Rectal delivery of antiinflammatory drugs. IV. Effect of amino acids on the change in the rectal mucosa induced by diclofenac sodium.

1982 ◽  
Vol 30 (9) ◽  
pp. 3302-3309 ◽  
Author(s):  
HIDEYA YAGINUMA ◽  
YUTAKA KOHNO ◽  
SOICHI ITOH ◽  
KAZUYOSHI KUBO ◽  
MASARU YAMAZAKI ◽  
...  
Keyword(s):  
Amino Acids ◽  
Diclofenac Sodium ◽  
Rectal Mucosa ◽  
Antiinflammatory Drugs ◽  
Rectal Delivery

scholarly journals Directed Search of Anti-inflammatory Agents Among (3HQuinazoline- 4-ylidene)hydrazides of N-protected Amino acids and their Heterocyclization Products

2020 ◽  
Vol 19 (1) ◽  
pp. 61-73
Author(s):  
Yulya Martynenko ◽  
Oleksii Antypenko ◽  
Inna Nosulenko ◽  
Galina Berest ◽  
Sergii Kovalenko
Keyword(s):  
Amino Acids ◽  
Molecular Mechanisms ◽  
Diclofenac Sodium ◽  
Inflammatory Activity ◽  
Directed Search ◽  
Reference Drug ◽  
Aryl Amines ◽  
Anti Inflammatory ◽  
Sar Analysis ◽  
Cox 1

Background: (Quinazoline-4-ylidene)hydrazides are valued intermediates in modern organic chemistry, as they are commonly used for the synthesis of substituted [1,2,4]triazolo[1,5-c]quinazolines. Objective: Unknown N-acyl-2-([1,2,4]triazolo[1,5-c]quinazoline-2-yl)-alkyl-(alkaryl-, aryl-) amines were synthesized and evaluated for anti-inflammatory potential. Methods: The peculiarities of the synthesized compounds structures were studied by IR-, NMR spectroscopy and chromatography-mass spectrometry and were discussed in detail. Probable molecular mechanisms of activity (inhibition of COX-1 and COX-2) were predicted due to molecular docking. Anti-inflammatory activity of synthesized compounds was determined by their ability to reduce the formalin-induced paw edema in rats. Diclofenac sodium was used as reference drug. Results: In this study, the synthesis of N-acetyl-(benzoyl)-2-([1,2,4]triazolo[1,5-c]quinazolinе- 2-yl)alkyl-(aralkyl-, aryl-)amines, using (3H-quinazoline-4-ylidene)hydrazides of Nprotected amino acids or 4-hydrazinoquinazoline and N-prorotected amino acids as starting compounds was developed. It was established that the reaction of (3H-quinazoline-4- ylidene)hydrazides of Boc-amino acids occurred with the formation of N-acetyl-substituted triazoloquinazolines. High anti-inflammatory activity was detected for unknown (3Hquinazoline- 4-ylidene)hydrazides Boc-amino acids (1.13-1.15) and N-acetyl-(benzoyl)-2- ([1,2,4]triazolo[1,5-c]quinazoline-2-yl-)aralkyl-(aryl-)amines (3.2, 3.3, 3.11, 3.12), using the experimental formalin test. Conclusion: The conducted SAR-analysis allowed to detect critical fragments. Namely, the Boc-aminoaralkyl-(aryl-)acid residue in (3H-quinazoline-4-ylidene)hydrazides (1.13- 1.15), benzyl and phenyl linker groups in N-acetyl-(benzoyl)-2-([1,2,4]triazolo[1,5- c]quinazoline-2-yl-)aralkyl-(aryl-) amines (3.2, 3.3, 3.11, 3.12) are believed to be substantial for anti-inflammatory activity.

scholarly journals Rectal delivery of antiinflammatory drugs. I. The influence of antiinflammatory drugs on rectal absorption of .BETA.-lactam antibiotics.

