Roussel Uclaf

About: Roussel Uclaf is a based out in . It is known for research contribution in the topics: Alkyl & Alkoxy group. The organization has 1888 authors who have published 2338 publications receiving 36508 citations.

Process for the preparation of 21-hydroxy-20-keto-delta__ -steroids and new intermediate compounds formed in this process

Abstract: The invention relates to a new process for the preparation of 20-keto-.DELTA.16 steroids wherein a 17-isocyanosulfonylmethylene steroid is converted in one step into the new 20-isocyano-20-sulfonyl-.DELTA.16 steroid using an alkylating agent such as methylio-dide. The resulting steroid is hydrolyzed in a subsequent step to the corresponding 20-keto-.DELTA.16 steroid. The final products are suitable starting compounds for the preparation of therapeuti-cally useful steroids, comprising pregnanes and, particularly, progesterone derivatives.

Novel indoles in the treatment of pain

Abstract: 1-CARBOXYALKYL-2-METHYL-INDOLES OF THE FORMULA WHEREIN A is a divalent aliphatic hydrocarbon derived from a linear or branched alkyl, R is selected from the group consisting of cyclohexyl and an aromatic radical, R' is selected from the group consisting of halogen, trifluoromethyl, lower alkyl, lower alkoxy and N,N-dilower-alkylamino and R1 is selected from the group consisting of hydrogen and lower alkyl and a cation of a nontoxic, therapeutically acceptable base which possess anti-inflammatory and analgesic activity and their preparation.

Antibacterial activity of RU44790, a new N-tetrazolyl monocyclic beta-lactam.

Abstract: RU44790 belongs to a new class of synthetic monocyclic beta-lactam antibiotics which feature a bioisosteric tetrazole moiety instead of the more classical acidic functions at the N-1 position of the beta-lactam ring. Its antibacterial activity was evaluated against some 900 strains and was compared with those of other recent beta-lactam derivatives, especially aztreonam. RU44790 is endowed with potent activity against gram-negative bacteria. At less than or equal to 0.6 micrograms/ml, RU44790 inhibited 90% of all strains of the family Enterobacteriaceae with the exception of Citrobacter spp. (MIC for 90% of strains tested, 1.2 micrograms/ml). The activity was similar to that of aztreonam against strains that are normally susceptible to expanded-spectrum cephalosporins. On the other hand, the new compound was 10 to 100 times more potent than aztreonam and most of the other antibiotics tested against enterobacteria that produce chromosome-encoded or plasmid-mediated extended-spectrum beta-lactamases. Pseudomonas aeruginosa isolates were equally susceptible to both monobactams. RU44790 was inactive against staphylococci and had only marginal activity against streptococci (MIC for 50% of strains tested, 2.5 micrograms/ml). RU44790 was highly resistant to hydrolysis by various beta-lactamases, particularly cephalosporinases such as P99. The latter enzyme was also inhibited by the compound. RU44790 showed a high affinity for penicillin-binding protein 3 of Escherichia coli. The results suggest that RU44790 has good potential in the treatment of infections caused by gram-negative microorganisms.