Original drugs created in the Center for Drug
Chemistry
The list of the original drugs includes highly effective neurothropic,
cardiovascular, antihystaminic (antiallergic), antibacterial, antiviral,
antitumor and other preparations.
Neurotropic drugs include:
-
For the first time, there has been created at the Institute, family of
tetracyclic antidepressants with a new mechanism of action - the reversible
monoaminooxydase (MAO) inhibitors. This family represents a new heterocyclic
system - derivatives of pyrazino-carbazole and pyrazino-carboline and contains
such drugs as pirlindole, metralindole and tetrindole;
-
Tricyclic antidepressant from a new chemical class (a derivative of 3,4-diazaphenoxazine)
- pipofezine, combines an anti-depressive effect with a sedative
activity and is deprived of anticholinergic properties.
-
Peripheral and central anticholinergic and cholinomimetic drugs, including
anticholinergic alkaloid platyphylline, synthetic anticholinergics
metacine
and aprofene; highly effective bronchodilatator drug troventol
(truvent); central anticholinergic and antiparkinsonic drug tropacine
(dipheniltropin hydrochloride); ganglioblocker dimecoline, cholinomimetic
drug aceclidine, anticholineesterase alkaloid galanthamine
(attracting now attention as a drug for treatment of Alzheimer's disease)
etc.
-
Psychostimulators mesocard and feprosidine.
-
Miorelaxants diplacine and qualidile;
-
Synthetic analgesics trimeperidine and dimenoxadole.
Original cardiovascular drugs include:
-
Class III antiarrhythmic drug nibentane,
created as a result of extensive studies of a large group of derivatives
of diaminoalkanes;
-
new by its structure and action, the hybrid alpha- and beta-blocker proxodolole,
having high antihypertensive antiischemic and antiglaucomal activity;
-
highly effective alpha-blocker tropodifene;
-
antihypertensive and sedative drug benzochlidene.
Original H1-antihystaminic preparations include quibenadine
and sequifenadine. Both of these have high antiallergic activity
and are deprived of the central depressive (sedative) effect. These drugs,
as well as the cholinomimetic aceclidine and antihypertensive drug
benzalidine,
were created in the Institute as a result of synthesis and study of a large
group of quinoclidine derivatives.
The results of a search for a new antibacterial preparations
were:
-
Creation of a new group of antibacterial drugs - derivatives of quinoxaline
chinoxydine
and dioxydine, which are highly effective against gram positive
and gram negative aerobic bacteria. They are also effective against micobacteria
tuberculosis according to the latest studies.
-
Creation of original combined sulphanilamide drug sulfatone, similar
by its efficiency with co-trimexazole.
-
Creation of a number antituberculesis drugs, hydrazine derivatives of isonicotinic
acid: ftivazid, saluside, saluside soluble,
methazid
etc.
Among the original antiviral drugs created at the Institute is the
large group of synthetic compounds, effective against herpes, influenza
and acute respiratory diseases: oxoline, bonaphtone, florenale
and some others. Another drug created in the Institute that is highly effective
against influenza and other infections is arbidol,
which has immunomodulatory interferoneinductive and antioxydative properties.
The Institute launched a number of antitumor drugs, including
original derivatives of a dispirotripiperasinium (prospidin, spirobromine
etc) and ethylenimine (dipin, pumitepa and fotretamine).
Several other preparations important for medical practice were also
created at the Institute: emoxipinum - antihypoxante and
antioxydante,
mexamine
- radioprotective drug, leukogene - leukopoese stimulator
etc.
Search for new drugs in various classes of organic compounds is now
in progress at the Center for Drug Chemistry. Thus, the Institute is carrying
out a search for:
-
class III antiarrhythmics;
-
antibacterial compounds among the quinolonecarboxylic acid derivatives;
-
substances with antiviral and immunomodulatory activity among analogues
of arbidole;
-
antituberculesis drugs with new mechanism of action;
-
antifungal drugs.
A number of potential drugs from these groups of compounds are at different
stages of the pre-clinical and clinical studies.