In order to identify new solid forms of diclofenac-an analgesic with extremely poor aqueous solubility for which few co-crystal structur...

An RNA containing 2'-amino pyrimidines has been isolated using in vitro selection techniques that specifically and avidly (apparent Kd approximately 30 nM) binds a mouse monoclonal antibody called MA20. This 2'-amino-derivatized RNA is at least 10,000-fold more stable than unmodified RNA in serum, and can act as a decoy and block MA20 binding to its natural antigen, the human insulin receptor, ...

Pyrimidines represent an important class of heterocycles containing two nitrogen atoms at position 1 and 3 the six membered ring show wide range biological activities. Numerous methods for synthesis pyrimidine their diverse reactions offer enormous scope in field medicinal chemistry. Pyrimidine possesses spectrum activities including antitubercular, antibacterial, antifungal, antiviral, anti-in...

2-Amino-5-nitro-6-ribitylamino-4(3H)-pyrimidinone (7) was phosphorylated with chlorophosphoric acid yielding an isomer mixture containing about 63% of the 5'-phosphate 7a together with other monophosphates and bisphosphates of 7. Preparative HPLC afforded pure 7a. Catalytic hydrogenation of 7a yields the labile substrate of pyrimidine deaminase, 2,5-diamino-6-ribitylamino-4(3H)-pyrimidinone 5'-...

The distribution of purines and pyrimidines in desoxypentose nucleic acids prepared from a variety of animal and plant sources has been studied. 1. The nucleic acids were prepared from calf thymus, calf kidney, sheep spleen, horse spleen, chicken erythrocyte, turtle erythrocyte, trout sperm, shad testes, sea urchin sperm, wheat germ, and Pneumococcus Type III. 2. Separate hydrolyses were carrie...

Seven pyrimidines with a lipophilic substituent at position 5 have been investigated with respect to inhibition of both dihydrofolate reductases of Sarcoma 180 and Escherichia coli and site of inhibitory action in mammalian cells in culture. Of the 7 pyrimidines, 5 were competitive inhibitors of both dihydrofolate reductases, 1 was noncompetitive, and 1 produced no effect. The Sarcoma 180 enzym...

Protein kinase CK1? expression and activity is involved in different pathological situations that include neuroinflammatory neurodegenerative diseases. For this reason, protein has become a possible therapeutic target for these conditions. 5,6-fused bicyclic heteroaromatic systems resemble adenine of ATP represent optimal scaffolds the development new class competitive inhibitors. In particular...

In a preliminary report (1) a biotin deficiency in Streptococcus lactis 8039l was found to result, in a greatly diminished ability to convert ornit,hine and carbamyl phosphate to citrulline. In the present investigation a study of the conditions necessary to restore normal activity to biotindeficient, cells has been made. Normal activity is restored to biotindeficient, cells when the cells are ...