Abstract: A process is provided which yields derivatives of cephalosporins and penicillins. The process starts with 7-acylaminocephalosporin, or 6-acylaminopenicillin, then the latter compounds are treated with an organolithium compound, followed with t-butyl-hypochlorite. Finally, a defined reagent is added yielding a side chain on the carbon adjacent to the amino-nitrogen. Novel intermediate compounds are also described. The end compounds prepared are active against both gram-positive and gram-negative bacteria.

Abstract: Method of preparing antimicrobial compounds of the formula: ##STR1## comprising the following steps: (1) halogenating allyl halide to form 1,2,3-trihalopropane; (2) dehydrohalogenating the 1,2,3-trihalopropane to form 2,3-dihalo-1-propene;(3) treating the 2,3-dihalo-1-propene with a Grignard reagent of the formula R--MgHal, where R is as defined above, followed by treatment with magnesium, to form 3-(R-substituted)-2-magnesiumhalide)-1-propene;(4) treating the 3-(R-substituted)-2-(magnesiumhalide)-1-propene with cyanogen to form 3-(R-substituted)-2-cyano-1-propene; and(5) brominating the 3-(R-substituted)-2-cyano-1-propene to form the desired product.

Abstract: Antimicrobial compounds of the formula: ##STR1## wherein: Hal is bromine or chlorine; andR is halo; mono- or di-substituted mono- or diloweralkylamino wherein the loweralkyl substituents are hydroxy or loweralkanoyloxy; 4-morpholino; thiocyano; mercapto; straight or branched chain C.sub.1-8 alkylthio; mono- or di-substituted loweralkylthio wherein the substituents are hydroxy, amino, loweralkanoylamino, or loweralkoxycarbonyl; arylthio; loweralkylsulfoxy; or loweralkylsulfonyl;R.sup.1 is hydrogen; or loweralkyl;R.sup.2 is hydroxyloweralkyl; (CH.sub.2).sub.n COOR.sup.a, where R.sup.a is hydrogen, loweralkyl, or benzyl; and n is 1 to 3;R.sup.1 and R.sup.2 are taken together with an oxygen or nitrogen atom to form morpholino, piperazinyl, or piperazinyl which is N-loweralkyl substituted; andR.sup.3 is hydrogen; straight or branched C.sub.1-8 alkyl, provided that when R.sup.3 is hydrogen or C.sub.

Abstract: Antimicrobial compounds of the formula: ##STR1## wherein: Hal is bromine or chlorine; andR is halo; mono- or di-substituted mono- or diloweralkylamino wherein the loweralkyl substituents are hydroxy or loweralkanoyloxy; 4-morpholino; thiocyano; mercapto; straight or branched chain C.sub.1-8 alkylthio; mono- or di-substituted loweralkylthio wherein the substituents are hydroxy, amino, loweralkanoylamino, or loweralkoxycarbonyl; arylthio; loweralkylsulfoxy; or loweralkylsulfonyl;R.sup.1 is hydrogen; or loweralkyl;R.sup.2 is (CH.sub.2).sub.n COOR.sup.a, where R.sup.a is hydrogen, loweralkyl, or benzyl; and n is 1 to 3;R.sup.1 andR.sup.2 are taken together with an oxygen or nitrogen atom or form morpholino, piperazinyl, or piperazinyl which is N-loweralkyl substituted;R.sup.3 is hydrogen; straight or branched C.sub.1-8 alkyl; aryl; aryl substituted with up to two members selected from the group consisting of C.sub.1-3 alkyl, C.sub.1-3 alkoxy, halo, and mono- or di-C.sub.

Abstract: Antimicrobial compounds of the formula: ##STR1## wherein: Hal is bromine or chlorine; andR is halo; mono- or di-substituted mono- or diloweralkylamino wherein the loweralkyl substituents are hydroxy or loweralkanoyloxy; 4-morpholino; thiocyano; mercapto; straight or branched chain C.sub.1-8 alkylthio; mono- or di-substituted loweralkylthio wherein the substituents are hydroxy, amino, loweralkanoylamino, or loweralkoxycarbonyl; arylthio; loweralkylsulfoxy; or loweralkylsulfonyl;R.sup.1 is hydrogen; or loweralkyl;R.sup.2 is (CH.sub.2).sub.n COOR.sup.3, where R.sup.3 is hydrogen, loweralkyl, or benzyl; and n is 1 to 3; andR.sup.1 and R.sup.2 are taken together with an oxygen or nitrogen atom to form morpholino, piperazinyl, or piperazinyl which is N-loweralkyl substituted; are useful in various agricultural and industrial areas.

Abstract: Antimicrobial compounds of the formula: ##STR1## where R is C.sub.3-12 alkyl, straight or branched chain C.sub.3 -C.sub.8 cycloalkyl; C.sub.3-8 cycloalkylC.sub.1-3 alkyl; or saturated heterocyclic radical selected from the group consisting of pyrrolidinyl, tetrahydrofuranyl, tetrahydrothienyl, isoxazolidinyl, oxazolidinyl, isothiazolidinyl, pyrazolidinyl, imidazolidinyl, piperazinyl, and piperidinyl.

Abstract: Novel 4-[5(and 4)-substituted-2-thienyl]-3-hydroxy-3-pyrroline-2,5-diones are disclosed which inhibit glycolic acid oxidase and thus are useful in the treatment and prevention of calcium oxalate kidney stone formation. A novel process for their preparation is also disclosed.

