Vikas Shirsath - Academia.edu (original) (raw)
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A series of novel title compounds 4a-o has been synthesized through two different synthetic route... more A series of novel title compounds 4a-o has been synthesized through two different synthetic routes. While the first involves the condensation of pyrazole o-aminoester 1 with aryl isothiocyanates 2, the second involves cyciocondensation of alkyl isothiourea ethers of sym-diarylthioureas 5 with 1. The compounds have been evaluated for analgesic, as well as, anti-inflammatory activities in rodents. The lead compound, 4c (LM-22835), exhibits analgesic activity comparable to morphine and aspirin at the dose levels of 10 mg/kg p.o. and 100 mg/kg p.o. In the acetic acid induced writhing test, in mice, it has been found to be superior to aspirin in the rat caudal immersion test. Efforts towards optimization of lead compound 4c have resulted in identifying more active compounds. Compounds 4b, 4c, 4e, 4h, 4i and 40 exhibit antiinflammatory activity superior to aspirin at 100 mg/kg, p.o. in the colton pellet induced granuloma test(rats); compound 40, is also found to be superior to aspirin whe...
ChemInform, 2010
The synthesis of a series of C(8) unsubstituled (lla-h), C(8) substituted (12a-e), 8-mercapto (13... more The synthesis of a series of C(8) unsubstituled (lla-h), C(8) substituted (12a-e), 8-mercapto (13a-e) 1,3-diaryl-2lhioxanthines, as well as, 8-aza-I,3-diaryl-2-thioxanthines 14a-g, through precursors, 5,6-diamino-l,3-diaryl-2-thiouracils 10 has been reported. Recently, the synthesis of a novel series of 6-amino-I,3-diaryl-2-thiouracils 8 under the influence of dry HCI gas has been reported. 14. 15. These compounds are converted to the requisite 5,6-diamino-I,3-diaryl-2-thiouraci ls 10 via reduction of an intermediate 5-nitroso-6-amino-I ,3-diaryl-2-thiouracils 9. Cyclocondensation of 5,6-diamino-2thiouracils 10 with appropriate one carbon donors afford the desired purines 11-13.
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A series of novel title compounds 4a-o has been synthesized through two different synthetic route... more A series of novel title compounds 4a-o has been synthesized through two different synthetic routes. While the first involves the condensation of pyrazole o-aminoester 1 with aryl isothiocyanates 2, the second involves cyciocondensation of alkyl isothiourea ethers of sym-diarylthioureas 5 with 1. The compounds have been evaluated for analgesic, as well as, anti-inflammatory activities in rodents. The lead compound, 4c (LM-22835), exhibits analgesic activity comparable to morphine and aspirin at the dose levels of 10 mg/kg p.o. and 100 mg/kg p.o. In the acetic acid induced writhing test, in mice, it has been found to be superior to aspirin in the rat caudal immersion test. Efforts towards optimization of lead compound 4c have resulted in identifying more active compounds. Compounds 4b, 4c, 4e, 4h, 4i and 40 exhibit antiinflammatory activity superior to aspirin at 100 mg/kg, p.o. in the colton pellet induced granuloma test(rats); compound 40, is also found to be superior to aspirin whe...
ChemInform, 2010
The synthesis of a series of C(8) unsubstituled (lla-h), C(8) substituted (12a-e), 8-mercapto (13... more The synthesis of a series of C(8) unsubstituled (lla-h), C(8) substituted (12a-e), 8-mercapto (13a-e) 1,3-diaryl-2lhioxanthines, as well as, 8-aza-I,3-diaryl-2-thioxanthines 14a-g, through precursors, 5,6-diamino-l,3-diaryl-2-thiouracils 10 has been reported. Recently, the synthesis of a novel series of 6-amino-I,3-diaryl-2-thiouracils 8 under the influence of dry HCI gas has been reported. 14. 15. These compounds are converted to the requisite 5,6-diamino-I,3-diaryl-2-thiouraci ls 10 via reduction of an intermediate 5-nitroso-6-amino-I ,3-diaryl-2-thiouracils 9. Cyclocondensation of 5,6-diamino-2thiouracils 10 with appropriate one carbon donors afford the desired purines 11-13.