1981 ◽  
Vol 29 (10) ◽  
pp. 2974-2982 ◽  
Author(s):  
HIDEYA YAGINUMA ◽  
TOHRU NAKATA ◽  
HARUMASA TOYA ◽  
TERUO MURAKAMI ◽  
MASARU YAMAZAKI ◽  
...  
Keyword(s):  
Beta Lactam ◽  
Rectal Absorption ◽  
Antiinflammatory Drugs ◽  
Beta Lactam Antibiotics ◽  
Rectal Delivery

scholarly journals Evaluation of the Anti-Inflammatory Activities of Diclofenac Sodium, Prednisolone and Atorvastatin in Combination with Ascorbic Acid

2020 ◽  
Vol 19 (3) ◽  
pp. 291-301 ◽  
Author(s):  
Tanvir Ahmed ◽  
Sabrina Rahman Archie ◽  
Asef Faruk ◽  
Fabliha Ahmed Chowdhury ◽  
Abdullah Al Shoyaib ◽  
...  
Keyword(s):  
Ascorbic Acid ◽  
Defense Mechanism ◽  
Diclofenac Sodium ◽  
Antiinflammatory Drugs ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Inflammation Group ◽  
Neuropsychiatric Effect ◽  
Normal Defense

Objectives: Inflammation is our body’s normal defense mechanism, but in some cases, it may be responsible for causing different kinds of disorders. Several antiinflammatory drugs are present for the treatment of these disorders; however, the conventional anti-inflammatory drugs cause side effects when used in the long term and therefore, it is better to use them in a low dose for a shorter duration of time. This study was designed to find out whether there is an augmentation of the therapeutic effectiveness of the antiinflammatory drugs like diclofenac sodium (NSAID), prednisolone (steroid) and atorvastatin (statin) when used in combination with ascorbic acid (antioxidant). Methods: Wistar Rats (n=144) were selected and divided into 24 groups of 6 rats in each. Carrageenan and formalin were used to induce local inflammation and neuropsychiatric effects, respectively. The inhibitions of such responses were measured after administering a drug alone and in combination with ascorbic acid. Results: In case of carrageenan mediated inflammation, the combination of 5 mg/kg diclofenac and 200 mg/kg ascorbic acid gave the highest inhibition of 74.19% compared to other groups of drugs. The combination of 5 mg/kg diclofenac and 200 mg/kg ascorbic acid gave 97.25% inhibition for formalin-mediated inflammation group. In both cases, combination therapy showed statistically significant anti-inflammatory activities compared to monotherapy (p values <0.05). Conclusion: All the data clearly indicate new combinations of drug therapy comprising diclofenac sodium, prednisolone, atorvastatin with ascorbic acid, which may be more effective against both local edema and the neuropsychiatric effect caused due to inflammation.

scholarly journals Rectal delivery of antiinflammatory drugs. III. Effect of basic amino acid salts of diclofenac on the rectal absorption of ampicillin sodium.

1982 ◽  
Vol 30 (3) ◽  
pp. 1073-1076 ◽  
Author(s):  
HIDEYA YAGINUMA ◽  
YOSHIKO ISODA ◽  
YASUSHI WADA ◽  
SOICHI ITOH ◽  
MASARU YAMAZAKI ◽  
...  
Keyword(s):  
Amino Acid ◽  
Basic Amino Acid ◽  
Rectal Absorption ◽  
Antiinflammatory Drugs ◽  
Ampicillin Sodium ◽  
Amino Acid Salts ◽  
Rectal Delivery ◽  
Acid Salts

Influence of Antiinflammatory Drugs (Methylprednisolone and Diclofenac Sodium) on Experimental Pleurodesis Induced by Silver Nitrate or Talc

CHEST Journal ◽  
2005 ◽  
Vol 128 (6) ◽  
pp. 4041-4045 ◽  
Author(s):  
Lisete R. Teixeira ◽  
Francisco S. Vargas ◽  
Milena M.P. Acencio ◽  
Pedro F.S. Paz ◽  
Leila Antonangelo ◽  
...  
Keyword(s):  
Silver Nitrate ◽  
Diclofenac Sodium ◽  
Antiinflammatory Drugs

Physicochemical Characterization of Diclofenac Sodium-Loaded Poloxamer Gel as a Rectal Delivery System with Fast Absorption

