Literature DB >> 3508538

N-Mannich-base prodrugs of 5-iodo-2'-deoxycytidine as topical delivery enhancers.

S A Koch1, K B Sloan.   

Abstract

Two Mannich-base prodrugs of 5-iodo-2'-deoxycytidine (5-IDC) have been synthesized. The prodrugs exhibit increased lipid solubility compared to 5-IDC and rapidly revert to 5-IDC in buffer. One of the prodrugs delivered about twice as much 5-IDC from isopropyl myristate (IPM) through hairless mouse skin in diffusion-cell experiments as did 5-IDC from IPM. Subsequent applications of theophylline/propylene glycol onto the diffusion cells to determine the effect of prodrug/IPM, 5-IDC/IPM, or IPM on the resistance of the skins to subsequent applications showed that the prodrug/IPM had no more effect than IPM itself.

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Year:  1987        PMID： 3508538     DOI： 10.1023/a:1016497204211

Source DB:  PubMed          Journal:  Pharm Res        ISSN： 0724-8741            Impact factor:   4.200


  10 in total

1.  Studies on the metabolism of 5-iodo-2'-deoxycytidine in vitro. Purification of nucleoside deaminase from mouse kidney.

Authors:  W A CREASEY
Journal:  J Biol Chem       Date:  1963-05       Impact factor: 5.157

2.  Selective inhibition of the replication of herpes simplex virus by 5-halogenated analogues of deoxycytidine.

Authors:  I Schildkraut; G M Cooper; S Greer
Journal:  Mol Pharmacol       Date:  1975-03       Impact factor: 4.436

3.  Use of solubility parameters of drug and vehicle to predict flux through skin.

Authors:  K B Sloan; S A Koch; K G Siver; F P Flowers
Journal:  J Invest Dermatol       Date:  1986-08       Impact factor: 8.551

4.  Reaction of cytidine with ethylating agents.

Authors:  L Sun; B Singer
Journal:  Biochemistry       Date:  1974-04-23       Impact factor: 3.162

5.  The cosmetic ingredient review--a safety evaluation program.

Authors:  R L Elder
Journal:  J Am Acad Dermatol       Date:  1984-12       Impact factor: 11.527

6.  Comparative efficacy of antiherpes drugs against different strains of herpes simplex virus.

Authors:  E De Clercq; J Descamps; G Verhelst; R T Walker; A S Jones; P F Torrence; D Shugar
Journal:  J Infect Dis       Date:  1980-05       Impact factor: 5.226

7.  Formaldehyde as a probe of DNA structure. I. Reaction with exocyclic amino groups of DNA bases.

Authors:  J D McGhee; P H von Hippel
Journal:  Biochemistry       Date:  1975-03-25       Impact factor: 3.162

8.  Formaldehyde as a probe of DNA structure. II. Reaction with endocyclic imino groups of DNA bases.

Authors:  J D McGhee; P H von Hippel
Journal:  Biochemistry       Date:  1975-03-25       Impact factor: 3.162

9.  Rational development of a soluble prodrug of a cytotoxic nucleoside: preparation and properties of arabinosyladenine 5'-formate.

Authors:  A J Repta; B J Rawson; R D Shaffer; K B Sloan; N Bodor; T Higuchi
Journal:  J Pharm Sci       Date:  1975-03       Impact factor: 3.534

10.  Prodrugs as drug delivery systems IV: N-Mannich bases as potential novel prodrugs for amides, ureides, amines, and other NH-acidic compounds.

Authors:  H Bundgaard; M Johansen
Journal:  J Pharm Sci       Date:  1980-01       Impact factor: 3.534
  10 in total

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