Design and synthesis of new imidazole derivatives of captopril

A new series of alkylthio imidazole analogues of captopril, an ACE inhibitor used in the treatment of hypertension, was designed and synthesized in order to obtain agents more active than captopril with less side effects. All the compounds thus prepared were purified and characterized by IR, NMR and Mass analytical instruments

Fused pyrimidines synthesis and anti-inflammatory testing of certainnovel imidazo [1,2-c] quinazoline, pyrimido [2,1-a] phthalazine derivatives

A number of heterocyclic compounds containing pyrimidine nucleus, namely, imidazo[l,2-c]quinazolines, pyrazolo[3,4-d]triazoIo[3.4-b]pyrimidines and pyrimido[2,1-a] phthalazines has been synthesized. Acidic moieties that characterize most of nonsteroidal antiinflammatory drugs [NSAIDs] or ester groups, as potential pro-drug functionaIities, have been incorporated. The potency of eight compounds to inhibit carrageenin-induced paw edema in rats has been evaluated

Synthesis and alpha-adrenergic activities of 2-and 4-substituted imidazoline and imidazole analogs of -and B-naphthalene

Seven analogs of medetomidine and naphazoline were synthesized and evaluated for their alpha 1- [aorta] and alpha 2- [platelet] activities. The analogs were composed of 2- and 4-substituted imidazoles and imidazolines attached through a methylene bridge to either an alpha- or beta-naphthalene ring system. In general, the alpha-naphthalene analogs were found to be the most potent inhibitors of platelet aggregation. The fact that the alpha-naphthalene analogs [2, 5, 6, and 7] were partial agonists, while the beta-naphthalene analogs [3, 8, 9] were antagonists in alpha 1-adrenergic system [aorta] was reported. Thus, appropriately substituted naphthalene analogs of medetomidine and naphazoline provided a broad spectrum of alpha 1-[agonist and antagonist] activity and alpha 2-antagonist activities

Synthesis of some new imidazolinones of expected antimicrobial activity

The action of hydrazine on 5-cinnamylidene-2-ethylthio-3-phenylhydantoin [Ic] gave 1-amino-2-anilino-4-cinnamylidine- delta[2] imidazolin-5-one [II]. The latter was deaminated with nitrous acid to yield 2-amino-4-cinnamylidene- delta[2]-imidazolin-5-one [IVa] which was also obtained from Ic by the action of ammonium acetate or Ia by the action of aniline. Compound II was condensed with aromatic aldehydes to give the corresponding Schiff's bases VIa-f. A number of 2-substituted aminoimidazolinones IVb-j and VIIIa-d were also prepared. Some of the obtained compounds showed antimicrobial activity