2003 ◽  
Vol 29 (5) ◽  
pp. 545-553 ◽  
Author(s):  
Chul Soon Yong ◽  
Hongkee Sah ◽  
Yurngdong Jahng ◽  
Hyeun Wook Chang ◽  
Jong-Keun Son ◽  
...  
Keyword(s):  
Delivery System ◽  
Diclofenac Sodium ◽  
Physicochemical Characterization ◽  
Fast Absorption ◽  
Rectal Delivery ◽  
Poloxamer Gel

scholarly journals Effect of Topical Antiinflammatory Drugs on Mechanical Behavior of Rabbit Cornea

2017 ◽  
Vol 15 (2) ◽  
pp. 142-148 ◽  
Author(s):  
Domenico Lepore ◽  
Roberto De Santis ◽  
Monica M. Pagliara ◽  
Antonio Gloria ◽  
Olimpia Oliviero ◽  
...  
Keyword(s):  
Wound Healing ◽  
Early Stage ◽  
Diclofenac Sodium ◽  
Healing Process ◽  
Tensile Modulus ◽  
Biomechanical Properties ◽  
Nonsteroidal Antiinflammatory Drugs ◽  
Full Thickness ◽  
Antiinflammatory Drugs ◽  
Rabbit Cornea

Background A variety of antiinflammatory therapies are employed to promote corneal wound healing. The effects of steroidal and nonsteroidal antiinflammatory drugs on the biomechanical properties of rabbit cornea were investigated over time using tensile tests. Methods Full-thickness incisions were made and used to analyze the effects of dexamethasone sodium phosphate 0.1% and diclofenac sodium 0.1% on corneal biomechanical properties during wound healing at 7, 14 and 21 days after surgery. Results The full-thickness incision deeply modified all of the mechanical properties. At 3 weeks after incision, regardless of the drug therapy, the tensile modulus was about 70% of the value for the intact cornea. Conclusions Topical treatment with dexamethasone was particularly effective during the first week after surgery; the second week after surgery, a similar result was observed in the corneas treated with diclofenac. Low doses of steroidal and nonsteroidal antiinflammatory drugs would seem to have the potential to improve biomechanical properties only during the early stage of the healing process of the cornea.

scholarly journals Rectal delivery of antiinflammatory drugs. II. The influence of basic amino acid salts on rectal absorption of diclofenac.

1981 ◽  
Vol 29 (11) ◽  
pp. 3326-3333 ◽  
Author(s):  
HIDEYA YAGINUMA ◽  
TOHRU NAKATA ◽  
HARUMASA TOYA ◽  
TERUO MURAKAMI ◽  
MASARU YAMAZAKI ◽  
...  
Keyword(s):  
Amino Acid ◽  
Basic Amino Acid ◽  
Rectal Absorption ◽  
Antiinflammatory Drugs ◽  
Amino Acid Salts ◽  
Rectal Delivery ◽  
Acid Salts

Homochirality as the Signature of Extra-Terrestrial Life

1997 ◽  
Vol 161 ◽  
pp. 505-510
Author(s):  
Alexandra J. MacDermott ◽  
Laurence D. Barron ◽  
Andrè Brack ◽  
Thomas Buhse ◽  
John R. Cronin ◽  
...  
Keyword(s):  
Amino Acids ◽  
Protein Synthesis ◽  
Optical Rotation ◽  
Physical Origin ◽  
Natural Choice ◽  
Rosetta Mission ◽  
Terrestrial Life ◽  
Subsurface Layers ◽  
Solar System Bodies ◽  
Origin Of Homochirality

AbstractThe most characteristic hallmark of life is its homochirality: all biomolecules are usually of one hand, e.g. on Earth life uses only L-amino acids for protein synthesis and not their D mirror images. We therefore suggest that a search for extra-terrestrial life can be approached as a Search for Extra- Terrestrial Homochirality (SETH). The natural choice for a SETH instrument is optical rotation, and we describe a novel miniaturized space polarimeter, called the SETH Cigar, which could be used to detect optical rotation as the homochiral signature of life on other planets. Moving parts are avoided by replacing the normal rotating polarizer by multiple fixed polarizers at different angles as in the eye of the bee. We believe that homochirality may be found in the subsurface layers on Mars as a relic of extinct life, and on other solar system bodies as a sign of advanced pre-biotic chemistry. We discuss the chiral GC-MS planned for the Roland lander of the Rosetta mission to a comet and conclude with theories of the physical origin of homochirality.

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