Ceforanide

Abstract

Ceforanide is a 'second generation' cephalosporin administered intravenously or intramuscularly. It is similar to cefamandole and cefonicid in its in vitro superiority to 'first generation' cephalosporins against several species of Enterobacteriaceae as well as its activity against Haemophilus influenzae, including beta-lactamase-producing strains. Its activity against Staphylococcus aureus is less than that of cefamandole, cefuroxime and first generation cephalosporins. The in vitro activity against Neisseria gonorrhoeae is excellent. Pseudomonas, Acinetobacter and Serratia species, and Bacteroides fragilis are resistant, as are many strains of Proteus and Providencia species. The elimination half-life is relatively long, although shorter than that of cefonicid, and in most clinical trials ceforanide has been administered twice daily. It appeared to be comparable in therapeutic efficacy to procaine penicillin and cephazolin in the treatment of patients with community-acquired pneumonia, to cephazolin in the treatment of skin and soft tissue infections due to S. aureus or beta-haemolytic streptococci and to cefapirin in S. aureus endocarditis in parenteral drug abusers. Also, it was comparable in efficacy to cephalothin in the prophylaxis of infection in patients undergoing open heart surgery or vaginal hysterectomy, and to cephazolin in patients undergoing cholecystectomy. Thus, ceforanide is an alternative to first and certain other second generation cephalosporins in several important therapeutic and prophylactic situations. It has no advantage over other cephalosporins with regard to spectrum of antibacterial activity, but has a longer half-life than other second generation cephalosporins, except cefonicid, and can be administered according to a twice daily dosage schedule.

Repurposing of drugs against methyltransferase as potential Zika virus therapies

“…All 28 compounds showed a favorable binding affinity toward NS5, indicating that they can act as inhibitors. From this result we selected five compounds that showed good binding affinity from the three docking software which do not directly target human receptors except Ol_Me; however, they showed binding to the bacterial or viral receptors 45 – 47 . The details of binding energy, hydrogen bond interactions, and other interacting residues are shown in Supplementary Table 2 .…”

Integrated Drug Expression Analysis for leukemia: an integrated in silico and in vivo approach to drug discovery

“…In particular, we tested sulfasalazine, fluoxetine, clozapine, betulinic acid, and ceforanide, which were originally intended to treat arthritis, depression, schizophrenia, viral infections, and bacterial infections, respectively 42–46 . All five of these drugs were predicted to impact patient survival via pharmacological activity as shown by Figs.…”

One-Pot Parallel Synthesis of 5-(Dialkylamino)tetrazoles

“…Whereas 5-substituted tetrazoles are well-known bioisosteres of carboxylic acid function, 1,5-disubstituted derivatives can be used to mimic the cis configuration of the amide bond, , which is higher in energy to the commonly found trans configuration (Figure A). Recently, the 1-alkyl-5-(alkylamino)­tetrazole motif was envisioned as a potential replacement of the alkyl urea moiety, which is present in the structures of dozens therapeutics. , 1,5-Disubstituted tetrazoles are represented by a series of approved cephalosporin antibiotics (e.g., cefmetazole, , ceforanide , ) and antiplatelet therapeutic cilostazol , (Figure B). Therefore, access to the diverse library based on an N-substituted 1-alkyl-5-aminotetrazole scaffold 1 became the prime objective of the current work.…”

“…Recently, the 1-alkyl-5-(alkylamino)tetrazole motif was envisioned as a potential replacement of the alkyl urea moiety, 20 which is present in the structures of dozens therapeutics. 21,22 1,5-Disubstituted tetrazoles are represented by a series of approved cephalosporin antibiotics (e.g., cefmetazole, 23,24 ceforanide 25,26 ) and antiplatelet therapeutic cilostazol 27,28 (Figure 1B). Therefore, access to the diverse library based on an N-substituted 1-alkyl-5-aminotetrazole scaffold 1 became the prime objective of the current work.…”