Abstract: 2,4-Disubstituted-1,2,5-thiadiazol-3(2H)-one antimicrobials have broad spectrum antibacterial and antifungal activity. They are found to be especially useful in agriculture to protect plants against diseases such as leaf, stem, and fruit spotting, internal discoloration and decay of fruits and vegetables. These compounds are particularly active against diseases caused by the genera Pseudomonas, Xanthomonas, Erwinia, and Corynebacterium.

Abstract: 4-Hydroxy-5-substituted-3(2H)-isothiazolone-1,1-dioxide derivatives of the formula: ##STR1## where X and Y are independently selected from the group consisting of hydrogen, halogen, and C.sub.1-6 alkyl; provided that positions 2 and 6 of the substituted phenyl moiety may not be substituted by C.sub.3-6 alkyl; or a pharmaceutically acceptable salt thereof;useful in treating urinary tract, especially renal calcium oxalate lithiasis.

Abstract: Novel 4-alkylsubstituted-3-hydroxy-3-pyrroline-2,5-diones are disclosed which inhibit glycolic acid oxidase and thus are useful in the treatment and prevention of calcium oxalate kidney stone formation. A novel process for their preparation is also disclosed.

Abstract: 4-Hydroxy-5-substituted-3(2H)-isothiazolone-1,1-dioxide derivatives of the formula: ##STR1## where X and Y are independently selected from the group consisting of hydrogen, halogen, and C.sub.1-6 alkyl; provided that positions 2 and 6 of the substituted phenyl moiety may not be substituted; and n is 0 or 1;or a pharmaceutically acceptable salt thereof; useful in treating urinary tract, especially renal calcium oxalate lithiasis.

Abstract: The Antibiotics-875A are obtained from the controlled aerobic cultivation of Streptomyces hygroscopicus ATCC 39067. The Antibiotics-875A show in vitro and in vivo activity against gram positive and gram negative organisms including the genera; Staphylococcus, Streptococcus, Aerobacter, Escherichia, Klebsiella, Parlacolobactrum, Pseudomonas and Salmonella.

Abstract: 2,4-Dioxo-4-substituted-1-butanoic acid derivatives of the formula: ##STR1## where R is hydrogen or C.sub.1-4 alkyl; andL is a lipophilic group consisting essentially of ##STR2## where R' is (a) hydrogen; (b) C.sub.1-3 alkyl; (c) benzyl; (d) pyridyl C.sub.1-3 alkyl or (e) (3,4-dihydro-3-hydroxy-2H-1,5-benzodioxepin-3-yl) methyl; provided that positions 2 and 6 of the substituted phenyl moiety may not be substituted; or ##STR3## where R' has the same meaning as above; or a pharmaceutically acceptable salt thereof; useful in treating urinary tract, especially renal calcium oxalate lithiasis.

Abstract: Antimicrobial compositions for use in agriculture and methods of treatment are disclosed. The compounds are 3-amino-5,6-dihalopyrazine-2-carbonitrile.

Abstract: 2,3-Dihydro-substituted-5-(acyl)benzofuran-2-carboxylic acids, the pharmaceutically acceptable salt, ester and amide derivatives thereof and combinations of these compounds with antikaluretic agents are disclosed having diuretic-saluretic, uricosuric and antihypertensive activity.

Abstract: Antimicrobial compounds of the formula: ##STR1## wherein Hal is bromine or chlorine; R is C.sub.1-4 alkyl, straight or branched chain; and one of R.sup.1 and R.sup.2 is hydrogen and the other is selected from the group consisting of C.sub.3-8 cycloalkyl; C.sub.3-8 cycloalkyl C.sub.1-3 alkyl; phenyl; phenyl C.sub.1-3 alkyl; mono- or disubstituted phenyl or phenyl C.sub.1-3 alkyl wherein the substituents are halo, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, hydroxy, nitro, cyano, or trifluoromethyl; a heterocyclic radical selected from the group consisting of thienyl, furanyl, pyrrolyl, isoxazolyl, oxazolyl, isothiazolyl, thiazolyl, pyrazolyl, imidazolyl, pyridazinyl, pyrimidinyl, pyrazinyl, and pyridinyl, and N-oxides thereof; and a saturated heterocyclic radical selected from the group consisting of pyrrolidinyl, tetrahydrofuranyl, tetrahydrothienyl, isoxazolidinyl, oxazolidinyl, isothiazolidinyl, thiazolidinyl, pyrazolidinyl, imidazolidinyl, piperazinyl, and piperidinyl.

Abstract: Disclosed are N-acyl and carboxyl derivatives of the antibiotic thienamycin, which has the following structure: ##STR1## Such derivatives are useful as antibiotics. Also disclosed are processes for the preparation of such derivatives, pharmaceutical compositions comprising such derivatives and methods of treatment comprising administering such derivatives and compositions when an antibiotic effect is indicated.

Abstract: Statine (Sta), a naturally-occurring amino acid and closely related derivatives, are prepared by a novel method involving an oxidative route to the requisite chiral .alpha.-aminoaldehyde intermediate, L-leucinal; the novel method may be illustrated by the following reaction scheme: ##STR1## .

Abstract: Antimicrobial agents suitable for use in aqueous systems for their preservation against biodeterioration include substitutedpiperidinomethylpropenenitriles and propanenitriles. The unsaturated compounds are prepared by reaction of a suitable piperidine with cyano acetic acid and formaldehyde: the propane derivatives therefrom by nucleophilic addition.

Abstract: Novel cephalosporin compounds having a substituted or unsubstituted vinyl group at the 3-position are prepared by the reaction of a phosphoranylidene compound with a compound containing a carbonyl group. The novel cephalosporin compounds are active against a range of gram-negative and gram-positive microorganisms and are of value in human and veterinary medicine.