Antiparasitic agents. 5. Synthesis and anthelmintic activities of novel 2-heteroaromatic-substituted isothiocyanatobenzoxazoles and -benzothiazoles
Тип публикации: Journal Article
Дата публикации: 1982-08-01
scimago Q1
wos Q1
БС1
SJR: 1.801
CiteScore: 11.5
Impact factor: 6.8
ISSN: 00222623, 15204804
PubMed ID:
7120286
Drug Discovery
Molecular Medicine
Краткое описание
The synthesis and antiparasitic properties of 22 isothiocyanato-2-pyridinylbenzoxazoles and benzothiazoles are described; the preparation and anthelmintic activities of 14 isothiocyanato-2-thienyl-, -furyl-, and -pyrrolylbenzoxazoles are outlined. In mice experimentally infected with Nematospiroides dubius (nematode) and Hymenolepis nana (tapeworm), three derivatives, i.e., 5-isothiocyanato-2-(2-furyl)benzoxazole (34), 5-isothiocyanato-2-(5-methyl-2-furyl)benzoxazole (35), and 5-isothiocyanato-2-(1-methyl-1H-2-pyrroly)benzoxazole (37), show 100% nematocidal activity and two, i.e., 5- and 6-isothiocyanato-2-(3-pyridinyl)benzoxazole (5) and 5- and 6-isothiocyanato-2-(3-pyridinyl)benzthiazole (21), show 10% taeniacidal activity at 0.2% in the diet. Two derivatives (5 and 21) show good nematocidal activity in sheep. Maximum activity requires 3-pyridinyl derivatives for both the benzoxazole and benzothiazole series.
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Haugwitz R. D. et al. Antiparasitic agents. 5. Synthesis and anthelmintic activities of novel 2-heteroaromatic-substituted isothiocyanatobenzoxazoles and -benzothiazoles // Journal of Medicinal Chemistry. 1982. Vol. 25. No. 8. pp. 969-974.
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Haugwitz R. D., Angel R. G., JACOBS G. A., Maurer B. V., Narayanan V. L., Cruthers L., Szanto J. Antiparasitic agents. 5. Synthesis and anthelmintic activities of novel 2-heteroaromatic-substituted isothiocyanatobenzoxazoles and -benzothiazoles // Journal of Medicinal Chemistry. 1982. Vol. 25. No. 8. pp. 969-974.
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TY - JOUR
DO - 10.1021/jm00350a017
UR - https://doi.org/10.1021/jm00350a017
TI - Antiparasitic agents. 5. Synthesis and anthelmintic activities of novel 2-heteroaromatic-substituted isothiocyanatobenzoxazoles and -benzothiazoles
T2 - Journal of Medicinal Chemistry
AU - Haugwitz, R. D.
AU - Angel, R G
AU - JACOBS, G A
AU - Maurer, B V
AU - Narayanan, V L
AU - Cruthers, L.R
AU - Szanto, J.
PY - 1982
DA - 1982/08/01
PB - American Chemical Society (ACS)
SP - 969-974
IS - 8
VL - 25
PMID - 7120286
SN - 0022-2623
SN - 1520-4804
ER -
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@article{1982_Haugwitz,
author = {R. D. Haugwitz and R G Angel and G A JACOBS and B V Maurer and V L Narayanan and L.R Cruthers and J. Szanto},
title = {Antiparasitic agents. 5. Synthesis and anthelmintic activities of novel 2-heteroaromatic-substituted isothiocyanatobenzoxazoles and -benzothiazoles},
journal = {Journal of Medicinal Chemistry},
year = {1982},
volume = {25},
publisher = {American Chemical Society (ACS)},
month = {aug},
url = {https://doi.org/10.1021/jm00350a017},
number = {8},
pages = {969--974},
doi = {10.1021/jm00350a017}
}
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MLA
Скопировать
Haugwitz, R. D., et al. “Antiparasitic agents. 5. Synthesis and anthelmintic activities of novel 2-heteroaromatic-substituted isothiocyanatobenzoxazoles and -benzothiazoles.” Journal of Medicinal Chemistry, vol. 25, no. 8, Aug. 1982, pp. 969-974. https://doi.org/10.1021/jm00350a017.