Novel substituted nicotinamide derivatives: synthesis and evaluation for antihypertensive activity

The synthesis of 2 novel series of nicotinamide derivatives VI and IX has been carried out. 3-[carboxyphenylaminocarbonyl] pyridine [III] was converted to its acid chloride IV which was reacted with different alicyclic and /or aromatic secondary amines to give the first series of nicotinamide derivative IX in a quantitative yield. The sodium salt of III was also reacted with different N-chloroacetyl derivatives of alicyclic and /or aromatic secondary amines giving the second series of nicotinyl derivatives VI. Compounds VI and IX were converted to their methyl iodide salts VII and X, respectively, which were reduced with sodium borohydride to yield 1,2,3,6-tetrahydropyridine derivatives VIII and XI, respectively. The structure of new products was substantiated by spectral as well as microanalytical data. Eight of the new synthesized compounds were tested for hypotensive activity in anesthetized normotensive rabbits

Synthesis of novel furan containing DNA minor groove binding oligopeptides related to netropsin for pharmaceutical interest

Certain oligopeptides, structurally related to the antiviral antitumor antibiotic netropsin, have been synthesized. The pyrrole units have been replaced by a furan or difuran moiety. One of the amidines moieties of netropsin has been replaced by certain alicyclic and /or aromatic secondary amines to examine the effect of such structural modification on the antitumor activity of oligopeptides. Eight new compounds were tested for in-vitro cytotoxic activity against Ehrlich ascites carcinoma

Synthesis of 9-thioureido, cyanoguanidino and nitroethenylamine derivatives of acridines as potential Antimicrobial agents

Three series of substituted arcading derivatives, III, IV and VIII were prepared for potential antimicrobial activity. Compounds IIIa-d as the first series were prepared through the reaction of 9-aminoacridine [I] with different alkylisothiocyanates. They were treated with lead cyanamide to give compounds IVa-d of the second series. The reaction of compounds VI with different primary and secondary amines gave compounds VIIIe-I of the third series. The structure of the novel products was substantiated by spectral and microanalytical data. The stereochemistry of the compounds of the third series was studied using nuclear over-hauser enhancement NOE difference. Eight new compounds were in vitro tested for antimicrobial activity

Synthesis of 3-chloro-7-methoxy-9-substituted acridine derivatives as pot entail Antimicrobial agents

Three series of 3-chloro-7-methoxy-9-substituted acridine derivatives II-IV were prepared for potential antimicrobial activity. The first series, compounds IIa-i, was prepared via the reaction of I with different aromatic amines. The second, compounds IIIa-i, were obtained by the treatment of I with different phenolic compounds; while the third series, compounds IVa-c, involved reaction of I with different heterocyclic thiols viz. benzothiazole-2-thiol, benzimidazole-2-thiol and uracil-2-thiol. The structure of the novel products was substantiated by spectral and microanalytical data. Nine new compounds were tested for in vitro antimicrobial activity

Synthesis of n-acyl- and n-aroylamino-1,2,3,6-tetrahydro 4-substituted pyridines

Reaction of N-amino-4-substituted pyridinium iodide I with the acid chlorides II afforded the ylides III in high yields. Their reduction with sodium borohydride in absolute ethanol at ice-bath temperature was found to be more favorable than in 95% ethanol to give higher yields of the title N-carbonylamino-1,2,3,6-tetrahydropyridines IV. The chemical constitution of the products was proved by spectral as well as elemental analyses