Novel quaternary ammonium carbapenems: 1.BETA.-Methyl-2-(5'-substituted pyrrolidinylthio)carbapenems.

Nitroimidazoles XIII. Synthesis of Substituted (1-Methyl-5-Nitro-2-Imidazolyl) Isoxazoles

The beta0diketone derivatives of nitroimidazole were synthesized from the reaction of magnesium salt of beta-ketoaccids 3 with imidazolide 4. The raction of beta-diketones with hydroxylamine hydrochloride afforded either the isoxazoles or the 5-hydroxyl-2-isoxazolines.

NITROIMIDAZOLES XI1 [I]: SYNTHESES OF TRISUBSTITUTED PYRAZOLES AND SUBSTITUTED (1 -METHYL-5-NITRO-2- IMIDAZOLYL) PYRIMIDINONES

The reaction of P-diketones 1 with phenyl hydrazine afforded 5-aryl-3-(1- methyl-5-nitro-2-imidazoly1)-1-phenylpyrazole (2) and 3-aryl-5-(1-methyl-5- nitro-2-imidazoly1) -1-phenylpyrazole (3). The reaction of diketones (1) with urea in the presence of p-toluenesulfonic acid gave 4-(or 6-)aryl-6-(or 4-)(1-methyl- 5-nitro-2-imidazolyl)-1-(lH)pyrimidones (4). The structures of all compounds w...

Synthesis and structure-activity relationships of 1beta-methylcarbapenems with quaternary ammonium side chains.

The synthesis and antibacterial activity of 1beta-methylcarbapenems with quaternary ammonium groups at the C-2 position have been studied. Two types of new carbapenem derivatives have been synthesized. These 1beta-methylcarbapenems, one type having a (2S,4S)-2-[1,1-dimethyl-2-(1-piperazinyl)carbonyl]pyrrolidinio-4-+ ++ylthio group and the other type having a (2S,4S)-2-(4-carbamoylmethyl-4-methy...

Testing quaternary ammonium germicides.

Development of Novel Quaternary Ammonium Linkers for Antibody-Drug Conjugates.

A quaternary ammonium-based drug-linker has been developed to expand the scope of antibody-drug conjugate (ADC) payloads to include tertiary amines, a functional group commonly present in biologically active compounds. The linker strategy was exemplified with a β-glucuronidase-cleavable auristatin E construct. The drug-linker was found to efficiently release free auristatin E (AE) in the presen...