Carboxylic biological activity

Pharmaceuticals and Agrochemicals. Thioglycohc acid and its esters are useful as a raw material to obtain biologically active molecules. In cephalosporine syntheses, (4-pyridyl)thioacetic acid [10351 -19-8] (65) and trifluoromethane (ethyl) thioglycolate [75-92-9] (66) are used as intermediates. Methyl-3-ainino-2-thiophene carboxylate can be used as intermediate for herbicidal sulfonylureas (67) and various thiophenic stmctures (68). 

Pyromucic acid — see Furan-2-carboxylic acid Pyronaridine biological activity, 2, 625... 

AH-Pyrrolo[3,4-c]isoxazole, 3-amino-biological activity, 6, 1024 4H-Pyrrolo[3,4- c]isoxazole-5(6/7)-carboxylic acid, 3-amino-ethyl ester... 

Thieno[3,4-d]isothiazole, 2,3-dihydro-3-oxo-1,1-dioxide, 6, 989 biological activity, 6, 1024 Thieno[2,3-c]isothiazole-3-carboxylic acid synthesis, 6, 1023... 

Specific biological activity of carboxylic acids peroxide derivatives in compaiison with their oxidation ability and ionization degree in aqueous solutions has been considered. Peroxyoctanoic, diperoxynonandioic and diperoxydecandioic acids give the most intense bactericidal effect among researched cai boxylic acids peroxide derivatives. The perspectives of use of the aliphatic middle-chain peracid C8-C9 as anti-infective agents have been discussed. 

Finally, the quinoline ring can be methylated at the 3 position with retention of biologic activity. The starting quinoline is prepared by the same scheme as that used for the desmethyl compound by substituting the methylated oxosuccinate ester, S6, in the sequence. The initial quinoline carboxylate (87) is taken on to the dichloro compound (88) by the standard reactions. Condensation with the ubiquitous diamine (76) affords sontoquine (89)... 

More recently, self-assembling 3//-azepine monolayers on a gold surface have been obtained by the photodecomposition of bis ll-[(4-azidobenzoyl)oxy]undec-l-yl disulfide.284 Other than some alkyl and aryl 177-azepine-l-carboxylates, which possess fungicidal activity, particularly against Sclerotium rolfsii,104 the unsaturated azepine systems surveyed in this section do not have any notable biological activity. 

In addition to effects on biochemical reactions, the inhibitors may influence the permeability of the various cellular membranes and through physical and chemical effects may alter the structure of other subcellular structures such as proteins, nucleic acid, and spindle fibers. Unfortunately, few definite examples can be listed. The action of colchicine and podophyllin in interfering with cell division is well known. The effect of various lactones (coumarin, parasorbic acid, and protoanemonin) on mitotic activity was discussed above. Disturbances to cytoplasmic and vacuolar structure, and the morphology of mitochondria imposed by protoanemonin, were also mentioned. Interference with protein configuration and loss of biological activity was attributed to incorporation of azetidine-2-carboxylic acid into mung bean protein in place of proline. 

Niacin (Fig. 1) is a collective name for all vitamers having the biological activity associated with nicotinamide (= pyridine-3-carboxamide), including nicotinic acid (= pyridine-3-carboxylic acid) and a variety of pyridine nucleotide structures. 

Biological activity tests on organotin(lV) complexes with a potent antihypertensive agent, captopril[(2S)-l-[(2S)-2-methyl-3-sulfanyl propanoyl]pyrroli-dine-2-carboxylic acid cap], were carried toward the embryos of C. intestinalis. The main results obtained were as follows ... 

It is worthy of note that a-sulfanyl phosphonic acids, which can now be obtained enantioselectively from corresponding a-hydroxyphosphonates, are analogues of the a-sulfanyl carboxylic acids, which, for some of them, are metallo- -lactamases inhibitors [ 112]. To our knowledge, it does not seem that biological activities of a-sulfanyl phosphonic acids have been examined so far. 

On the analogy of the physicochemical relation, one was led to define a biological Hammett equation which related the equilibrium constant of the drug-receptor complex to the electronic a parameters of the substituents (e.g. chlorine, bromine, methyl, ethyl, hydroxyl, carboxyl, acetyl, etc.) of the drug molecule. Since the equilibrium constant of a drug-receptor complex is reflected by the biological activity, this led to the first extrathermodynamic relationship in QS AR ... 

Wong and co-workers have prepared various quaternary cx-nitro-cx-methyl carboxylic acid esters by the palladium-catalyzed allylic alkylation of a-nitropropionate ester (Eq. 5.59). The products can be kinetically resolved by using cx-chymotrypsin and are converted into optical active a-methyl cx-amino acids. Such amino acids are important due to the unique biological activity of these nonproteinogenic a-amino acids.82... 

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