Chapter 7. Pulmonary and Antiallergy Drugs

Devlin, John P.

doi:10.1016/s0065-7743(08)61274-9

Annual Reports in Medicinal Chemistry

1981

DOI: 10.1016/s0065-7743(08)61274-9

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Chapter 7. Pulmonary and Antiallergy Drugs

John P. Devlin¹

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Cited by 2 publications

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“…DSCG, however, suffers from the fact that it is not orally absorbed but must be administered as a finely powdered aerosol.1 As a result, the focus of attention for more than a decade has been on the development of more potent, orally active DSCG-like compounds. 2,3 In 1975, it was reported2 34 that a number of oxanilates and jV-heteroaryloxamates were active in the rat passive cutaneous anaphylaxis (PCA) assay. More recently, iV, -) J. S. G. Cox, J. E. Beach, A. .…”

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confidence: 99%

N-(4-Substituted-thiazolyl)oxamic acid derivatives, new series of potent, orally active antiallergy agents

Hargrave¹,

Hess²,

Oliver³

1983

J. Med. Chem.

296

119

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A series of N-(4-substituted-thiazolyl)oxamic acid derivatives were synthesized and tested for antiallergy activity in the rat PCA model. These compounds were conveniently prepared by treatment of the appropriate acetophenone with thiourea and iodine or by reaction of the chloroacetylbenzene with thiourea to give the corresponding aminothiazoles; subsequent condensation with ethyloxalyl chloride gave the thiazolyloxamates. Many of the analogues showed a 50% inhibition at less than 2 mg/kg po or less than 0.4 mg/kg iv and were significantly more potent than disodium cromoglycate, which in the rat PCA model is orally inactive and gives a 50% inhibition at 1.2 mg/kg iv. Hydrolysis of the oxamates generally resulted in enhanced activities, while substitution of the phenyl ring with a variety of substituents (e.g., 4-F, 4-OEt, and 4-NHCOCH3) did not significantly enhance the activity of the unsubstituted phenyl derivative. One of the ethanolamine salts, N-[4-(1,4-benzodioxan-6-yl)-2-thiazolyl]oxamic acid ethanolamine salt (61, PRH-836-EA), has been selected for further pharmacological evaluation.

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mentioning

confidence: 99%

N-(4-Substituted-thiazolyl)oxamic acid derivatives, new series of potent, orally active antiallergy agents

Hargrave¹,

Hess²,

Oliver³

1983

J. Med. Chem.

296

119

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Synthesis of heterocyclic analogs of isoflavone and homoisoflavone based on 3-formylchromone

et al. 2021

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The review is focused on recent developments of chemistry of synthetic analogs of natural compounds, isofl avone and homoisofl avone. The possible synthetic strategies to access heterocyclic analogs of these compounds starting from readily available 3-formylchromone and its derivatives (3-cyanochromone, 2-amino-3-formylchromone) and products of its condensation with simplest Cand N-nucleophiles are discussed. The structural features of the reaction products that depend on the nature of the reaction medium, structure of the starting compounds, and reagent ratio are considered. Particular attention is given to the application of the modern strategies of organic synthesis, namely green chemistry approaches, click reactions, domino reactions, etc. Examples of compounds of this group most promising for clinical application due to wide and pronounced pharmacological eff ects are given.

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Chapter 7. Pulmonary and Antiallergy Drugs

Cited by 2 publications

References 69 publications

N-(4-Substituted-thiazolyl)oxamic acid derivatives, new series of potent, orally active antiallergy agents

N-(4-Substituted-thiazolyl)oxamic acid derivatives, new series of potent, orally active antiallergy agents

Synthesis of heterocyclic analogs of isoflavone and homoisoflavone based on 3-formylchromone

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