Synthesis of some diazabicyclic compounds of expected non narcotic analgetic activity

The biologically active 4H-pyrido [1, 2-a] pyrimidin-4-ones [1] including some hexahydro derivatives [2] are non acidic non-steroidal anti-inflammatory agents. Other pyrido [1, 2-a] pyrimidines were reported as analgetic anti-inflammatory agents [3-8]. In a search of analgetic pharmacophore in condensed pyrimidines, the chemistry and analgetic activity of the bioisoster pyrimido-[1, 2-a] azepine [9] 1 was reported. This work found that ester, carbamate, thiosemicarbazide, semicarbazide, urea and acyl urea groups are of special value in the analgetic activity of 1. On the other h and, it was assumed that any changes in the structure of 1, that might add to its analgetic effect, would be beneficial

Synthesis of certain period [1,2-c] pyramid [5,4-e] pyrimidines of expected pharmacological interest

Five series of the titled nucleus were prepared. Enaminonitrile I reacted with oxalyl chloride and chloroacetyl chloride to afford the tricyclic compounds II and III, respectively. II reacted with various alcohols to give the corresponding ester, also III reacted with various amines to yield the corresponding compounds. The anti-inflammatory effect of some members showed significant results as compared with Diclofenac. Another derivatives were found to inhibit 50% of the histamine induced contraction of guinea pig ileum. It is worth mentioning that the animals treated with the test substances were more quiet and less aggressive than the control

Substituted nitrogen bridgehead heterocycles of potential smooth muscle relaxant and antihypertensive activities

Pyrrolo [1,2-c] pyrimidine derivatives I reacted with various acid chlorides to afford a number of 3-substituted pyrimido [5,4-e] pyrrolo [1,2-c] pyrimidines. The 3-chlorocarbonyl intermediate I-A reacted with different alcohols to give the corresponding esters. Moreover, 3-chloromethyl derivative I-B reacted with thiourea, alkoxides and sodium salts of aromatic acids to yield thiouronium salts, ethers and esters, respectively. Some members were tested as smooth muscle relaxant diuretic and hypotensive activities. It was shown that compound VII-a is the potent as hypotensive and diuretic agent. Also, it was noticed that, while all the test substances inhibit the uterine motility, VII-a stimulates the uterine motility in all stages

Synthesis of some novel heterocyclic compounds of potential antiallergic activity

Dicyanomethylidene 1a and its piperidine analogue 1b reacted with B-chloroethylisocyanate to afford unexpectedly the heterocycles: imidazo [1,2-c] pyrrolo [2,1-f] pryrimidine-10-carbonitrile and imidazo [1,2-c] pyrido [2,1-f] pyrimidine-11-carbonitrile hydrochlorides 3a and 3b respectively. Subsequent hydrolysis gave the corresponding carboxamides 4a,b and carboxylic acids 6a,b. The structures of the new nuclei have been confirmed by chemical and spectral means. Two compounds were subjected to pharmacological testing and have shown 50% inhibition of the histamine induced contraction of guinea pig ileum

Influence of supplemental selenium and vitamin E on immunobiological reactivity of sheep vaccinated with chlostridial vaccine

Forty ewes were vaccinated with Cl. perfringens vaccine during the last third of gestation period and supplemented according to the divided groups: The first group received selenium, the second received vitamin E, the third received both selenium and vitamin E and the fourth group served as control. The injected dose was 5 mg sodium selenite and 400 mg tocopherol. Selenium and /or vitamin E improved the antibody titers for clostridial toxiodes [beta and epsilon] in ewes and their lambs, by their intensification of protein synthesis. Better results were obtained when both selenium and vitamin E used simultaneously with the vaccine

Synthesis of certain 4 [3H] quinazolinone compounds containing imidazolinone and azomethine moieties

The synthesis of several 3-[4-arylindine-2-alkyl [aryl] 5[4H] imidazolon-1-yl] phenyl]-2-methyl-7-nitro-4 [3H]-quinazolinones are described. Structured establishment of the new compounds is substantiated by element analysis, IR and h- NMR spectra. Preliminary biological screening of some selected members showed no detectable antimicrobial activity in vitro, chloramphenicol and nystatin were included in the study for sake of comparison

Synthesis of certain 4 [3H] quinazolinones likely to possess CNN depressants and antimalarial activities

Several new 3-substituted 7-nitro-4 [3H] quinazolinones were prepared. The structures of the obtained compounds based on elemental analysis, IR and H-NMR spectra. Anti-convulsant and hypnotic activities of some compounds were tested and compared to phenytoin and pentobarbital sodium