Novel coumarins of potential adrenergic antagonistic activity

A series of 1-[8-methyl-4-phenyl-coumarin-7-yloxy]-3-[substituted amino] propan-2-ol [10-18], 1-[substituted coumarinyloxy]-3-[substituted-amino] propane [19-35], and 6 or 7 [[3.t.butyl-5-oxazolidinyl] methoxy substituted coumarins [36-39] were prepared to study the effect of change of structure on the beta- adrenergic antagonistic activity. The preliminary pharmacological tests were carried out, the results were given and a conclusion was drawn

Synthesis of some parabanic acid and thiazoline derivatives coumarines with expected pharmacological activity part II

New parabanic acids and thiazolines derived from different coumarinyloxyacetic acid hydrazides have been prepared and subjected to preliminary pharmacological screening. Some of the tested compounds showed anticonvulsant activity

New furobenzopyrone analogues as photochemotherapeutic agents

The present work described the synthesis and investigation of some new linear and angular furobenzo-alpha-pyrone analogues as photochemotherapeutic agents with the aim of producing compounds with high activity and reduced toxicity. Besides, 3 D-models have been simulated to study the effect of peripheral substituents on the photosensitizing activity of the new furobenzo-alpha-pyrone

New furobensopyrones as possible agents for the photochemotherapy of psoriasis with expected monofunctional mode for DNA

This work involved the synthesis of linear furobenzopyrone analogs as monofunctional photochemotherapeutic agents, aiming to obtain compounds with increased activity and reduced toxicity. A rough investigation was carried out on the conformation of a new bulky substituent like phenyl group in the furobenzopyrone system to produce compounds that could react with DNA in a monofunctional sense, therefore reducing or eliminating skin phototoxicity or the risk of skin cancer and, at the same time, maintaining the same selectivity of action as psoralen, [linear furobenzopyrone]. So, they have synthesized linear furobenzopyrone derivatives [3a-c and 8a1-6], in which methyl and phenyl groups were systematically varied at the 2, 3, 5, and 9 positions. Preliminary screening for the photosensitizing activity of some of the new analogs have revealed that compound [8a1] is more active as photosensitizer than xanthotoxin [reference], while 3b, c and 8a4-6 are less active. In addition, 3a and 8a2-3 showed no photosensitizing activity

Synthesis of trioxo-perhydro-imidazolyl benzopyrones with hypnotic activity

5 amino-6-hydroxy-4, 7-dimethyl-2H-1-benzopyran-2-one II and 6-amino-7-hydroxy-4,8-dimethyl-2H-1-benzopyran-2-one-VI add substituted isocyanates to give the N, N-di-substituted ureas III and VII than can be cyclized by the use of oxallyl chloride to the corresponding imidazolyl-2,4,5-triones IV and VIII, respectively. Some of the synthesized compounds have been screened for CNS depressant and hypnotic activities. The administration of some of these products at a dose of 20 mg/kg b. wt. showed CNS depressed activity, but in a dose of 40 mg/kg b. wt. exhibited hypnotic effect. The antimicrobial evaluation of certain novel compounds is also done, and it was found that some derivatives inhibit the growth of Salmonella typhi and Escherichia coli

Synthesis of some 1,3,4-oxadizolines and thiazolidinones of expected anti-bacterial activity

Reaction of the acid hydrazide [3] with different carbonyl compounds gave the corresponding hydrazones [4]. The oxadiazolines [5] were obtained by refluxing [4] with acetic anhydride. The thiazolidinones [6] were achieved by the cyclocondensation of [4] with mercaptoacetic acid. The antimicrobial activity was determined for eight representative compounds and some of them were active

Synthesis and biological activity some new thiadiazolo, triazolo and fused s-triazolo [3,4-b] -1,3,4-thiadiazolo-coumarins

In this study, some new thiadiazolo triazolo and fused s-triazolo [3,4-b]-1,3,4-thiadiazolo-coumarins were prepared from [4,8-dimethyl- 7-coumarinyloxy] acetic acid hydrazide via different intermediates, and evaluated for their pharmacological activities. Some of the tested compounds exhibited CNS depressant activity in the experimental animals

Synthesis of certain novel coumarins as possible CNS active agents

A number of new compounds derived from 4-methyl-6-hydroxycoumarin were synthesized and evaluated for their pharmacological activity. Some of the tested compounds exhibited CNS depressant and hypotensive action in the experimental animals

Synthesis and biological activity of some new coumarins

The synthesis of a series of 6, and 7-aryloxyalkyloxycoumarins and a new class of 1-[4-methylcoumarin-6-yloxy]-3-[substituted amino] program-2-ol, is described. Some of these compounds were evaluated for their antihistaminic activity and were found to be active

Synthesis and hypotensive activity of certain benzofuran derivatives

Some 6-hydroxy -4- methoxy -7- morpholinomethylbenzofuran derivatives with various 5- cinnamoyl or heterocyclic substituents have been prepared. The hypotensive activity of some of the synthesized compounds was evaluated