Preparation and in vitro antibacterial activity of 9-O-glycosyloxime derivatives of erythromycin A, a new class of macrolide antibiotics.
نویسندگان
چکیده
9-O-Glycosyloxime derivatives of erythromycin A have been synthesized and their in vitro antibacterial activity compared with that of erythromycin A (1). This new class of macrolide antibiotics showed reduced antibacterial spectrum. However, some derivatives were as or more active than erythromycin A (1) against strains, responsible for respiratory track infections, such as Haemophilus influenzae, Moraxella catarrhalis or Streptococcus pneumoniae.
منابع مشابه
Studies on macrolide antibiotics I. Synthesis and antibacterial activity of erythromycin A 9-O-substituted oxime ether derivatives against Mycobacterium avium complex.
A series of erythromycin A 9-O-substituted oxime ether derivatives have been synthesized and evaluated for antibacterial activity against Mycobacterium avium complex (MAC) and Staphylococcus aureus. These compounds possessed stronger in vitro activity against MAC including macrolide-resistant strains than clarithromycin (2), although in vitro antibacterial activities of these compounds were les...
متن کاملSynthesis and antibacterial activity of (9S)-9-dihydroclarithromycin.
Clarithromycin1* (1, 6-O-methylerythromycin A, A-56268, TE-031) is a new macrolide currently undergoing clinical development. The excellent properties2) of 1 make it attractive for further synthetic modifications. It is knownthat, reduction of the 9-keto group of erythromycin A (2), for example with sodium borohydride, gives the corresponding secondary alcohol, predominantly as the 9(S) epimer,...
متن کاملAntibacterial activity of roxithromycin: a laboratory evaluation.
Roxithromycin, formerly known as RU 28965 (9-[O [(2-methoxyethoxy)methyl]oxime]-erythromycin), is a novel 14 atom-membered semisynthetic macrolide with an antibacterial spectrum directed towards Gram-positive cocci and bacilli, Gram-negative cocci and some Parvobacteriaceae. The in vitro antibacterial activity of roxithromycin was compared with those of erythromycin and spiramycin against 275 c...
متن کاملMacrolide antibiotics and pulmonary inflammation.
Many clinically effective therapeutic agents can exhibit localized and systemic effects that are manifestly different from their intended primary pharmacological mode of action. Macrolide antibiotics such as erythromycin and its derivatives are no exception. In addition to their antibacterial action, this class of antibiotics exhibits anti-inflammatory activity in a variety of airway diseases s...
متن کاملStructure-activity relationship studies on 4''-O-acyltylosin derivatives: significance of their 23-O-mycinosyl and 4''-O-acyl moieties in antimicrobial activity against macrolide-resistant microbes.
Essential roles for both the 23-O-mycinosyl and 4''-O-acyl moieties of 4''-O-acyltylosin derivatives in the expression of antimicrobial activity against multiple macrolide-resistant strains of Staphylococci and mycoplasmas were demonstrated by in vitro comparison of the MICs of erythromycin, josamycin, tylosin and its 3- and 4''-O-acyl derivatives, demycinosyltylosin (DMT) and its 3- and 4''-O-...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید
ثبت ناماگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید
ورودعنوان ژورنال:
- The Journal of antibiotics
دوره 49 10 شماره
صفحات -
تاریخ انتشار 1996