Synthesis of some 1-[(N,N-disubstituted thiocarbamoylthio)acetyl]-3-(2-thienyl)-5-aryl-2-pyrazoline derivatives and investigation of their antibacterial and antifungal activities

Turan-Zitouni G., ÖZDEMİR A., Guven K.

ARCHIV DER PHARMAZIE, cilt.338, sa.2-3, ss.96-104, 2005 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 338 Sayı: 2-3
  • Basım Tarihi: 2005
  • Doi Numarası: 10.1002/ardp.200400935
  • Dergi Adı: ARCHIV DER PHARMAZIE
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Index Chemicus (IC)
  • Sayfa Sayıları: ss.96-104
  • Anahtar Kelimeler: 2-pyrazoline, sodium salts of N,N-disubstituted dithiocarbamoic acids, antibacterial activity, antifungal activity, antituberculosis activity, CARBAMODITHIOIC ACID-ESTERS, ANTI-MRSA ACTIVITY, BICYCLIC PYRAZOLIDINONES, DITHIOCARBAMATE CARBAPENEMS, SUBSTITUTED PYRAZOLINES, RESISTANCE, PHARMACOLOGY, THERAPY, AGENTS
  • Anadolu Üniversitesi Adresli: Evet

Özet

Fourteen new 1-[(N,N-disubstituted thiocarbamoylthio)acetyl]-3-(2-thienyl)-5-aryl-2-pyrazoline derivatives (7a-n) were synthesised by reacting 1-(chloroacetyl)-3-(2-thienyl)-5-aryl-2-pyrazolines (5a-g) and appropriate sodium salts of N,N-disubstituted dithiocarbamoic acids (6a, b). The structures of the synthesised compounds were confirmed by elemental analyses, UV, IR, H-1-NMR and FAB(+)-MS spectral data. Their antibacterial activities against Proteus vulgaris (NRRL B-123), Escherichia coli (NRRL B-3704), Aeromonas hydrophila (Ankara University, Faculty of Veterinary Sciences), Salmonella typhimurium (NRRL B-4420), Streptococcus feacalis (NRRL B-14617), Micrococcus luteus (NRLL B-4375) were investigated and in this investigation, a significant level of activity was illustrated. Antifungal activities of the compounds against Candida albicans and Candida globrata (isolates obtained from Osmangazi Uni. Fac. of Medicine) were found to be inactive. Compounds 7c-n were also evaluated for antituberculosis activity against Mycobacterium tuberculosis H(37)Rv using the BACTEC 460 radiometric system and BACTEC 12B medium. The preliminary results indicated that all of the tested compounds were inactive against the test organism.