Synthesis of ciprofloxacin derivatives and screening their biological activities

What is it about?

Ciprofloxacin hydrochloride is the most widely used broad-spectrum fluoroquinolone antibacterial agent. Since antibiotic resistance is a major concern in the present time, more potent antibiotic with desirable biological properties have been in the hunt at present. With a view to examine the Structure-Activity-Relationship of ciprofloxacin, the latter has been converted into some derivatives. Secondary amino group of piperazine moiety was modified to yield five derivatives. Reaction of ciprofloxacin with acetic anhydride, Schotten–Baumann reaction of ciprofloxacin with benzoyl chloride, p-nitro benzoyl chloride, 3-(2-chloro-6-fluoro-phenyl)-5-methyl-isoxazole-4-carbonyl chloride (FCMIC), 3-(2-chloro phenyl)-5-methyl-isoxazole-4-carbonyl chloride (CMIC) yielded those derivatives. Later those derivatives,screening their biological properties. The derivatives showed varying degrees of antimicrobial activities. Most of the derivatives showed enhanced antimicrobial activities compared to the parent antibiotic ciprofloxacin. However para nitro derivatives showed significantly enhanced activities compared to ciprofloxacin.

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Why is it important?

In recent years the antibiotic resistance is a major concern all over the world in health sector. Finding out the desirable antibacterial agent is one of the prime interests of the present scientists. Anti-fungal activities of the synthesized drugs are also an another impotent issue.