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• W2888016871 abstract "Fast and effective relief of pain and inflammation in the human being is continued to bea major challenge for the medicinal chemistry researchers. Non-steroidal anti-inflammatorydrugs (NSAIDs) are important therapeutic agents for the alleviation of pain and inflammationassociated with a number of pathological conditions. However, chronic administration ofNSAIDs has been associated with clinically significant complications such as gastrointestinal(GI) symptoms including mucosal damage, bleeding, nausea, heartburn, dyspepsia,abdominal pain and renal toxicity.Co-administration of multiple drugs for treatment of inflammatory conditionsassociated with microbial infection is a major risk especially in patients with prior history ofpeptic ulcer disease, patients with impaired liver or kidney functions and patients takinganticoagulants, corticosteroids, etc. concurrently. A mono therapy of a drug with dualantimicrobial and anti-inflammatory activity would be preferred from the pharmacoeconomicand patient compliance point of view. In view of the above-mentioned facts some novel 2-mercaptobenzothiazoles carrying 1,3,4-oxadiazole (ODZ1-15 and OXZ1-13), acetohydrazide(ACH1-5), 1,3,4-thiadiazole (TDZ1-13), 1,3,4-triazole (TRZ1-13) and 2-pyrazoline (PYZ1-19and PYS1-9) moieties at the second position were synthesized. This combination wassuggested in an attempt to develop hybrid compounds that would act as antimicrobial andanalgesic-anti-inflammatory agents with minimal gastrointestinal (GI) side effects.The synthesized compounds were evaluated for their in vitro antimicrobial activity bythe cup plate method. The tested compounds ODZ1-4, ODZ6, ODZ10, ODZ11 and ODZ13showed significant inhibitory activity (inhibition zone 24-32 mm) against all the testedbacterial strains whereas compounds OXZ8, TRZ1, ATZ1, TDZ4, TDZ8, TDZ9, TDZ10,PYZ8, PYZ9, PYZ10 and PYZ14 indicated specific inhibitory activity (inhibition zone > 19mm) against the Gram-negative bacteria Pseudomonas aeruginosa. In the presentinvestigation tested compounds did not posses antifungal activity.Compounds that showed significant antibacterial activity were evaluated for their invivo analgesic activity using tail immersion method in mice and results were compared withthe reference standard drug paracetamol. In case of 2-(1,3-benzothiazol-2-ylsulfanyl)-N-[5-(aryloxymethy)-1,3,4-oxadiazol-2-yl]acetamide the highest activity (76.5% analgesia) wasobserved at 3 h in derivative ODZ10. At first and second hour derivatives OXZ8 and OXZ11belonging to the 2-{(benzo[d]thiazol-2-ylthio)methyl}-5-(aryloxymethyl)-1,3,4-oxadiazolesseries and derivatives TDZ1 and TDZ9 belonging to the 2-(1,3-benzothiazol-2-ylsulfanyl)-N-[5-(aryloxymethyl)-1,3,4-thiadiazol-2-yl]acetamide series exhibited significant analgesicactivity (46.0-76.8%). Among 2-pyrazoline incorporated 2-mercaptobenzothiazoles,derivatives PYZ5, PYZ9, PYZ10 and PYZ14 exhibited potent analgesic activity (55.9 to69.8%) at second and third hour following oral administration.Compounds were evaluated for their anti-inflammatory activity using the carrageenaninduced paw oedema method in rats. At 2 and 3 h compounds ODZ4, ODZ6 and ODZ10belonging to the 2-(1,3-benzothiazol-2-ylsulfanyl)-N-[5-(aryloxymethy)-1,3,4-oxadiazol-2-yl]acetamide series were effective in inhibiting the paw oedema (58.2-68.2%), whencompared with the reference drug diclofenac sodium. In case of 2-{(benzo[d]thiazol-2-ylthio)methyl}-5-(aryloxymethyl)-1,3,4-oxadiazole/triazole and 2-(1,3-benzothiazol-2-ylsulfanyl)-N-[5-(aryloxymethyl)-1,3,4-thiadiazol-2-yl]acetamide series highest activity(81.6%) was found in derivative TDZ4 at 1h after carrageenan injection. Among the 2-pyrazoline incorporated 2-mercaptobenzothiazole analogs highest activity (76.9%) wasobserved at second hour in derivative PYZ14. On the other hand, sulfonyl analogs (PYS1-3)showed weak anti-inflammatory activity at all time interval.Compounds that exhibited higher analgesic and anti-inflammatory profiles in the prementionedanimal models and promising antibacterial activities were further evaluated fortheir ulcerogenic potential. The results indicated low severity index of the tested compoundsODZ10, TDZ4, TDZ9, PYZ9 and PYZ14 ranging from 2.0±0.3 to 3.2±0.7." @default.
• W2888016871 created "2018-08-31" @default.
• W2888016871 creator A5064538743 @default.
• W2888016871 date "2011-06-01" @default.
• W2888016871 modified "2023-09-24" @default.
• W2888016871 title "Synthesis and biological evaluation of some 2-mercaptobenzothiazole derivatives." @default.
• W2888016871 hasPublicationYear "2011" @default.
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