Analele UniversităŃii din Bucureti – Chimie (serie nouă), vol 19 no. 2, pag. 09 – 21
© Analele UniversităŃii din Bucureti
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(&!)* A novel series of 3%(2%amino%6%pyrimidin%4%yl)%6%bromo%2H%chromen%2%one (+,+-)
were synthesized from 3%acetyl%6%bromo%2H%chromen%2%one (.). The structures of the
synthesized compounds were elucidated by IR,
1
H%NMR,
13
C%NMR, and mass spectroscopic
techniques. The synthesized compounds were screened for in%vivo analgesic activity at a dose of
20 mg/kg body weight. Among them, compounds +, +( and +$ exhibited significant analgesic
activity and compounds +/ and +- exhibited highly significant activity comparable with standard
drug Diclofenac sodium using Acetic acid induced writhing model. Compounds +, +/ and +-
were further evaluated for acute%ulcerogenesis activity. Among them, compound +- was found to
be most promising analgesic agent devoid of ulcerogenic effects.
0$’ 12!#&* Coumarin; Pyrimidines; Knoevenagel reaction; Claisen%schmidt condensation;
Writhing Test; Analgesic activity; Ulcerogenic activity.
received: September 9, 2010 accepted: October 7, 2010
%!2#)/2%
The investigation of compounds able to treat both acute and chronic pain is challenging in
pharmaceutical research [1], pain is in fact a very important problem present in 90% of
diseases, from the simple back pain to pain associated with different forms of cancer. The
classical therapies for pain treatment are mainly the non%steroidal%anti%inflammatory drugs
(NSAIDs) and opiates, whose lead compounds, acetylsalicylic acid and morphine,
respectively, were isolated in 19th century [2].
NSAIDs show side effects such as gastrointestinal irritation and lesions, renal toxicity and
inhibition of platelet aggregation, while the use of opioids is limited to severe pain because
of adverse secondary reactions as respiratory depression, dependence, sedation, and
Department of Pharmaceutical Technology, Meerut Institute of Engineering & Technology, NH%58, Baghpat
Bypass Crossing, Meerut (U. P.) India.%250005. corresponding author email: rdudhe121@rediffmail.com,
jitendraeishwer@yahoo.co.in, jitendraeishwer@gmail.com
Uttarakhand Technical University, Dehradun (Uttarakhand), Pin – 248007.
NIMS University, Shobha Nagar, Jaipur (Rajasthan), India%303001.
M.D.University, Rohtak, Haryana. India.
Department of Physical Chemistry
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