Analogs and Derivatives

Until recently, advances in insulin formulation were limited to improvements in insulin purity, insulin species, and adjustment of the vehicle composition. With the advent of recombinant DNA techniques, it has been 

More recently, manipulation of the structure of the B-chain, aiming at decreasing the potential for P-sheet interactions of the peptide backbone between insulin monomers, has also resulted in insulins with decreased tendency to self-associate. Examples of such analogs are the LysPro insulin (Brems et al, 1992), in which the B28 and B29 residues are interchanged, as is the case in insulin-like growth factor-I, and analogs characterized by deletion of one of the amino acid residues in the B25 B28 sequence (Balschmidt and Brange, 1992). 

Controlled parenteral delivery of proteins has recently been reviewed by Pitt (1950) and Heller (1993a,b). Developments in insulin delivery systems have been reviewed by Saudek (1993), devices for insulin administration by Selam and Charles (1990), and subcutaneous insulin therapy by Houtzagers (1989), Home and Alberti (1992), Koivisto (1993), and Heine (1993). 

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White, E. H., and Roswell, D. F. (1991). Analogs and derivatives of firefly oxyluciferin, the light emitter in firefly bioluminescence. Photochem. Photobiol. 53 131—136. 

Coincidental with the above developments, biomedical scientists in pharmaceutical companies were actively pursuing purified extracts and pure compounds derived from plants and animal sources (e.g., digitalis, rauwolfia alkaloids, and animal hormones) as human medicaments. Analogs and derivatives of these purified substances were also investigated... 

Carboranes, 18 2, see also specific types analogs and derivatives, 18 97-132 BH group-substituted, 18 78 CNPR theory, 18 125-127 bond distances in, 18 46 bonding in, 18 7-16 bridge hydrogen, 18 90-93... 

Non-aromatic Hydrocarbons, Heterocyclic Analogs and Derivatives , A. F. Cameron, in Molecular Structure by Diffraction Methods , ed. G. A. Sim and L. E. Sutton, Royal Society of Chemistry, London, 1975, vol. 3, pp. 128-162. 

A strict substantiation for this analogy and derivation of this relationship in terms of the Mason rule [5] can be found in refs. 6 and 7. In our monograph [7] we also give proofs for the fact that the terms of eqn. (11) obtained using the Kramer rule are spanning tree weights of various nodes. A brief substantiation for eqn. (11) will be given below. 

Implications for the Synthesis of Cucurbit[n]uril Analogs and Derivatives... 

The aromatic, tetramethoxy-substituted, tetrahydroisoquinoline alkaloid weberine has been isolated recently from extracts of the Mexican cactus Pachycereus weberi (38). The rare occurrence of four adjacent methoxy groups on an aryl moiety prompted the synthesis and examination by crystal-structure analyses of analogs and derivatives with four and five adjacent methoxy groups on the phenyl ring. In contrast to the problem with... 

This chapter does not cover cyclic amides and peptides, since their number would enormously expand this text. They are reviewed only if they serve as reaction intermediates during synthesis of cyclic amines. In addition, metal ions complexation will be presented in required minimum, for example, if it serves for template formation during ring synthesis or as a main topic in some application. In this chapter, most of the sections deal with the literature data for all cycle types, except Section 14.11.6, which focuses mainly on chemistry of cyclen and cyclam and their analogs and derivatives. In Section 14.11.8, we give only a brief overview of the utilizations and provide a reader with reviews where more detailed information may be found. 

Essentially every analog and derivative prepared in the project was ultimately derived from the corresponding 3-chloro-pyri-dazine. With the exception of a few 3-chloropyridazines which originated from a Friedel-Crafts acylation of benzene, the large majority of chloropyridazines were prepared by a sequence based on the addition of the masked acyl anion equivalent of a benzaldehyde to the appropriately substituted acrylate ester. 

Continued development of peptide, pep-toid, and PNA analogs and derivatives that cross membrane barriers, target intercellular receptor/acceptors, and enhance bioavailability. 

Finally, application of a particular biofunctional molecule in agriculture and other bioindustries or health care and medicine is the practical goal of the research. Chemists will synthesize many analogs and derivatives, and biologists will evaluate their biological effects. If one can find a useful compound, it will be commercialized for practical application. For example, gibberellin A3 (1) is used in Japan to produce seedless grapes. 

There are other curious binding similarities and differences between the pyridyl ethers or AXP analogs and derivatives of nicotine. For example, substitution at the pyridine 2-position typically decreases the affinity of nico-... 

Speaking of side effects, folic acid and its analogs and derivatives inhibit other enzymes. These other enzymes are listed in Jain s handbook (1982), and the fisting includes thymidylate synthetase or synthase, as well as dihydrofolate reductase, the enzymes blocked by antifolates, as previously indicated.)... 

Since Cgo (Buckminster Fullerene) was discovered in 1985 [1535], the IR and Raman spectra of Ceo and a large number of its analogs and derivatives (fullerenes) have been studied extensively. Among them, Cgo has attracted considerable attention because of... 

Because of the marked biological activity of this group of antibiotic substances, a great number of analogs and derivatives—differing in both the sugar and purine or pyrimidine portions—have been synthesized, but it is beyond the scope of this review to discuss these. 

Scheme 1. TADDOLs, Analogs, and Derivatives Thereof Constructed from +)- or (-)-Tar-trate. Aldehydes or Ketones, and a Grignard Reagent (shown here is the structure derived from (+)-(i ,i )-tartrate). Instead of tartrate acetals (R = H) or ketals (R, R H) [12], other chiral nonracemic dicarboxylates may be employed in the Grignard reaction [13] [14], Aryl = Ph can be hydrogenated to CgHn [15] [16], and the diastereoisomeric derivatives with geminal Ph/Me instead of Aryl/Aryl groups are available through the 4,5-dibenzoyl-dioxolane [14], For examples, for OH derivatizations, and for OH/Y and OH/Z substitutions, see Schemes 2 and 3.

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