Drugs amine

HPMA copolymer Melphalan Amide bond between drug amine and variable oligopeptide spacer carboxyl None... 

Chitins Carboxymethyl chitin Mitomycin C Amide bond between drug amine and carrier carboxyl None N/A N/T Conjugate showed less anticancer activity than free drug against L1210 leukemia, but greater activity against B16 melanoma 52... 

Dextrans Anionically charged dextran Mitomycin C Amide bond between drug amine and hexamethyl spacer carboxyl Monoclonal antibody (A7) against human colon carcinoma and murine myeloma Amide bond between antibody lysine amine and spacer carboxyl Conjugate showed cytotoxicity against W 1116 colorectal carcinoma, but less activity than free mitomycin C NfT 53... 

Figure 3 Basic design of a drug-amine carrier conjugate for lung targeting.

Note that p-acetamidobenzenesulphonyl chloride will similarly react with primary and secondary amines, and the products, after hydrolysis of the acetyl group, may furnish notable drugs e.g., the condensation products with 2-amino-pyridine and 2-aminothiazole, after remo al of the acetyl groups, provide the drugs commonly known as sulphapyridine (M B 693) and sulphathidzole respectively. 

Methamphetannne is a notorious street drug One synthesis involves reductive amination of benzyl methyl ketone with methylamine What is the structure of methamphetamine ... 

Amines as Natural Products From Dyes to Sulfa Drugs... 

Acutrim 16 Hour Steady Control Tablets. Acuttim is an appetite suppressant diet aid available without a prescription and marketed by CIBA Consumer Pharmaceuticals. The active ingredient is phenylpropanolamine hydrochloride [154-41 -6] a sympathomimetic amine (see Antiobesity drugs). Acutrim dehvers its dosage at a precisely controlled rate for up to 16 hours. This is achieved through the OROS technology. 

Thiirane is more bactericidal than oxirane, and derivatives of 2-mei captomethylthiirane inhibit tuberculosis. The following pharmacological uses have been reported for compounds derived from thiirane derivatives gold complexes of the adducts of diethylphosphine and thiirane (antiarthritic), adducts of thiiranes and malononitrile (antibacterial, blood vessel dilators, muscle relaxants, sedatives), thermolysis products of thiirane 1-oxides and adducts of thiirane 1-oxides with sulfenyl chlorides (antibacterial), adducts of 2,3-diarylthiirene 1,1-dioxides with ynamines (antibacterial, parasiticidal), adducts of 2,3-diarylthiirene 1,1-dioxides with enamines (antifertility), adducts of p-aminophenylacetic esters with thiirane (immunosuppressants), adducts of amines and thiiranes (radioprotective drugs). 

Epinephrine itself does find some use in clinical medicine. The drug is used in order to increase blood pressure in cases of circulatory collapse, and to relax the bronchial muscle in acute asthma and in anaphylactic reactions. These activities follow directly from the agent s physiologic role. The biogenetic precursor of epinephrine, norepinephrine, has activity in its own right as a mediator of sympathetic nerve action. (An apocryphal story has it that the term nor is derived from a label seen on a bottle of a key primary amine in a laboratory in Germany N ohne... 

Further substitution of benzoic acid leads to a drug with antiemetic activity. Alkylation of the sodium salt of p-hydroxy-benzaldehyde (8) with 2-dimethylaminoethyl chloride affords the so-called basic ether (9). Reductive amination of the aldehyde in the presence of ammonia gives diamine, 10. Acylation of that product with 3,4,5-trimethoxybenzoyl chloride affords trimetho-benzamide (11). ... 

Careful metabolic work on this drug by a group of French workers showed that the agent was in fact cleaved to sulfanilamide (83) and the amine, 84, in vivo. Testing of the two fragments revealed that the activity of the drug resided entirely in the sulfanilamide fragment. That compound in fact showed full activity when administered alone in vitro or in vivo. ... 

The drugs are available by one of two fairly straightforward routes. Chlorosulfonation of acetanilide gives the corresponding sulfonyl chloride (88) reaction with the appropriate amine gives the intermediate, 89. Hydrolysis in either acid or base leads to the sulfanilamide (90). 

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