Abstract: 2.beta.-Chloromethyl-2.alpha.-methylpenam-3.alpha.-carboxylic acid sulfone and salts and esters thereof were synthesized and found to be potent inhibitors of .beta.-lactamases.

Abstract: 5-Mercaptotetrazolyl-1-acetic acid is prepared by bromination with molecular bromine of tetrazolyl-1-acetic acid to produce 5-bromotetrazolyl-1-acetic acid which is then reacted with thiourea to displace the bromine and, after alkaline hydrolysis, to produce 5-mercaptotetrazolyl-1-acetic acid.

Abstract: This invention provides tetrapeptide derivatives of the formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are methyl, 1-methylethyl, 2-methylpropyl, 1-hydroxyethyl, 2-carboxyethyl or 4-aminobutyl and Y is ##STR2## wherein R.sup.3 is methyl, 1-methylethyl, 2-methylpropyl, 1-methylpropyl, hydroxymethyl, 1-hydroxyethyl, carboxymethyl, 2-carboxyethyl, 4-aminobutyl, 3-guanidinopropyl, benzyl or p-hydroxybenzyl excluding the compounds in which R.sup.1 and R.sup.2 are each 1-methylethyl and also R.sup.3 is carboxymethyl or 2-carboxyethyl, the first and leftmost .beta.-amino acid moiety in said tetrapeptide derivatives having the (2S,3R)-configuration and a primary amino group and the second, third and fourth .alpha.-amino acid moieties in said tetrapeptide derivatives having the L-configuration. These compounds have an inhibitory activity on several types of aminopeptidases.

Abstract: In the preferred embodiment of the present invention trimethylsilyl 7-trimethylsilyloxycarbonylaminodecephalosporanate was prepared by bubbling dry carbon dioxide into an anhydrous solution of trimethylsilyl 6-trimethylsilylaminodecephalosporanate and found to be a useful intermediate in the production of cefadroxil and cephalexin by its acylation in anhydrous media with the appropriate 2-phenylglycyl chloride hydrochloride. Other cephalosporins are produced by acylation of 7-trimethylsilyloxycarbonylaminoceph-3-em-4-carboxylic acids or esters having a variety of substituents at the 3-position.

Abstract: Certain cephalosporins having a heterocyclicthiomethyl group at the 3-position such as cefoperazone are prepared by reacting a solution of a 7-acylamidocephalosporanic acid having a free amino group as part of said acyl substituent with about an equi-molar amount of the thiolester ##STR1## wherein --S-Het is the desired conventional heterocyclicthio group which displaces the 3-acetoxy group of the starting acid and ##STR2## is the conventional acyl group which displaces a hydrogen on the free amino group which is part of the acyl substituent of the starting 7-acylamidocephalosporanic acid.

Abstract: In the preferred embodiment of the present invention trimethylsilyl 7-trimethylsilyloxycarbonylaminodecephalosporanate was prepared by bubbling dry carbon dioxide into an ahydrous solution of trimethylsilyl 6-trimethylsilylaminodecephalosporanate and found to be a useful intermediate in the production of cefadroxil and cephalexin by its acylation in anhydrous media with the appropriate 2-phenylglycyl chloride hydrochloride. Other cephalosporins are produced by acylation of 7-trimethylsilyloxycarbonylaminoceph-3-em-4-carboxylic acids or esters having a variety of substituents at the 3-position.

Abstract: Trimethylsilyl or another easily hydrolyzed ester of 6-trimethylsilyloxycarbonylaminopenicillanic acid was prepared by bubbling dry carbon dioxide into an anhydrous solution of the corresponding 6-trimethylsilylaminopenicillanate and found to be a useful intermediate in the production of penicillins, e.g., amoxicillin and ampicillin, by its acylation in anhydrous media with the appropriate acid chloride or acid chloride hydrochloride.

Abstract: A stable, sterile aqueous solution of cisplatin in a sealed container such as an ampul or vial in unit dosage form suitable for intravenous administration to man is provided which has a concentration of cisplatin between about 0.1 and about 1.0 mgm./ml. and a pH in the range of 2.0 to 3.0 or preferably about 2.5. It can also contain sodium chloride and mannitol.

Abstract: 3',4'-Dideoxy derivative and 1-N-((S)-.alpha.-hydroxy-.omega.-aminoalkanoyl)-3',4'-dideoxy derivative of kanamycin A are now synthetized from kanamycin A and show a wider and/or higher antibacterial activity than the parent kanamycin A so that they are useful in therapeutic treatment of infections by gram-negative and gram-positive bacteria, including drug-resistant strains thereof.

