Glaxosmithkline Istrazivacki Centar Zagreb D.o

Glaxosmithkline Istrazivacki Center Zagreb

Karmen Brajsa

Nedjeljko Kujundzic

Mirjana Bukvic Krajacic

The invention relates to substituted 9a-N-{N'-[4-(sulfonyl)phenyl]carbamoyl} derivatives of 9-deoxo-9-dihydro-9a-aza-9a-homoerithromycin A and 5-0-desosaminyl-9-deoxo-9-di-hydro-9a-aza-9a-homoerithronolide A, novel semisynthetic macrolide antibiotics of the azalide series general formula (1), wherein R represents H or cladinosyl moiety and R1 represents chloro, amino, phenylamino, 2-pyridylamino, 3,4-dimethyl-4-isoxalylamino and 5-methyl-3-isoxazolylamino group, and pharmaceutically acceptable addition salts thereof with inorganic or organic acids. to the process for their preparation of pharmaceutical composition as well as the use their compositions for sterilization rooms and medical instruments as well as for protection of wall and wooden coatings 

Substituted 9a-N-(N'-(sulfonyl)phenylcarbamoyl)derivatives of 9-deoxo-9-dihydro-9a-aza-9a-homoerithomycin A and 5-0-desosaminyl-9-deoxo-9-dihydro-9-a-aza-9a-homoerithronolide A

The invention relates to N&#x2033;-substituted 9a-N-(N'-carbamoyl-&#x3b3;-aminopropyl), 9a-N-(N&#x2032;-thiocarbamoyl-&#x3b3;-aminopropyl), 9a-N-[N&#x2032;-&#x3b2;-cyanoethyl)-N&#x2032;-carbamoyl-&#x3b3;-aminopropyl] and 9a-N-[N&#x2032;-&#x3b2;-cyanoethyl)-N&#x2032;-thiocarbamoyl-&#x3b3;-am inopropyl] derivatives of 9-deoxo-9-dihydro-9a-aza-9a-homoerithromycin A and 5-O-desosaminyl-9-deoxo-9-dihydro-9a-aza-9a-homoerithronolide A, novel semi-synthetic macrolide antibiotics of the azalide series, of the general formula 1, wherein R represents H or cladinosyl moiety, Rrepresents H or &#x3b2;-cyanoethyl moiety, Rrepresents isopropyl, 1-naphtyl, 2-naphtyl, benzyl, 2-(trifluoromethyl)phenyl, 3-phenylpropyl, &#x3b2;-phenylethyl, ethoxycarbonyl-methyl, 1-(1-naphtyl)ethyl, 3,4,5-trimethoxyphenyl and 2,4-dichlorophenyl group, and X represents O and S, and their acceptable addition salts thereof with inorganic or organic acids, to the process for preparation of their pharmaceutical compositions as well as the use their compositions in the treatment of bacterial infections.

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Zagreb, Croatia

Karmen Brajsa