Biomedical subjects

V Kalcheva

Publications and source records attributed to V Kalcheva.

At least 19 recordsLinked to original sources

PubMed2001

Matrix-assisted laser desorption/ionization, fast atom bombardment and plasma desorption mass spectrometry of polyethylene glycol esters of (2-benzothiazolon-3-yl)acetic acid.

Fast atom bombardment (FAB), matrix-assisted laser desorption/ionization time-of-flight (MALDI-TOF) and plasma desorption (PD) mass spectra of newly synthesized polyethylene glycols (PEGs), (M(w) 600-4000 Da) chemically modified with biologically active (2-benzothiazolon-3-yl)acetyl end-groups are described (products 1-6). The spectra were also used for the determination of the molecular mass characteristics (number average (M(n)) and weight average (M(w)) molecular masses) of the initial and modified PEGs. As expected, M(n) and M(w) of the modified samples are higher than those of the non-modified samples. However, it is shown that molecular mass dispersity (determined by the comparison of the polydispersity indices (PDI = M(w)/M(n)) of both types of PEGs) essentially do not change during this modification. The FAB mass spectra, together with molecular species, show the presence of abundant [M + Na](+) ions of product 1 and [M + Na + H](+) species of 2 and 3, and [M + Na + 2H](+) of product 4. Two main series of fragment ions, derived from the cleavage of the ether bonds, are observed. The number fractions of the molecular adduct ions and fragment adduct ions, determined from the FAB and PD mass spectra of the modified PEGs, are compared. The MALDI-TOF mass spectra of compounds 1-6 show the presence of two series of polymers. The most abundant peaks are due to [M + Na](+) and [M + K](+) ions originating from the polymers, in which the two terminal hydroxyl groups of PEGs are esterified with (2-benzothiazolon-3-yl)acetic acid. The less abundant peaks are due to the monosubstituted polymers.

Journal Article↗

PubMed1992

Penicillin amidase-catalysed transfer of low specific acyl moiety. Synthesis of 7-benzoxazolonylacetamido desacetoxycephalosporanic acid.

The methyl ester of 2-benzoxazolon-3-yl-acetic acid was used as an acyl donor in the penicillin amidase-catalysed transfer reaction to 7-aminodesacetoxycephalosporanic acid. The synthesis of 7-(2-benzoxazolon-3-yl-acetamido)-desacetoxycephalosporanic acid was carried out as a kinetically controlled reaction. A characteristic feature of this system is that the benzoxazolone derivatives are very low specific substrates for penicillin amidase (the kcat/Km values for their hydrolysis were shown to be 10(5)-fold lower compared to the corresponding values for phenylacetyl derivatives). Nevertheless, penicillin amidase proved to be an effective catalyst for the synthesis of these new cephem derivatives (50% yield for 6 h). The reason is the observed unusually high value for the transferase-hydrolase activity ratio. The determined value for (k3'/k3)app = 120,000 implies that in this case of low specific acyl moiety, penicillin amidase acts more like a transferase than a hydrolase. The maximum yield has been increased up to 70% by lowering the reaction temperature and stepwise feeding of the reaction medium with the acyl component. The results obtained extend the potential of the penicillin amidase as a catalyst for the synthesis of a new group of biologically active cephem derivatives.

Acylation↗

PubMed1991

Synthesis and antimicrobial evaluation of some cephem derivatives.

Two novel cephem derivative series were synthesized: 7-(D-alpha-aminophenyl-acetamido-)-3-methyl-3-cephem-4-carboxylic acid monohydrate (Cephalexin) derivatives and those of 7-amino-3-(1-methyl-1H-tetrazol-5-yl)-thio methyl-3-cephem-4-carboxylic acid (7-AMTCA). The antimicrobial activity of the prepared compounds was studied and compared to that of known cephalosporin antibiotics of the first generation against 12 standard strains and 189 clinical isolates of Gram-positive and Gram-negative microorganisms. The Cephalexin derivatives 4a-f show a narrow activity spectrum and are inactive while 5c and 5d are more active than the Cephalexin and Cephazolin antibiotics against clinically isolated S. aureus and S. epidermidis strains.

Anti-Bacterial Agents↗

PubMed1990

Synthesis and in vitro activity of new cephalosporin derivatives containing a benzoxazolone ring.

New cephalosporin derivatives containing a benzoxazolone ring in the side acylamino chain are synthesized using chlorides of non-substituted and halogen substituted (2-benzoxazolone-3-yl) acetic acids for the acylation of the 7-aminodesacetoxy-cephalosporanic acid and 7-amino-cephalosporanic acid amino group. Some of these new compounds exhibit a biological activity higher than that of cephalexin and cephazolin against clinical strains of Staphylococcus aureus, Staphylococcus epidermidis and Streptococcus group A and B.

Anti-Bacterial Agents↗

PubMed1990

[A modified technic of preoperative acute normovolemic hemodilution--the advantages and economic effect of its use in planned colorectal surgery].

In a prospective and comparative study were included 129 patients undergone planned operation for colorectal cancer. They were divided in two randomized groups: Group A consisted of 65 patients operated under conditions of preoperative acute normovolemic hemodilution (PANHD) by an own modified technique with Ringer-lactate and hemodex. Group B (control) included 64 patients operated with the use of homologous blood substitution. The results in the two groups were compared as to: intra- and postoperative blood transfusions; time (in days) of postoperative treatment; number of postoperative complications. Statistically significant differences (p less than 0.001) referrable to all three compared values were found. The modified PANHD technique in planned colorectal surgery is safer for the patients than the so far suggested techniques and may readily gain acceptance with the use of solutions of domestic produce. It leads to significant decrease in homologous blood transfusion, shortening the postoperative stay in hospital of patients subjected to hemodilution. The number of patients in whom postoperative complications developed was reduced.

Adult↗

PubMed1990