Abstract: Certain 7-acylamido-3-(1-carboxy-loweralkyl-tetrazol-5-ylthiomethyl)-3-cephem-4-ca rboxylic acids and their salts and easily hydrolyzed esters of the 4-carboxyl group were synthesized and found to be potent antibacterial agents which exhibited good aqueous solubility. In a preferred embodiment the 7-substituent was 2'-aminomethylphenylacetamido.

Abstract: 7-[D-.alpha.-(4-Hydroxy-1,5-naphthyridine-3-carboxamido)-.alpha.-phenyl (and thienyl and substituted phenyl) acetamido]-3-(2-, 3- or 4-N,N-dimethylaminomethyl-pyridinium)methyl-3-cephem-4-carboxylates were synthesized and found to have potent antibacterial activity in vitro especially against many strains of Pseudomonas aeruginosa.

Abstract: Trimethylsilyl or another easily hydrolyzed ester of 6-trimethylsilyloxycarbonylaminopenicillanic acid was prepared by bubbling dry carbon dioxide into ananhydrous solution of the corresponding 6-trimethylsilylaminopenicillanate and found to be a useful intermediate in the production of penicillins, e.g., amoxicillin and ampicillin, by its acylation in anhydrous media with the appropriate acid chloride or acid chloride hydrochloride.

Abstract: Ceforanide is produced by the reduction in aqueous solution of a water-soluble salt 7-(2-azido-methylphenylacetamido)-3-(1-carboxymethyltetrazol-5-ylthiomethy l)-3-cephem-4-carboxylic acid using a borane-amine complex and Raney nickel.

Abstract: A new physiologically active substance named esterastin is now provided, which inhibits the activity of esterase and is useful as an immunosuppressive drug. Esterastin is produced by cultivating a micro-organism Streptomyces MD4-C1 identified as FERM-P 3723 or ATCC. 31336 in a culture medium under aerobic conditions and recovering it from the resulting culture.

Abstract: Bestatin, which is [(2S,3R)-3-amino-2-hydroxy-4-phenylbutanoyl]-L-leucine, and related compounds which inhibit aminopeptidase B, leucino aminopeptidase and Bleomycin hydrolase, enhance the anti-tumor effect of Bleomycin and exhibit an antifertility effect were synthesized and tested.

Abstract: Trimethylsilyl or another easily hydrolyzed ester of 6-trimethylsilyloxycarbonylaminopenicillanic acid was prepared by bubbling dry carbon dioxide into an anhydrous solution of the corresponding 6-trimethylsilylaminopenicillanate and found to be a useful intermediate in the production of penicillins, e.g., amoxicillin and ampicillin, by its acylation in anhydrous media with the appropriate acid chloride or acid chloride hydrochloride.

Abstract: In the preferred embodiment of the present invention trimethylsilyl 7-trimethylsilyloxycarbonylaminodecephalosporanate was prepared by bubbling dry carbon dioxide into an anhydrous solution of trimethylsilyl 6-trimethylsilylaminodecephalosporanate and found to be a useful intermediate in the production of cefadroxil and cephalexin by its acylation in anhydrous media with the appropriate 2-phenylglycyl chloride hydrochloride. Other cephalosporins are produced by acylation of 7-trimethylsilyloxycarbonylaminoceph-3-em-4-carboxylic acids or esters having a variety of substituents at the 3-position.

Abstract: .beta.-Methoxyethoxymethyl esters of cephalosporins and penicillins are exemplified by such esters of hetacillin and heta-amoxicillin were synthesized and found to exhibit advantageous biological properties.

Abstract: New routes are provided for the synthesis of 3',4'-dideoxykanamycin B which is effective in inhibiting kanamycin-resistant organisms from kanamycin B through new intermediate, of which a fundamental process comprises a new reaction of a 3',4'-epoxy derivative of amino- and hydroxyl-protected kanamycin B with a xanthate to form a corresponding 3',4'-dideoxy-3'-eno derivative followed by removal of the amino- and hydroxyl-protecting groups thereof and by hydrogenation of the resulting 3',4'-dideoxy-3'-eno-kanamycin B. A 3',4'-episulfide derivative corresponding to the 3',4'-epoxy derivative which is formed as second product in the reaction of 3',4'-epoxy derivative with xanthate is also used as intermediate for the preparation of 3',4'-dideoxykanamycin B.

Abstract: A new physiologically active substance named esterastin is now provided, which inhibits the activity of esterase and is useful as an immunosuppressive drug. Esterastin is produced by cultivating a microorganism Streptomyces MD4-C1 identified as FERM-P 3723 or ATCC. 31336 in a culture medium under aerobic conditions and recovering it from the resulting culture.