7-{2-Hydroxy-3-[4-(2-phenoxyethyl)-piperazinyl-1-yl]-propyl}-1,3-di-methyl-3,7-dihydro-1H-purine-2,6-dione dihydrochloride (2), and several of its 8-alkylamino substituted derivatives (11-17) were synthesized and tested for electrocardiographic, antiarrhythmic and hypotensive activity. Also their alpha(1)- and alpha(2)-adrenoreceptor affinities were determined. It was found that compound 2, and...

Department of Pharmaceutical technology, Meerut Institute of Engineering and Technology, Meerut. ABSTRACT Pyrazole and pyrimidine derivatives attracted organic chemists due to their various biological and chemotherapeutic significance. Pyrazolopyrimidines and related fused heterocycles are of important as probable bioactive molecules. The heterocyclic fusion of pyrimidine ring and pyrazole ring...

A model for computing image ow in image sequences containing a very wide range of instantaneous ows is proposed. This model integrates the spatio-temporal image derivatives from multiple temporal scales to provide both reliable and accurate instantaneous ow estimates. The integration employs robust regression and automatic scale weighting in a generalized brightness constancy framework. In addi...

Three series of nucleotide analogues were synthesized and evaluated as potential CD73 inhibitors. Nucleobase replacement consisted in connecting the appropriate aromatic or purine residues through a triazole moiety that is generated from 1,3-dipolar cycloaddition. The first related to 4-substituted-1,2,3-triazolo-?-hydroxyphosphonate ribonucleosides. Additional also obtained, which phosphonate ...

Extensive efforts by the Burroughs-Wellcome group, the Sloan-Kettering group, and others have led to a considerable knowledge of purine antagonists that inhibit the growth of bacteria, experimental neoplasms, and human leukemias (18). Although 6-mercaptopurine (6-MP) is the most widely employed purine antagonist from the clinical standpoint, "related compounds, thioguanine, 6-chloropurine, 6-me...

Thymidine monophosphate kinase (TMPK) from Mycobacterium tuberculosis (TMPKmt) is an attractive target for the design of specific inhibitors. This fact is the result of its key role in the thymidine pathway and of unique structural features in the active site observed by X-ray crystallography, especially in comparison to its human counterpart (TMPKh). Different 5-modified thymidine derivatives,...

Fulp et al., “Diphenyl Purine Derivatives as Peripherally Selective Cannabinoid Receptor 1 Antagonists,” Journal of Medicinal Chem istry, 2012, pp. 10022-10032, vol. 55, No. 2. Griffith et al., “Discovery of 1-9-(4-Chlorophenyl)-8-(2chlorophenyl)-9H-purin-6-yl)-4-ethylaminopiperidine-4-carbox ylic Acid Amide Hydrochloride (CP-945,598), a Novel, Potent, and Selective Cannabinoid Type 1 Receptor ...

Demain, Arnold L. (Merck Sharp & Dohme Research Laboratories, Division of Merck & Co., Inc., Rahway, N.J.). Nutrition of "adenineless" auxotrophs of yeasts. J. Bacteriol. 88:339-345. 1964.-Nutritional studies on 29 "adenineless" yeast strains were carried out. In no case could guanine, xanthine, or their ribonucleosides or ribonucleotides be used to satisfy the purine requirement. The cultures ...

Some alkyl and aryl derivatives of 9H-purine-6-thiol were synthesized and evaluated in vitro and in vivo for potential antithyroid effects. Spectrophotometric studies demonstrated 1:1 charge transfer complexation between iodine and these compounds with quite high values of the formation constants. The blood assays of rats treated with these compounds revealed significant antithyroid activity fo...

Brucella abortus 2308 derivatives with mini-Tn5 insertions in purE, purL, and purD display significant attenuation in the BALB/c mouse model, while isogenic mutants with mini-Tn5 insertions in pheA, trpB, and dagA display little or no attenuation in cultured murine macrophages or mice. These experimental findings confirm the importance of the purine biosynthesis pathways for the survival and re...