Boholmycin antibiotic

#This invention is directed to novel antibiotics, to a novel microorganism for producing the antibiotics, to a method of producing the antibiotic utilizing the microorganism, to compositions containing the antibiotics and to a method of treating bacterial infections with the antibiotics.

#Previous aminoglycoside antibiotic complexes have been reported in literature such as in J. Antibiotics 29:1137-1146 (1976) which discusses sorbistin. These aminoglycosides possess specific antibacterial activity.

#It is an object of the instant invention to produce an aminoglycoside antibiotic having broad spectrum activity. Broad spectrum activity is used herein to mean possessing antibacterial activity to Gram-positive, Gram-negative and acid-fast bacteria. It is a further object of the instant invention to provide an aminoglycoside antibiotic complex which possesses antibacterial aciivity against bacterial strains which are resistant to previously known aminoglycoside antibiotics.

#The following are presented in the drawings:

#FIG. 1--.sup.13 C-NMR spectrum of boholmycin hydrochloride at 20 MHz, in D.sub.2 O at PD 5.0;

#FIG. 2--Infrared absorption spectrum of boholmycin hydrochloride in KBr;

#Boholmycin and its pharmaceutically acceptable salts are water-soluble, weakly basic antibiotics. They are freely soluble in water, slightly soluble in methanol and ethanol but practically insoluble in other organic solvents. Boholmycin gives a positive reaction in ninhydrin and anthrone tests, but is negative to Tollen's and Sakaguchi reagents. The antibiotic is reasonably stable in neutral and acidic solution but unstable in alkaline solution.

#The dihydrochloride salt of boholmycin is characterized by physico-chemical properties as set forth in Table 1 below. In this table the .sup.13 C-NMR spectrum of boholmycin dihydrochloride is that depicted in FIG. 1. The IR spectrum of boholmycin dihydrochloride in KBr is depicted in FIG. 2 and the .sup.1 H-NMR spectrum of boholmycin dihydrochloride is depicted in FIG. 3.

#TABLE 1 ______________________________________ Nature white amorphous powder M.p. 214-219.degree. C. (dec.) [.alpha]sub.D.sup.28 +52.degree. (c 0.5, H.sub.2 O) Elemental analysis Calcd. for C.sub.27 H.sub.48 N.sub.4 O.sub.21.2HCl.4H.sub.2 O C 35.65, H 6.43, N 6.16, Cl 7.80 Found C 35.44, H 6.00, N 5.96, Cl 8.13 Mass spectrum (FD-MS) m/z 787 (M + Na), 765 (M + H) UV no absorption above 210 nm .sup.13 C--NMR in ppm (multiplicity): 31.7 (q), 56.2 (d), 61.3 (t), 61.4 (d), 61.8 (t), 62.4 (t) 64.1 (d), 68.0 (d), 69.0 (d), 70.6 (d), 71.4 (d), 71.7 (d) 71.9 (d), 72.4 (d), 74.2 (d), 74.4 (d), 76.3 (d), 77.3 (d) 77.7 (d), 81.6 (d), 92.9 (d), 100.9 (d), 102.6 (d), 158.4 (s), 159.2 (s) ______________________________________